Ethionamide Boosters. 2. Combining Bioisosteric Replacement and Structure-Based Drug Design To Solve Pharmacokinetic Issues in a Series of Potent 1,2,4-Oxadiazole EthR Inhibitors
Flipo, Marion Desroses, Matthieu Lecat-Guillet, Nathalie Villemagne, Baptiste Blondiaux, Nicolas Leroux, Florence Piveteau, Catherine Mathys, Vanessa Flament, Marie-Pierre Siepmann, Juergen Villeret, Vincent Wohlkonig, Alexandre Wintjens, Rene Soror, Sameh H. Christophe, Thierry Jeon, Hee Kyoung Locht, Camille Brodin, Priscille Deprez, Benoit Baulard, Alain R. Willand, Nicolas
Alexandre Wohlkonig
Wohlkonig Alexandre / Wohlkonig
ORCID: 0000-0003-3103-5022
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Baptiste Villemagne
Villemagne Baptiste
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Fragment-Based Optimized EthR Inhibitors with in Vivo Ethionamide Boosting Activity 10.1021/acsinfecdis.9b00277
Camille Locht
Locht Camille
ORCID: 0000-0001-7295-7336
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Priscille Brodin
Brodin Priscille
ORCID: 0000-0003-0991-7344
Email: priscille.brodin@inserm.fr
How can nanoparticles contribute to antituberculosis therapy? 10.1016/j.drudis.2017.01.011
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A Bacterial Toxin with Analgesic Properties: Hyperpolarization of DRG Neurons by Mycolactone 10.3390/toxins9070227
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LppM impact on the colonization of macrophages by Mycobacterium tuberculosis 10.1111/cmi.12619
Phenotypic assays for Mycobacterium tuberculosis infection 10.1002/cyto.a.23129 10.1002/cyto.a.23129.
Reversion of antibiotic resistance in Mycobacterium tuberculosis by spiroisoxazoline SMARt-420 10.1126/science.aag1006
A fragment merging approach towards the development of small molecule inhibitors of Mycobacterium tuberculosis EthR for use as ethionamide boosters 10.1039/c5ob02630j
Khaya grandifoliola C.DC: a potential source of active ingredients against hepatitis C virus in vitro 10.1007/s00705-016-2771-5
Mycobacterium tuberculosis LppM Displays an Original Structure and Domain Composition Linked to a Dual Localization 10.1016/j.str.2016.07.009
Mycolactone The amazing analgesic mycobacterial toxin 10.1051/medsci/20163202007
STAT3 Represses Nitric Oxide Synthesis in Human Macrophages upon Mycobacterium tuberculosis Infection 10.1038/srep29297
2-Carboxyquinoxalines Kill Mycobacterium tuberculosis through Noncovalent Inhibition of DprE1 10.1021/cb5007163
Cytosolic Access of Mycobacterium tuberculosis: Critical Impact of Phagosomal Acidification Control and Demonstration of Occurrence In Vivo 10.1371/journal.ppat.1004650
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High-Content Screening Technology Combined with a Human Granuloma Model as a New Approach To Evaluate the Activities of Drugs against Mycobacterium tuberculosis 10.1128/aac.03705-14
Increased protective efficacy of recombinant BCG strains expressing virulence-neutral proteins of the ESX-1 secretion system 10.1016/j.vaccine.2015.03.083
Plant extracts from Cameroonian medicinal plants strongly inhibit hepatitis C virus infection in vitro 10.3389/fmicb.2015.00438
Polyphenols Inhibit Hepatitis C Virus Entry by a New Mechanism of Action 10.1128/jvi.01473-15
Testing chemical and genetic Modulators in Mycobacterium tuberculosis infected cells using phenotypic assays 10.1007/978-1-4939-2450-9_24
A Microscopic Phenotypic Assay for the Quantification of Intracellular Mycobacteria Adapted for High-throughput/High-content Screening 10.3791/51114
Ligand Efficiency Driven Design of New Inhibitors of Mycobacterium tuberculosis Transcriptional Repressor EthR Using Fragment Growing, Merging, and Linking Approaches 10.1021/jm500422b
Mycobacterial Toxin Induces Analgesia in Buruli Ulcer by Targeting the Angiotensin Pathways 10.1016/j.cell.2014.04.040
Potent antiviral activity of Solanum rantonnetii and the isolated compounds against hepatitis C virus in vitro 10.1016/j.jff.2014.09.022
A novel specific edge effect correction method for RNA interference screenings 10.1093/bioinformatics/btr648
Discovery of Novel N-Phenylphenoxyacetamide Derivatives as EthR Inhibitors and Ethionamide Boosters by Combining High-Throughput Screening and Synthesis 10.1021/jm3003779
Ethionamide Boosters. 2. Combining Bioisosteric Replacement and Structure-Based Drug Design To Solve Pharmacokinetic Issues in a Series of Potent 1,2,4-Oxadiazole EthR Inhibitors 10.1021/jm200825u
The Balance of Apoptotic and Necrotic Cell Death in Mycobacterium tuberculosis Infected Macrophages Is Not Dependent on Bacterial Virulence 10.1371/journal.pone.0047573
Analogous Mechanisms of Resistance to Benzothiazinones and Dinitrobenzamides in Mycobacterium smegmatis 10.1371/journal.pone.0026675
Ethionamide Boosters: Synthesis, Biological Activity, and Structure-Activity Relationships of a Series of 1,2,4-Oxadiazole EthR Inhibitors 10.1021/jm200076a
High-content screening in infectious diseases 10.1016/j.cbpa.2011.05.023
Functional characterization of the Mycobacterium tuberculosis serine/threonine kinase PknJ 10.1099/mic.0.038133-0
High Content Phenotypic Cell-Based Visual Screen Identifies Mycobacterium tuberculosis Acyltrehalose-Containing Glycolipids Involved in Phagosome Remodeling 10.1371/journal.ppat.1001100
High-content imaging of Mycobacterium tuberculosis-infected macrophages: an in vitro model for tuberculosis drug discovery 10.4155/fmc.10.223
Long-circulating DNA lipid nanocapsules as new vector for passive tumor targeting 10.1016/j.biomaterials.2009.09.044
Automated High-Throughput siRNA Transfection in Raw 264.7 Macrophages: A Case Study for Optimization Procedure 10.1177/1087057108328762
Benzothiazinones Kill Mycobacterium tuberculosis by Blocking Arabinan Synthesis 10.1126/science.1171583
High Content Screening Identifies Decaprenyl-Phosphoribose 2 ' Epimerase as a Target for Intracellular Antimycobacterial Inhibitors 10.1371/journal.ppat.1000645
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Control of M-tuberculosis ESAT-6 secretion and specific T cell recognition by PhoP 10.1371/journal.ppat.0040033
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Benzofuro 3,2-f 1 benzopyrans: A new class of antitubercular agents 10.1016/j.bmc.2006.03.033
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High frequency of CD4(+) T cells specific for the TB10.4 protein correlates with protection against Mycobacterium tuberculosis infection 10.1128/iai.02086-05
Inactivation of Rv2525c, a substrate of the twin arginine translocation (Tat) system of Mycobacterium tuberculosis, increases beta-lactam susceptibility and virulence 10.1128/jb.00631-06
Evaluation of vaccines in the EU TB vaccine cluster using a guinea pig aerosol infection model of tuberculosis 10.1016/j.tube.2004.09.009
Functional analysis of early secreted antigenic target-6, the dominant T-cell antigen of Mycobacterium tuberculosis, reveals key residues involved in secretion, complex formation, virulence, and immunogenicity 10.1074/jbc.M503515200
Immunogenic membrane-associated proteins of Mycobacterium tuberculosis revealed by proteomics 10.1099/mic.0.27799-0
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Cell envelope protein PPE68 contributes to Mycobacterium tuberculosis RDI immunogenicity independently of a 10-kilodalton culture filtrate protein and ESAT-6 10.1128/iai.72.4.2170-2176.2004
Enhanced protection against tuberculosis by vaccination with recombinant Mycobacterium microti vaccine that induces T cell immunity against region of difference 1 antigens 10.1086/421468
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CD8(+)-T-cell responses of mycobacterium-infected mice to a newly identified major histocompatibility complex class I-restricted epitope shared by proteins of the ESAT-6 family 10.1128/iai.71.12.7173-7177.2003
Recombinant BCG exporting ESAT-6 confers enhanced protection against tuberculosis 10.1038/nm859
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Disruption of HIV-1 integrase-DNA complexes by short 6-oxocytosine-containing oligonucleotides 10.1021/bi015732y
Loss of RD1 contributed to the attenuation of the live tuberculosis vaccines Mycobacterium bovis BCG and Mycobacterium microti 10.1046/j.1365-2958.2002.03237.x
6-Oxocytidine containing oligonucleotides inhibit the HIV-1 integrase in vitro 10.1081/ncn-100002322
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Inhibition of the human immunodeficiency virus type 1 DNA integration by modified oligonucleotides 10.1023/a:1026631910681
Branched oligonucleotide-intercalator conjugate forming a parallel stranded structure inhibits HIV-1 integrase 10.1016/s0014-5793(99)01350-2
Inhibition of HIV-1 integration by mono- & bi-functionalized triple helix forming oligonucleotides 10.1080/07328319908044831
Optimization of alternate-strand triple helix formation at the 5 '-TpA-3 ' and 5 '-ApT-3 ' junctions 10.1093/nar/27.15.3029
A truncated HIV-1 Tat protein basic domain rapidly translocates through the plasma membrane and accumulates in the cell nucleus 10.1074/jbc.272.25.16010
Mycobacterium tuberculosis inhibits human innate immune responses via the production of TLR2 antagonist glycolipids 10.1073/pnas.1707840114
ArfGAP1 restricts Mycobacterium tuberculosis entry by controlling the actin cytoskeleton 10.15252/embr.201744371
ArfGAP1 restricts Mycobacterium tuberculosis entry by controlling the actin cytoskeleton 10.15252/embr.201744371 10.15252/embr.201744371.
Combination therapy for tuberculosis treatment: pulmonary administration of ethionamide and booster co-loaded nanoparticles 10.1038/s41598-017-05453-3
Cyclipostins and Cyclophostin analogs as promising compounds in the fight against tuberculosis 10.1038/s41598-017-11843-4 10.1038/s41598-017-11843-4.
Fragment-Sized EthR Inhibitors Exhibit Exceptionally Strong Ethionamide Boosting Effect in Whole-Cell Mycobacterium tuberculosis Assays 10.1021/acschembio.7b00091
Host-pathogen systems for early drug discovery against tuberculosis 10.1016/j.mib.2017.11.017 10.1016/j.mib.2017.11.017.
Legionella pneumophila Modulates Mitochondrial Dynamics to Trigger Metabolic Repurposing of Infected Macrophages 10.1016/j.chom.2017.07.020 10.1016/j.chom.2017.07.020. Epub 2017 Aug 31.
Mycobacterium tuberculosis Controls Phagosomal Acidification by Targeting CISH-Mediated Signaling 10.1016/j.celrep.2017.08.101 10.1016/j.celrep.2017.08.101.
Mycobacterium tuberculosis inhibits human innate immune responses via the production of TLR2 antagonist glycolipids 10.1073/pnas.1707840114 10.1073/pnas.1707840114.
Identification of Piperazinylbenzenesulfonamides as New Inhibitors of Claudin-1 Trafficking and Hepatitis C Virus Entry 10.1128/jvi.01982-17
Multiplexed Quantitation of Intraphagocyte Mycobacterium tuberculosis Secreted Protein Effectors 10.1016/j.celrep.2018.03.125
Oxadiazolone derivatives, new promising multi-target inhibitors against M. tuberculosis 10.1016/j.bioorg.2018.08.025
Proteomics of Mycobacterium infection: Moving towards a Better Understanding of Pathogen-Driven immunomodulation 10.3389/fimmu.2018.00086
Synergy between circular bacteriocin AS-48 and ethambutol against Mycobacterium tuberculosis 10.1128/aac.00359-18
The EU approved antimalarial pyronaridine shows antitubercular activity and synergy with rifampicin, targeting RNA polymerase 10.1016/j.tube.2018.08.004
Cyclipostins and Cyclophostin analogs as promising compounds in the fight against tuberculosis 10.1038/s41598-017-11843-4
Cyclodextrin-based nanocarriers containing a synergic drug combination: A potential formulation for pulmonary administration of antitubercular drugs 10.1016/j.ijpharm.2017.05.030
Host-pathogen systems for early drug discovery against tuberculosis 10.1016/j.mib.2017.11.017
Legionella pneumophila Modulates Mitochondrial Dynamics to Trigger Metabolic Repurposing of Infected Macrophages 10.1016/j.chom.2017.07.020
Mycobacterium tuberculosis Controls Phagosomal Acidification by Targeting CISH-Mediated Signaling 10.1016/j.celrep.2017.08.101
Phenotypic assays for Mycobacterium tuberculosis infection 10.1002/cyto.a.23129
A fast, fully automated cell segmentation algorithm for high-throughput and high-content screening 10.1002/cyto.a.20627
Compartmentalized Encapsulation of Two Antibiotics in Porous Nanoparticles: an Efficient Strategy to Treat Intracellular Infections 10.1002/ppsc.201800360
Spatiotemporal Changes of the Phagosomal Proteome in Dendritic Cells in Response to LPS Stimulation 10.1074/mcp.RA119.001316
Mycolactone as Analgesic: Subcutaneous Bioavailability Parameters 10.3389/fphar.2019.00378
Intrinsic Antibacterial Activity of Nanoparticles Made of β-Cyclodextrins Potentiates Their Effect as Drug Nanocarriers against Tuberculosis 10.1021/acsnano.8b07902
Mitochondrial Dynamics and Activity in Legionella-Infected Cells 10.1007/978-1-4939-9048-1_13
Heparin-Binding Hemagglutinin Adhesin (HBHA) Is Involved in Intracytosolic Lipid Inclusions Formation in Mycobacteria 10.3389/fmicb.2018.02258
Dehydrojuncusol, a Natural Phenanthrene Compound Extracted from Juncus maritimus, Is a New Inhibitor of Hepatitis C Virus RNA Replication 10.1128/jvi.02009-18
A novel codrug made of the combination of ethionamide and its potentiating booster: synthesis, self-assembly into nanoparticles and antimycobacterial evaluation 10.1039/C9OB00680J
Could Mycolactone Inspire New Potent Analgesics? Perspectives and Pitfalls 10.3390/toxins11090516
Paradoxical Roles of the MAL/Tirap Adaptor in Pathologies. 10.3389/fimmu.2020.569127
Fragment-Based Optimized EthR Inhibitors with in Vivo Ethionamide Boosting Activity. 10.1021/acsinfecdis.9b00277
Intracellular and in vivo evaluation of imidazo[2,1-b]thiazole-5-carboxamide anti-tuberculosis compounds. 10.1371/journal.pone.0227224
Preclinical assessment of a new live attenuated Mycobacterium tuberculosis Beijing-based vaccine for tuberculosis. 10.1016/j.vaccine.2019.11.085
IRG1 controls immunometabolic host response and restricts intracellular Mycobacterium tuberculosis infection 10.1101/761551
Worms' Antimicrobial Peptides. 10.3390/md17090512
Theaflavins, polyphenols of black tea, inhibit entry of hepatitis C virus in cell culture. 10.1371/journal.pone.0198226
Plant extracts from Cameroonian medicinal plants strongly inhibit hepatitis C virus infection in vitro. 10.3389/fmicb.2015.00488
Discovery of Q203, a potent clinical candidate for the treatment of tuberculosis. 10.1038/nm.3262
Discovery of novel N-phenylphenoxyacetamide derivatives as EthR inhibitors and ethionamide boosters by combining high-throughput screening and synthesis. 10.1021/jm300377g
Shortening the drug discovery pipeline: small molecule high content screening for lead discovery in neglected disease. 10.1186/1753-6561-5-s1-p38
Automated HTS/HCS for antivirals using visual HIV full replication assays. 10.1186/1742-4690-6-s2-p82
Influence of ESAT-6 secretion system 1 (RD1) of Mycobacterium tuberculosis on the interaction between mycobacteria and the host immune system. 10.4049/jimmunol.174.6.3570
Cell microbiology interview 10.1111/cmi.13288
Pathogenomic analyses of Mycobacterium microti, an ESX-1-deleted member of the Mycobacterium tuberculosis complex causing disease in various hosts 10.1099/mgen.0.000505
willand nicolas
nicolas willand
ORCID: 0000-0002-0784-0462
Neuraminidase inhibitors and risk of H5N1 influenza,Les inhibiteurs de neuraminidase face au risque de grippe aviaire 10.1016/s0003-4509(07)90016-4
Unconventional surface plasmon resonance signals reveal quantitative inhibition of transcriptional repressor EthR by synthetic ligands 10.1016/j.ab.2014.02.011
Water-based conditions for the microscale parallel synthesis of bicyclic lactams 10.1016/j.tetlet.2012.11.082
Exploring drug target flexibility using in situ click chemistry: Application to a mycobacterial transcriptional regulator 10.1021/cb100177g
Synthesis of N-(iodophenyl)-amides via an unprecedented Ullmann-Finkelstein tandem reaction 10.1016/j.tetlet.2005.12.022
Synthesis of functionalized 2-isoxazolines as three-dimensional fragments for fragment-based drug discovery 10.1016/j.tetlet.2015.05.035
Efficient, two-step synthesis of N-substituted nortropinone derivatives 10.1016/j.tetlet.2007.05.110
Natural compounds: Leads or ideas? Bioinspired molecules for drug discovery 10.1111/j.1747-0285.2008.00673.x
MALDI imaging techniques dedicated to drug-distribution studies 10.4155/bio.11.88
Solid and solution phase syntheses of the 2-cyanopyrrolidide DPP-IV inhibitor NVP-DPP728 10.1016/S0040-4020(02)00536-7
Original loading and Suzuki conditions for the solid-phase synthesis of biphenyltetrazoles. Application to the first solid-phase synthesis of irbesartan 10.1016/j.tetlet.2008.02.147
Application of Ullmann and Ullmann-Finkelstein reactions for the synthesis of N-aryl-N-(1H-pyrazol-3-yl) acetamide or N-(1-aryl-1H-pyrazol-3-yl) acetamide derivatives and pharmacological evaluation 10.1016/j.ejmech.2011.05.056
A simple reaction to produce small structurally complex and diverse molecules 10.1016/j.tetlet.2004.05.008
Efficient, protection-free Suzuki-Miyaura synthesis of ortho- biphenyltetrazoles 10.1016/j.tetlet.2005.07.082
Structural activation of the transcriptional repressor EthR from Mycobacterium tuberculosis by single amino acid change mimicking natural and synthetic ligands 10.1093/nar/gkr1113
Microwave-assisted synthesis of functionalized spirohydantoins as 3-D privileged fragments for scouting the chemical space 10.1016/j.tetlet.2016.05.065
Ethionamide boosters: Synthesis, biological activity, and structure-activity relationships of a series of 1,2,4-oxadiazole EthR inhibitors 10.1021/jm200076a
Carbohydrate-protein interactions at interfaces: Synthesis of thiolactosyl glycolipids and design of a working model for surface plasmon resonance 10.1039/b210672h
Structural and docking studies of potent ethionamide boosters 10.1107/S0108270113028126
A versatile solid-phase synthesis of 3-aryl-1,2,4-oxadiazolones and analogues 10.1016/j.tetlet.2006.12.050
UFU ('Ullmann-Finkelstein-Ullmann'): a new multicomponent reaction 10.1016/j.tetlet.2006.04.041
Palladium-free Sonogashira-type cross-coupling reaction of bromoisoxazolines or N-alkoxyimidoyl bromides and alkynes 10.1016/j.tetlet.2016.01.070
Tuberculosis: The drug development pipeline at a glance 10.1016/j.ejmech.2012.02.033
Synthesis and structural studies of a novel scaffold for drug discovery: A 4,5-dihydro-3H-spiro[1,5-benzoxazepine-2,4′-piperidine] 10.1016/j.tetlet.2003.11.079
Synthetic EthR inhibitors boost antituberculous activity of ethionamide 10.1038/nm.1950
A facile and rapid synthesis of N-benzyl-2-substituted piperazines 10.1016/j.tetlet.2011.02.011
Ligand efficiency driven design of new inhibitors of mycobacterium tuberculosis transcriptional repressor EthR using fragment growing, merging, and linking approaches 10.1021/jm500422b
Discovery of novel N -phenylphenoxyacetamide derivatives as EthR inhibitors and ethionamide boosters by combining high-throughput screening and synthesis 10.1021/jm300377g
Ethionamide boosters. 2. Combining bioisosteric replacement and structure-based drug design to solve pharmacokinetic issues in a series of potent 1,2,4-oxadiazole EthR inhibitors 10.1021/jm200825u
A comprehensive analysis of the protein-ligand interactions in crystal structures of Mycobacterium tuberculosis EthR 10.1016/j.bbapap.2018.12.003
A novel codrug made of the combination of ethionamide and its potentiating booster: Synthesis, self-assembly into nanoparticles and antimycobacterial evaluation 10.1039/c9ob00680j
Structural analysis of the interaction between spiroisoxazoline SMARt-420 and the Mycobacterium tuberculosis repressor EthR2 10.1016/j.bbrc.2017.04.074
Recent advances in the design of inhibitors of mycobacterial transcriptional regulators to boost thioamides anti-tubercular activity and circumvent acquired-resistance 10.1016/bs.armc.2019.06.003
New active leads for tuberculosis booster drugs by structure-based drug discovery 10.1039/c7ob00910k
Reversion of antibiotic resistance in Mycobacterium tuberculosis by spiroisoxazoline SMARt-420 10.1126/science.aag1006
Efficient analoging around ethionamide to explore thioamides bioactivation pathways triggered by boosters in Mycobacterium tuberculosis 10.1016/j.ejmech.2018.09.038
Intrinsic antibacterial activity of nanoparticles made of β-cyclodextrins potentiates their effect as drug nanocarriers against tuberculosis 10.1021/acsnano.8b07902
Combination therapy for tuberculosis treatment: Pulmonary administration of ethionamide and booster co-loaded nanoparticles 10.1038/s41598-017-05453-3
Fragment-Based Optimized EthR Inhibitors with in Vivo Ethionamide Boosting Activity 10.1021/acsinfecdis.9b00277
Discovery of the first Mycobacterium tuberculosis MabA (FabG1) inhibitors through a fragment-based screening 10.1016/j.ejmech.2020.112440
Microwave-Assisted Suzuki-Miyaura Cross Coupling using Nickel as Catalyst to Rapidly Access to 3-Arylazetidine 10.1002/slct.201702101
Cyclodextrin-based nanocarriers containing a synergic drug combination: A potential formulation for pulmonary administration of antitubercular drugs 10.1016/j.ijpharm.2017.05.030
A fragment-based approach towards the discovery of N-substituted tropinones as inhibitors of Mycobacterium tuberculosis transcriptional regulator EthR2 10.1016/j.ejmech.2019.02.023
Nathalie deboosere
deboosere Nathalie
ORCID: 0000-0002-2873-5485
ArfGAP1 restricts Mycobacterium tuberculosis entry by controlling the actin cytoskeleton. 10.15252/embr.201744371
Mycobacterium tuberculosis Controls Phagosomal Acidification by Targeting CISH-Mediated Signaling. 10.1016/j.celrep.2017.08.101
A Bacterial Toxin with Analgesic Properties: Hyperpolarization of DRG Neurons by Mycolactone. 10.3390/toxins9070227
Phenotypic assays for Mycobacterium tuberculosis infection. 10.1002/cyto.a.23129
Fragment-Sized EthR Inhibitors Exhibit Exceptionally Strong Ethionamide Boosting Effect in Whole-Cell Mycobacterium tuberculosis Assays. 10.1021/acschembio.7b00091
STAT3 Represses Nitric Oxide Synthesis in Human Macrophages upon Mycobacterium tuberculosis Infection. 10.1038/srep29297
LppM impact on the colonization of macrophages by Mycobacterium tuberculosis. 10.1111/cmi.12619
A microscopic phenotypic assay for the quantification of intracellular mycobacteria adapted for high-throughput/high-content screening. 10.3791/51114
Adhesion of human pathogenic enteric viruses and surrogate viruses to inert and vegetal food surfaces. 10.1016/j.fm.2012.04.007
Viral elution and concentration method for detection of influenza A viruses in mud by real-time RT-PCR. 10.1016/j.jviromet.2011.10.013
Comparison of chlorine and peroxyacetic-based disinfectant to inactivate Feline calicivirus, Murine norovirus and Hepatitis A virus on lettuce. 10.1016/j.ijfoodmicro.2011.08.011
Direct detection of highly pathogenic avian influenza A/H5N1 virus from mud specimens. 10.1016/j.jviromet.2011.06.002
Development and validation of a concentration method for the detection of influenza a viruses from large volumes of surface water. 10.1128/aem.02484-10
A predictive microbiology approach for thermal inactivation of Hepatitis A virus in acidified berries. 10.1016/j.fm.2010.05.018
Assessment of the removal and inactivation of influenza viruses H5N1 and H1N1 by drinking water treatment. 10.1016/j.watres.2010.01.013
Intra-laboratory validation of a concentration method adapted for the enumeration of infectious F-specific RNA coliphage, enterovirus, and hepatitis A virus from inoculated leaves of salad vegetables. 10.1016/j.ijfoodmicro.2005.11.007
Modelling effect of physical and chemical parameters on heat inactivation kinetics of hepatitis A virus in a fruit model system. 10.1016/j.ijfoodmicro.2003.10.015
Host-pathogen systems for early drug discovery against tuberculosis. 10.1016/j.mib.2017.11.017
Mycobacterium tuberculosis inhibits human innate immune responses via the production of TLR2 antagonist glycolipids. 10.1073/pnas.1707840114
Cyclipostins and Cyclophostin analogs as promising compounds in the fight against tuberculosis. 10.1038/s41598-017-11843-4
Legionella pneumophila Modulates Mitochondrial Dynamics to Trigger Metabolic Repurposing of Infected Macrophages. 10.1016/j.chom.2017.07.020
Combination therapy for tuberculosis treatment: pulmonary administration of ethionamide and booster co-loaded nanoparticles. 10.1038/s41598-017-05453-3
Host-directed therapies offer novel opportunities for the fight against tuberculosis. 10.1016/j.drudis.2017.05.005
Cyclodextrin-based nanocarriers containing a synergic drug combination: A potential formulation for pulmonary administration of antitubercular drugs. 10.1016/j.ijpharm.2017.05.030
Impact of pe_pgrs33 Gene Polymorphisms on Mycobacterium tuberculosis Infection and Pathogenesis. 10.3389/fcimb.2017.00137
Clofazimine encapsulation in nanoporous silica particles for the oral treatment of antibiotic-resistant Mycobacterium tuberculosis infections. 10.2217/nnm-2016-0364
Reversion of antibiotic resistance in Mycobacterium tuberculosis by spiroisoxazoline SMARt-420. 10.1126/science.aag1006
How can nanoparticles contribute to antituberculosis therapy? 10.1016/j.drudis.2017.01.011
Genome-wide, high-content siRNA screening identifies the Alzheimer's genetic risk factor FERMT2 as a major modulator of APP metabolism. 10.1007/s00401-016-1652-z
Identification of aminopyrimidine-sulfonamides as potent modulators of Wag31-mediated cell elongation in mycobacteria. 10.1111/mmi.13535
Mycobacterium tuberculosis LppM Displays an Original Structure and Domain Composition Linked to a Dual Localization. 10.1016/j.str.2016.07.009
Khaya grandifoliola C.DC: a potential source of active ingredients against hepatitis C virus in vitro. 10.1007/s00705-016-2771-5
[Mycolactone: the amazing analgesic mycobacterial toxin]. 10.1051/medsci/20163202007
A fragment merging approach towards the development of small molecule inhibitors of Mycobacterium tuberculosis EthR for use as ethionamide boosters. 10.1039/c5ob02630j
Polyphenols Inhibit Hepatitis C Virus Entry by a New Mechanism of Action. 10.1128/jvi.01473-15
Plant extracts from Cameroonian medicinal plants strongly inhibit hepatitis C virus infection in vitro. 10.3389/fmicb.2015.00488
Increased protective efficacy of recombinant BCG strains expressing virulence-neutral proteins of the ESX-1 secretion system. 10.1016/j.vaccine.2015.03.083
Cytosolic access of Mycobacterium tuberculosis: critical impact of phagosomal acidification control and demonstration of occurrence in vivo. 10.1371/journal.ppat.1004650
[High content screening in chemical biology: overview and main challenges]. 10.1051/medsci/20153102016
Testing chemical and genetic Modulators in Mycobacterium tuberculosis infected cells using phenotypic assays. 10.1007/978-1-4939-2450-9_24
2-Carboxyquinoxalines kill mycobacterium tuberculosis through noncovalent inhibition of DprE1. 10.1021/cb5007163
High-content screening technology combined with a human granuloma model as a new approach to evaluate the activities of drugs against Mycobacterium tuberculosis. 10.1128/aac.03705-14
Mycobacterial toxin induces analgesia in buruli ulcer by targeting the angiotensin pathways. 10.1016/j.cell.2014.04.040
Ligand efficiency driven design of new inhibitors of Mycobacterium tuberculosis transcriptional repressor EthR using fragment growing, merging, and linking approaches. 10.1021/jm500422b
Discovery of Q203, a potent clinical candidate for the treatment of tuberculosis. 10.1038/nm.3262
The balance of apoptotic and necrotic cell death in Mycobacterium tuberculosis infected macrophages is not dependent on bacterial virulence. 10.1371/journal.pone.0047573
Discovery of novel N-phenylphenoxyacetamide derivatives as EthR inhibitors and ethionamide boosters by combining high-throughput screening and synthesis. 10.1021/jm300377g
Ethionamide boosters. 2. Combining bioisosteric replacement and structure-based drug design to solve pharmacokinetic issues in a series of potent 1,2,4-oxadiazole EthR inhibitors. 10.1021/jm200825u
A novel specific edge effect correction method for RNA interference screenings. 10.1093/bioinformatics/btr648
Analogous mechanisms of resistance to benzothiazinones and dinitrobenzamides in Mycobacterium smegmatis. 10.1371/journal.pone.0026675
High-content screening in infectious diseases. 10.1016/j.cbpa.2011.05.023
Ethionamide boosters: synthesis, biological activity, and structure-activity relationships of a series of 1,2,4-oxadiazole EthR inhibitors. 10.1021/jm200076a
Shortening the drug discovery pipeline: small molecule high content screening for lead discovery in neglected disease. 10.1186/1753-6561-5-s1-p38
High content phenotypic cell-based visual screen identifies Mycobacterium tuberculosis acyltrehalose-containing glycolipids involved in phagosome remodeling. 10.1371/journal.ppat.1001100
High-content imaging of Mycobacterium tuberculosis-infected macrophages: an in vitro model for tuberculosis drug discovery. 10.4155/fmc.10.223
Functional characterization of the Mycobacterium tuberculosis serine/threonine kinase PknJ. 10.1099/mic.0.038133-0
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Large scale screening discovers clofoctol as an inhibitor of SARS-CoV-2 replication that reduces COVID-19-like pathology 10.1101/2021.06.30.450483
Benoit Deprez
Deprez Benoit
ORCID: 0000-0002-2777-4538
Structure-activity relationships of imidazole-derived 2-[ N-carbamoylmethyl-alkylamino]acetic acids, dual binders of human insulin-degrading enzyme 10.1016/j.ejmech.2014.12.005
Imidazole-derived 2-[N-carbamoylmethyl-alkylamino]acetic acids, substrate-dependent modulators of insulin-degrading enzyme in amyloid-β hydrolysis 10.1016/j.ejmech.2014.04.009
Genome-wide, high-content siRNA screening identifies the Alzheimer’s genetic risk factor FERMT2 as a major modulator of APP metabolism 10.1007/s00401-016-1652-z
Unconventional surface plasmon resonance signals reveal quantitative inhibition of transcriptional repressor EthR by synthetic ligands 10.1016/j.ab.2014.02.011
Microwave-assisted synthesis of functionalized spirohydantoins as 3-D privileged fragments for scouting the chemical space 10.1016/j.tetlet.2016.05.065
Access to newly functionalized imidazole derivatives: Efficient synthesis of novel 5-amino-2-thioimidazoles using propylphosphonic anhydride (®T3P) 10.1016/j.tetlet.2015.01.046
In vivo efficacy of microbiota-sensitive coatings for colon targeting: A promising tool for IBD therapy 10.1016/j.jconrel.2014.11.006
Synthesis of functionalized 2-isoxazolines as three-dimensional fragments for fragment-based drug discovery 10.1016/j.tetlet.2015.05.035
Identification of small inhibitory molecules targeting the Bfl-1 Anti-apoptotic protein that alleviates resistance to ABT-737 10.1177/1087057114534070
ADAM30 Downregulates APP-Linked Defects Through Cathepsin D Activation in Alzheimer's Disease 10.1016/j.ebiom.2016.06.002
The bile acid chenodeoxycholic acid increases human brown adipose tissue activity 10.1016/j.cmet.2015.07.002
Kinetic target-guided synthesis in drug discovery and chemical biology: A comprehensive facts and figures survey 10.4155/fmc-2015-0007
Catalytic site inhibition of insulin-degrading enzyme by a small molecule induces glucose intolerance in mice 10.1038/ncomms9250
Mutations in residue 61 of H-Ras p21 protein influence MHC class II presentation 10.1093/intimm/7.2.269
Structural and docking studies of potent ethionamide boosters 10.1107/S0108270113028126
Inhibition of aggrecanases as a therapeutic strategy in osteoarthritis 10.4155/FMC.14.84
Palladium-free Sonogashira-type cross-coupling reaction of bromoisoxazolines or N-alkoxyimidoyl bromides and alkynes 10.1016/j.tetlet.2016.01.070
Characterization of monoclonal antibodies by a fast and easy liquid chromatography-mass spectrometry time-of-flight analysis on culture supernatant 10.1016/j.ab.2015.08.006
Ligand efficiency driven design of new inhibitors of mycobacterium tuberculosis transcriptional repressor EthR using fragment growing, merging, and linking approaches 10.1021/jm500422b
Aggrecanase-2 inhibitors based on the acylthiosemicarbazide zinc-binding group 10.1016/j.ejmech.2013.08.027
Inhibition of the glucose transporter SGLT2 with dapagliflozin in pancreatic alpha cells triggers glucagon secretion 10.1038/nm.3828
Preface [Hot topic: Hit-to-Lead: Driving Forces for the Medicinal Chemist (Guest Editor: Benoit Deprez and Rebecca Deprez-Poulain)] 10.2174/1568026043451159
Trends in Hit-to-Lead: An Update 10.2174/978160805206610603010653
ChemInform Abstract: Convenient Synthesis of 4H-1,2,4-Triazole-3-thiols Using Di-2-pyridylthionocarbonate. 10.1002/chin.200809141
ChemInform Abstract: Efficient Propylphosphonic Anhydride (®T3P) Mediated Synthesis of Benzothiazoles, Benzoxazoles and Benzimidazoles. 10.1002/chin.201235137
ChemInform Abstract: Water-Based Conditions for the Microscale Parallel Synthesis of Bicyclic Lactams. 10.1002/chin.201322132
Parallel synthesis of polysubstituted tetrahydroquinolines 10.1016/s0040-4020(98)00140-9
High-Content Screening in Forward (Phenotypic Screening with Organisms) and Reverse (Structural Screening by NMR) Chemical Genetics 10.1007/978-3-642-19615-7_9
Synthetic vaccines: The mixotope strategy 10.1007/978-94-011-2264-1_339
An ADAM protein as a new actor of the APP metabolism 10.1016/j.jalz.2013.05.315
Lewis acid-induced reaction of homophthalic anhydride with imines: a convenient synthesis of trans-isoquinolonic acids 10.1016/s0040-4039(97)10742-0
The role of epitopes in selective T-cell activation 10.1016/0248-4900(92)90263-z
Long-lasting anti-viral cytotoxic T lymphocytes induced in vivo with chimeric-multirestricted lipopeptides 10.1016/0264-410x(94)00087-4
Combination therapy for tuberculosis treatment: pulmonary administration of ethionamide and booster co-loaded nanoparticles {10.1038/s41598-017-05453-3}
Topical Intestinal Aminoimidazole Agonists of G-Protein-Coupled Bile Acid Receptor 1 Promote Glucagon Like Peptide-1 Secretion and Improve Glucose Tolerance {10.1021/acs.jmedchem.6b01873}
Reversion of antibiotic resistance in Mycobacterium tuberculosis by spiroisoxazoline SMARt-420 {10.1126/science.aag1006}
Identification of novel TACE inhibitors compatible with topical application {10.1016/j.bmc1.2017.02.035}
Discovery and process development of a novel TACE inhibitor for the topical treatment of psoriasis. 10.1016/j.bmc.2017.07.054
Water-based conditions for the microscale parallel synthesis of bicyclic lactams 10.1016/j.tetlet.2012.11.082
Discovery of Novel N-Phenylphenoxyacetamide Derivatives as EthR Inhibitors and Ethionamide Boosters by Combining High-Throughput Screening and Synthesis 10.1021/jm3003779
Drug-to-Genome-to-Drug, Step 2: Reversing Selectivity in a Series of Antiplasmodial Compounds 10.1021/jm201422e
Efficient propylphosphonic anhydride (®T3P) mediated synthesis of benzothiazoles, benzoxazoles and benzimidazoles 10.1016/j.tetlet.2012.03.007
Ethionamide Boosters. 2. Combining Bioisosteric Replacement and Structure-Based Drug Design To Solve Pharmacokinetic Issues in a Series of Potent 1,2,4-Oxadiazole EthR Inhibitors 10.1021/jm200825u
Friedländer synthesis of polysubstituted quinolines and naphthyridines promoted by propylphosphonic anhydride (T3P®) under mild conditions 10.1039/c2nj21043f
Novel selective inhibitors of neutral endopeptidase: discovery by screening and hit-to-lead optimisation 10.1039/c2md00287f
Racemic and diastereoselective construction of indole alkaloids under solvent- and catalyst-free microwave-assisted Pictet-Spengler condensation 10.1039/c2gc16596a
Squaric acid is a suitable building-block in 4C-Ugi reaction: access to original bivalent compounds 10.1016/j.tetlet.2011.11.077
Stereoselective synthesis of enantiopure N-protected-3-arylpiperazines from keto-esters 10.1016/j.tetlet.2012.07.031
Structural activation of the transcriptional repressor EthR from Mycobacterium tuberculosis by single amino acid change mimicking natural and synthetic ligands 10.1093/nar/gkr1113
Structure-Activity Relationships and Blood Distribution of Antiplasmodial Aminopeptidase-1 Inhibitors 10.1021/jm301506h
Tuberculosis: The drug development pipeline at a glance 10.1016/j.ejmech.2012.02.033
A facile and rapid synthesis of N-benzyl-2-substituted piperazines 10.1016/j.tetlet.2011.02.011
Application of Ullmann and Ullmann-Finkelstein reactions for the synthesis of N-aryl-N-(1H-pyrazol-3-yl) acetamide or N-(1-aryl-1H-pyrazol-3-yl) acetamide derivatives and pharmacological evaluation 10.1016/j.ejmech.2011.05.056
Drug to Genome to Drug: Discovery of New Antiplasmodial Compounds 10.1021/jm1014617
Ethionamide Boosters: Synthesis, Biological Activity, and Structure-Activity Relationships of a Series of 1,2,4-Oxadiazole EthR Inhibitors 10.1021/jm200076a
MALDI imaging techniques dedicated to drug-distribution studies 10.4155/bio.11.88
Controlling Plasma Stability of Hydroxamic Acids: A MedChem Toolbox 10.1021/acs.jmedchem.7b01444
Efficient analoging around ethionamide to explore thioamides bioactivation pathways triggered by boosters in Mycobacterium tuberculosis 10.1016/j.ejmech.2018.09.038
Kinetic Target-Guided Synthesis: Reaching the Age of Maturity 10.1021/acs.jmedchem.9b01183
Discovery of novel N -phenylphenoxyacetamide derivatives as EthR inhibitors and ethionamide boosters by combining high-throughput screening and synthesis 10.1021/jm300377g
Rescue of nonsense mutations by amlexanox in human cells 10.1186/1750-1172-7-58
Setting up a bioluminescence resonance energy transfer high throughput screening assay to search for protein/protein interaction inhibitors in mammalian cells 10.3389/fendo.2012.00100
Designing focused chemical libraries enriched in protein-protein interaction inhibitors using machine-learning methods 10.1371/journal.pcbi.1000695
Exploring drug target flexibility using in situ click chemistry: Application to a mycobacterial transcriptional regulator 10.1021/cb100177g
New non-hydroxamic ADAMTS-5 inhibitors based on the 1,2,4-triazole-3-thiol scaffold 10.1016/j.bmcl.2010.08.108
Solvent-free microwave-assisted Meyers' lactamization 10.1039/b924111f
Synthesis of five- and six-membered lactams via solvent-free microwave Ugi reaction 10.1016/j.tetlet.2010.07.021
Ugi reaction for the synthesis of 4-aminopiperidine-4-carboxylic acid derivatives. Application to the synthesis of carfentanil and remifentanil 10.1016/j.tetlet.2010.03.120
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Fenofibrate-loaded PLGA microparticles: Effects on ischemic stroke 10.1016/j.ejps.2008.12.016
Hydroxamates: Relationships between structure and plasma stability 10.1021/jm900648x
Novel non-carboxylic acid retinoids: 1,2,4-Oxadiazol-5-one derivatives 10.1016/j.bmcl.2008.11.040
Synthetic EthR inhibitors boost antituberculous activity of ethionamide 10.1038/nm.1950
Alkylsquarates as key intermediates for the rapid preparation of original drug-inspired compounds 10.2174/138620708784246013
In silico-in vitro screening of protein-protein interactions: Towards the next generation of therapeutics 10.2174/138920108783955218
Natural compounds: Leads or ideas? Bioinspired molecules for drug discovery 10.1111/j.1747-0285.2008.00673.x
Original loading and Suzuki conditions for the solid-phase synthesis of biphenyltetrazoles. Application to the first solid-phase synthesis of irbesartan 10.1016/j.tetlet.2008.02.147
Synthesis of a 200-member library of squaric acid N-hydroxylamide amides 10.1016/j.bmcl.2008.08.025
A library of novel hydroxamic acids targeting the metallo-protease family: Design, parallel synthesis and screening 10.1016/j.bmc.2006.10.010
A versatile solid-phase synthesis of 3-aryl-1,2,4-oxadiazolones and analogues 10.1016/j.tetlet.2006.12.050
Convenient synthesis of 4H-1,2,4-triazole-3-thiols using di-2-pyridylthionocarbonate 10.1016/j.tetlet.2007.09.094
Efficient, two-step synthesis of N-substituted nortropinone derivatives 10.1016/j.tetlet.2007.05.110
Novel selective inhibitors of the zinc plasmodial aminopeptidase PfA-M1 as potential antimalarial agents 10.1021/jm061169b
PDE5 inhibitors: An original access to novel potent arylated analogues of tadalafil 10.1016/j.bmcl.2006.10.069
Synthesis of N-(iodophenyl)-amides via an unprecedented Ullmann-Finkelstein tandem reaction 10.1016/j.tetlet.2005.12.022
UFU ('Ullmann-Finkelstein-Ullmann'): a new multicomponent reaction 10.1016/j.tetlet.2006.04.041
Control of protein-protein interactions: Structure-based discovery of low molecular weight inhibitors of the interactions between Pin1 WW domain and phosphopeptides 10.1021/jm0500119
Efficient, protection-free Suzuki-Miyaura synthesis of ortho- biphenyltetrazoles 10.1016/j.tetlet.2005.07.082
A simple reaction to produce small structurally complex and diverse molecules 10.1016/j.tetlet.2004.05.008
Facts, figures and trends in lead generation 10.2174/1568026043451168
Synthesis and structural studies of a novel scaffold for drug discovery: A 4,5-dihydro-3H-spiro[1,5-benzoxazepine-2,4′-piperidine] 10.1016/j.tetlet.2003.11.079
From hit to lead. Analyzing structure-profile relationships 10.1021/jm010878g
From hit to lead. Combining two complementary methods for focused library design. Application to μ opiate ligands 10.1021/jm010877o
Parallel synthesis of 1,2,4-oxadiazoles from carboxylic acids using an improved, uronium-based, activation 10.1016/S0040-4039(00)02293-0
Parallel synthesis of a library of 1,4-Naphthoquinones and automated screening of potential inhibitors of trypanothione reductase from Trypanosoma cruzi 10.1016/S0960-894X(00)00056-1
Automated parallel synthesis of a tetrahydroisoquinolin-based library: Potential prolyl endopeptidase inhibitors 10.1016/S0960-894X(99)00003-7
Confronting the degeneracy of convergent combinatorial immunogens, or 'mixotopes', with the specificity of recognition of the target sequences 10.1016/S0264-410X(97)00079-0
Combinatorial chemistry: A rational approach to chemical diversity 10.1016/0223-5234(96)80441-7
Comparative efficiency of simple lipopeptide constructs for in vivo induction of virus-specific CTL 10.1016/0264-410X(95)00220-U
Monitoring of a three-step solid phase synthesis involving a Heck reaction using magic angle spinning NMR spectroscopy 10.1016/0040-4020(96)00701-6
Orthogonal combinatorial chemical libraries 10.1021/ja00124a042
Pimelautide or trimexautide as built-in adjuvants associated with an HIV- 1-derived peptide: Synthesis and in vivo induction of antibody and virus- specific cytotoxic T-lymphocyte-mediated response 10.1021/jm00003a009
Vincent Villeret
Villeret Vincent
ORCID: 0000-0003-4504-056X
Crystal structure of human Mediator subunit MED23 10.1038/s41467-018-05967-y
Computational characterization of the binding mode between oncoprotein Ets-1 and DNA-repair enzymes. 10.1002/prot.25578
Ets-1 interacts through a similar binding interface with Ku70 and Poly (ADP-Ribose) Polymerase-1. 10.1080/09168451.2018.1484276
Solution Structure of the N-Terminal Domain of Mediator Subunit MED26 and Molecular Characterization of Its Interaction with EAF1 and TAF7. 10.1016/j.jmb.2017.09.001
Structural basis for haem piracy from host haemopexin by Haemophilus influenzae. 10.1038/ncomms11590
1H, 15N and 13C assignments of the N-terminal domain of the Mediator complex subunit MED26. 10.1007/s12104-016-9673-z
Characterization of ERM transactivation domain binding to the ACID/PTOV domain of the Mediator subunit MED25. 10.1093/nar/gkv650
Conserved Omp85 lid-lock structure and substrate recognition in FhaC. 10.1038/ncomms8452
Virulence regulation with Venus flytrap domains: structure and function of the periplasmic moiety of the sensor-kinase BvgS. 10.1371/journal.ppat.1004700
A Salmonella type three secretion effector/chaperone complex adopts a hexameric ring-like structure. 10.1128/JB.02294-14
Probing the conformation of FhaC with small-angle neutron scattering and molecular modeling. 10.1016/j.bpj.2014.05.025
Ligand efficiency driven design of new inhibitors of Mycobacterium tuberculosis transcriptional repressor EthR using fragment growing, merging, and linking approaches. 10.1021/jm500422b
Structure of the secretion domain of HxuA from Haemophilus influenzae. 10.1107/S174430911302962X
The structural organization of the N-terminus domain of SopB, a virulence factor of Salmonella, depends on the nature of its protein partners. 10.1016/j.bbapap.2013.09.014
The DivJ, CbrA and PleC system controls DivK phosphorylation and symbiosis in Sinorhizobium meliloti. 10.1111/mmi.12347
The Mediator complex subunit MED25 is targeted by the N-terminal transactivation domain of the PEA3 group members. 10.1093/nar/gkt199
The level of Ets-1 protein is regulated by poly(ADP-ribose) polymerase-1 (PARP-1) in cancer cells to prevent DNA damage. 10.1371/journal.pone.0055883
Structural insights into ChpT, an essential dimeric histidine phosphotransferase regulating the cell cycle in Caulobacter crescentus. 10.1107/S1744309112033064
Discovery of novel N-phenylphenoxyacetamide derivatives as EthR inhibitors and ethionamide boosters by combining high-throughput screening and synthesis. 10.1021/jm300377g
Structural activation of the transcriptional repressor EthR from Mycobacterium tuberculosis by single amino acid change mimicking natural and synthetic ligands. 10.1093/nar/gkr1113
Ethionamide boosters. 2. Combining bioisosteric replacement and structure-based drug design to solve pharmacokinetic issues in a series of potent 1,2,4-oxadiazole EthR inhibitors. 10.1021/jm200825u
Purification of SUMO-1 modified IκBα and complex formation with NF-κB. 10.1016/j.pep.2011.06.009
Substrate recognition by the POTRA domains of TpsB transporter FhaC. 10.1111/j.1365-2958.2011.07680.x
Ethionamide boosters: synthesis, biological activity, and structure-activity relationships of a series of 1,2,4-oxadiazole EthR inhibitors. 10.1021/jm200076a
Exploring drug target flexibility using in situ click chemistry: application to a mycobacterial transcriptional regulator. 10.1021/cb100177g
Functional importance of a conserved sequence motif in FhaC, a prototypic member of the TpsB/Omp85 superfamily. 10.1111/j.1742-4658.2010.07881.x
Periplasmic domain of the sensor-kinase BvgS reveals a new paradigm for the Venus flytrap mechanism. 10.1073/pnas.1006267107
Solution structure of the N-terminal transactivation domain of ERM modified by SUMO-1. 10.1016/j.bbrc.2010.07.049
Structure and plasticity of the peptidyl-prolyl isomerase Par27 of Bordetella pertussis revealed by X-ray diffraction and small-angle X-ray scattering. 10.1016/j.jsb.2009.11.007
First structural insights into the TpsB/Omp85 superfamily. 10.1515/bc.2009.099
Phosphorylation of the MET receptor on juxtamembrane tyrosine residue 1001 inhibits its caspase-dependent cleavage. 10.1016/j.cellsig.2009.05.005
Synthetic EthR inhibitors boost antituberculous activity of ethionamide. 10.1038/nm.1950
Crystallization and preliminary X-ray diffraction analysis of the peptidylprolyl isomerase Par27 of Bordetella pertussis. 10.1107/S1744309108024731
Deletion of flagellin's hypervariable region abrogates antibody-mediated neutralization and systemic activation of TLR5-dependent immunity. 10.4049/jimmunol.181.3.2036
Crystallization and preliminary X-ray analysis of a family 19 glycosyl hydrolase from Carica papaya latex. 10.1107/S1744309108007823
Structure-based mechanism of ligand binding for periplasmic solute-binding protein of the Bug family. 10.1016/j.jmb.2007.08.006
Structure of the membrane protein FhaC: a member of the Omp85-TpsB transporter superfamily. 10.1126/science.1143860
Crystal structures of two Bordetella pertussis periplasmic receptors contribute to defining a novel pyroglutamic acid binding DctP subfamily. 10.1016/j.jmb.2007.04.047
Expression and purification in high yield of a functionally active recombinant human Type I inositol(1,4,5)P3 5-phosphatase. 10.1016/j.pep.2007.04.009
Structural analysis of Bordetella pertussis BugE solute receptor in a bound conformation. 10.1107/s0907444906032653
Crystallization and preliminary X-ray diffraction analysis of two extracytoplasmic solute receptors of the DctP family from Bordetella pertussis. 10.1107/S1744309106032982
Secretion signal of the filamentous haemagglutinin, a model two-partner secretion substrate. 10.1111/j.1365-2958.2006.05242.x
The influence of anionic lipids on SHIP2 phosphatidylinositol 3,4,5-trisphosphate 5-phosphatase activity. 10.1016/j.cellsig.2006.05.010
Crystal structure of papaya glutaminyl cyclase, an archetype for plant and bacterial glutaminyl cyclases. 10.1016/j.jmb.2005.12.029
Crystal structure of Bordetella pertussis BugD solute receptor unveils the basis of ligand binding in a new family of periplasmic binding proteins. 10.1016/j.jmb.2005.11.096
Insights into mechanisms of induction and ligands recognition in the transcriptional repressor EthR from Mycobacterium tuberculosis. 10.1016/j.tube.2005.07.005
Crystallization and preliminary X-ray diffraction studies of the glutaminyl cyclase from Carica papaya latex. 10.1107/S1744309104025904
Structure of EthR in a ligand bound conformation reveals therapeutic perspectives against tuberculosis. 10.1016/j.molcel.2004.09.020
Structural analysis of Escherichia coli OpgG, a protein required for the biosynthesis of osmoregulated periplasmic glucans. 10.1016/j.jmb.2004.07.004
The crystal structure of filamentous hemagglutinin secretion domain and its implications for the two-partner secretion pathway. 10.1073/pnas.0400291101
Crystal structures of a psychrophilic metalloprotease reveal new insights into catalysis by cold-adapted proteases. 10.1002/prot.10264
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Crystallographic evidence for the action of potassium, thallium, and lithium ions on fructose-1,6-bisphosphatase. 10.1073/pnas.92.19.8916
Structural aspects of the allosteric inhibition of fructose-1,6-bisphosphatase by AMP: the binding of both the substrate analogue 2,5-anhydro-D-glucitol 1,6-bisphosphate and catalytic metal ions monitored by X-ray crystallography. 10.1021/bi00013a020
Crystal structure of spinach chloroplast fructose-1,6-bisphosphatase at 2.8 A resolution. 10.1021/bi00013a019
Glycine 122 is essential for cooperativity and binding of Mg2+ to porcine fructose-1,6-bisphosphatase. 10.1074/jbc.270.1.54
Methionine-321 in the C-terminal alpha-helix of catabolic ornithine carbamoyltransferase from Pseudomonas aeruginosa is important for positive homotropic cooperativity. 10.1016/0378-1097(94)00465-x
Catabolic ornithine carbamoyltransferase of Pseudomonas aeruginosa. Changes of allosteric properties resulting from modifications at the C-terminus. 10.1111/j.1432-1033.1994.tb18768.x
DNA binding of the cell cycle transcriptional regulator GcrA depends on N6-adenosine methylation in Caulobacter crescentus and other Alphaproteobacteria. 10.1371/journal.pgen.1003541
NMR structure of the human Mediator MED25 ACID domain. 10.1016/j.jsb.2010.10.011
X-ray structure of papaya chitinase reveals the substrate binding mode of glycosyl hydrolase family 19 chitinases. 10.1021/bi800655u
Structural and phylogenetic relationships among plant and animal cystatins. 10.1006/abbi.1998.0875
Juergen Siepmann
Siepmann Juergen
ORCID: 0000-0001-9058-0579
Accelerated ketoprofen release from spray-dried polymeric particles: importance of phase transitions and excipient distribution 10.3109/03639045.2014.908902
Dexamethasone eluting electrodes for cochlear implantation: Effect on residual hearing 10.1179/1754762813y.0000000053
Does PLGA microparticle swelling control drug release? New insight based on single particle swelling studies 10.1016/j.jconrel.2015.06.039
How to easily provide zero order release of freely soluble drugs from coated pellets 10.1016/j.ijpharm.2014.10.071
In vivo efficacy of microbiota-sensitive coatings for colon targeting: A promising tool for IBD therapy 10.1016/j.jconrel.2014.11.006
In-situ forming composite implants for periodontitis treatment: How the formulation determines system performance 10.1016/j.ijpharm.2015.03.026
Mechanistic analysis of PLGA/HPMC-based in-situ forming implants for periodontitis treatment 10.1016/j.ejpb.2015.05.018
Quaternary polymethacrylate-magnesium aluminum silicate films: Water uptake kinetics and film permeability 10.1016/j.ijpharm.2015.05.048
In silico simulation of niacin release from lipid tablets: Theoretical predictions and independent experiments 10.1016/j.jconrel.2013.12.010
In situ forming implants for periodontitis treatment with improved adhesive properties 10.1016/j.ejpb.2014.05.006
Mechanisms Controlling Theophylline Release from Ethanol-Resistant Coated Pellets 10.1007/s11095-013-1194-1
Accelerated ketoprofen release from polymeric matrices: Importance of the homogeneity/heterogeneity of excipient distribution 10.1016/j.ijpharm.2013.09.023
Analysis of Bulk and Hydration Water During Thermal Lysozyme Denaturation Using Raman Scattering 10.1007/s11483-013-9294-3
Application of terahertz pulsed imaging to analyse film coating characteristics of sustained-release coated pellets 10.1016/j.ijpharm.2013.05.039
Characterization and optimization of GMO-based gels with long term release for intraarticular administration 10.1016/j.ijpharm.2013.04.079
Ethanol-resistant ethylcellulose/guar gum coatings - Importance of formulation parameters 10.1016/j.ejpb.2013.07.014
Ethanol-resistant polymeric film coatings for controlled drug delivery 10.1016/j.jconrel.2013.04.001
For the special IJP issue "Poorly soluble drugs" 10.1016/j.ijpharm.2013.05.056
In-silico simulations of advanced drug delivery systems: What will the future offer? 10.1016/j.ijpharm.2013.07.018
Mathematical modeling of drug dissolution 10.1016/j.ijpharm.2013.04.044
PLGA microparticles with zero-order release of the labile anti-Parkinson drug apomorphine 10.1016/j.ijpharm.2013.01.008
PLGAs bearing carboxylated side chains: Novel matrix formers with improved properties for controlled drug delivery 10.1016/j.jconrel.2012.12.024
Predicting drug release from HPMC/lactose tablets 10.1016/j.ijpharm.2012.12.009
Progress in film coating 10.1016/j.ijpharm.2013.10.009
Quaternary polymethacrylate-magnesium aluminum silicate films: Molecular interactions, mechanical properties and tackiness 10.1016/j.ijpharm.2013.10.016
Stability of aqueous polymeric controlled release film coatings 10.1016/j.ijpharm.2013.10.010
Comparative study of vascular prostheses coated with polycyclodextrins for controlled ciprofloxacin release 10.1016/j.carbpol.2012.07.052
Cubic phase-forming dry powders for controlled drug delivery on mucosal surfaces 10.1016/j.jconrel.2011.09.075
Development and evaluation of sustained-release clonidine-loaded PLGA microparticles 10.1016/j.ijpharm.2012.08.006
Drug release from extruded solid lipid matrices: Theoretical predictions and independent experiments 10.1016/j.ejpb.2011.10.002
Ethionamide Boosters. 2. Combining Bioisosteric Replacement and Structure-Based Drug Design To Solve Pharmacokinetic Issues in a Series of Potent 1,2,4-Oxadiazole EthR Inhibitors 10.1021/jm200825u
How Strongly Does Trehalose Interact with Lysozyme in the Solid State? Insights from Molecular Dynamics Simulation and Inelastic Neutron Scattering 10.1021/jp3058096
Impact of the experimental conditions on drug release from parenteral depot systems: From negligible to significant 10.1016/j.ijpharm.2012.04.053
MALDI-TOF MS imaging of controlled release implants 10.1016/j.jconrel.2012.04.017
Modeling of diffusion controlled drug delivery 10.1016/j.jconrel.2011.10.006
Modeling of drug release from delivery systems based on hydroxypropyl methylcellulose (HPMC) 10.1016/j.addr.2012.09.028
Novel preparation techniques for alginate-poloxamer microparticles controlling protein release on mucosal surfaces 10.1016/j.ejps.2011.12.004
Predictability of drug release from cochlear implants 10.1016/j.jconrel.2011.12.032
Sustained release from hot-melt extruded matrices based on ethylene vinyl acetate and polyethylene oxide 10.1016/j.ejpb.2012.08.008
Zinc-alginate microparticles for controlled pulmonary delivery of proteins prepared by spray-drying 10.1016/j.ejpb.2012.01.018
Cast Lipid Implants for Controlled Drug Delivery: Importance of the Tempering Conditions 10.1002/jps.22574
Controlled release implants based on cast lipid blends 10.1016/j.ejps.2011.03.013
Drug release mechanisms from Kollicoat SR:Eudragit NE coated pellets 10.1016/j.ijpharm.2011.02.026
Drug release mechanisms of cast lipid implants 10.1016/j.ejpb.2011.02.011
Drug release mechanisms of compressed lipid implants 10.1016/j.ijpharm.2010.10.048
Dynamic and static curing of ethylcellulose: PVA-PEG graft copolymer film coatings 10.1016/j.ejpb.2011.02.010
Higuchi equation: Derivation, applications, use and misuse 10.1016/j.ijpharm.2011.03.051
In honor of Takeru Higuchi 10.1016/j.ijpharm.2011.07.030
Diffusion-controlled drug delivery systems: calculation of the required composition to achieve desired release profiles 10.1016/s0168-3659(99)00093-0
HPMC-matrices for controlled drug delivery: A new model combining diffusion, swelling, and dissolution mechanisms and predicting the release kinetics 10.1023/a:1018914301328
Calculation of the dimensions of drug-polymer devices based on diffusion parameters 10.1021/js980006a
Modeling plasticizer uptake in aqueous polymer dispersions 10.1016/s0378-5173(97)00390-6
Mechanisms controlling protein release from lipidic implants: Effects of PEG addition 10.1016/j.jconrel.2006.11.001
New insight into the role of polyethylene glycol acting as protein release modifier in lipidic implants 10.1007/s11095-007-9271-y
Recombinant gelatin hydrogels for the sustained release of proteins 10.1016/j.jconrel.2007.03.003
Aqueous HPMCAS coatings: Effects of formulation and processing parameters on drug release and mass transport mechanisms 10.1016/j.ejpb.2005.12.009
Controlled drug release from Gelucire-based matrix pellets: Experiment and theory 10.1016/j.ijpharm.2006.03.006
Drug delivery to the upper small intestine window using gastroretentive technologies 10.1016/j.coph.2006.04.007
Drug release from lipid-based implants: Elucidation of the underlying mass transport mechanisms 10.1016/j.ijpharm.2005.08.030
Drugs acting as plasticizers in polymeric systems: A quantitative treatment 10.1016/j.jconrel.2006.08.016
Effects of the type of release medium on drug release from PLGA-based microparticles: Experiment and theory 10.1016/j.ijpharm.2005.07.030
How porosity and size affect the drug release mechanisms from PLGA-based microparticles 10.1016/j.ijpharm.2005.07.031
Key parameters affecting the initial release (burst) and encapsulation efficiency of peptide-containing poly(lactide-co-glycolide) microparticles 10.1016/j.ijpharm.2006.06.004
Local controlled drug delivery to the brain 10.1016/j.ijpharm.2006.01.038
Local controlled drug delivery to the brain: Mathematical modeling of the underlying mass transport mechanisms 10.1016/j.ijpharm.2005.07.027
Microparticles used as drug delivery systems 10.1007/2882_053
Paclitaxel-loaded microparticles and implants for the treatment of brain cancer: Preparation and physicochemical characterization 10.1016/j.ijpharm.2005.07.028
Programmable implants-From pulsatile to controlled release 10.1016/j.ijpharm.2005.12.051
Sustained release of nanosized complexes of polyethylenimine and anti-TGF-β2 oligonucleotide improves the outcome of glaucoma surgery 10.1016/j.jconrel.2006.02.010
Blends of aqueous polymer dispersions used for pellet coating: Importance of the particle size 10.1016/j.conrel.2005.03.038
How autocatalysis accelerates drug release from PLGA-based microparticles: A quantitative treatment 10.1021/bm050228k
Mobility of model proteins in hydrogels composed of oppositely charged dextran microspheres studied by protein release and fluorescence recovery after photobleaching 10.1016/j.jconrel.2005.09.005
pH-Sensitive polymer blends used as coating materials to control drug release from spherical beads: Elucidation of the underlying mass transport mechanisms 10.1007/s11095-005-5421-2
pH-sensitive polymer blends used as coating materials to control drug release from spherical beads: Importance of the type of core 10.1021/bm0500704
Effect of the size of biodegradable microparticles on drug release: experiment and theory 10.1016/j.jconrel.2004.01.011
Polymer blends used for the aqueous coating of solid dosage forms: importance of the type of plasticizer 10.1016/j.jconrel.2004.05.011
Polymer blends used for the coating of multiparticulates: Comparison of aqueous and organic coating techniques 10.1023/B:PHAM.0000026443.71935.cb
Blends of enteric and GIT-insoluble polymers used for film coating: physicochemical characterization and drug release patterns 10.1016/s0168-3659(03)00155-x
Floating matrix tablets based on low density foam powder: effects of formulation and processing parameters on drug release 10.1016/s0928-0987(02)00223-3
Mathematical modeling of drug release from bioerodible microparticles: effect of gamma-irradiation 10.1016/s0939-6411(03)00104-8
Multiple unit gastroretentive drug delivery systems: a new preparation method for low density microparticles 10.1080/0265204021000058384
Non-degradable microparticles containing a hydrophilic and/or a lipophilic drug: preparation, characterization and drug release modeling 10.1016/s0168-3659(03)00030-0
Pharmaceutical applications of shellac: Moisture-protective and taste-masking coatings and extended-release matrix tablets 10.1081/ddc-120024188
A new mathematical model quantifying drug release from bioerodible microparticles using Monte Carlo simulations 10.1023/a:1021457911533
Floating microparticles based on low density foam powder 10.1016/s0378-5173(02)00241-7
PLGA-based microparticles: elucidation of mechanisms and a new, simple mathematical model quantifying drug release 10.1016/s0928-0987(02)00023-4
The effect of gamma-irradiation on drug release from bioerodible microparticles: a quantitative treatment 10.1016/s0378-5173(02)00188-6
Understanding and predicting drug delivery from hydrophilic matrix tablets using the "sequential layer" model 10.1023/a:1014447102710
Calculation of the dimensions of dosage forms with release controlled by diffusion for in vivo use 10.1016/s0939-6411(00)00139-9
Mathematical modeling of bioerodible, polymeric drug delivery systems 10.1016/s0169-409x(01)00116-8
Modeling of drug release from delivery systems based on hydroxypropyl methylcellulose (HPMC) 10.1016/s0169-409x(01)00112-0
Bimodal drug release achieved with multi-layer matrix tablets: transport mechanisms and device design 10.1016/s0168-3659(00)00334-5
Calculation of the required size and shape of hydroxypropyl methylcellulose matrices to achieve desired drug release profiles 10.1016/s0378-5173(00)00390-2
Hydrophilic matrices for controlled drug delivery: An improved mathematical model to predict the resulting drug release kinetics (the "sequential layer" model) 10.1023/a:1026455822595
pH-independent release of a weakly basic drug from water-insoluble and -soluble matrix tablets 10.1016/s0168-3659(00)00200-5
A new model describing the swelling and drug release kinetics from hydroxypropyl methylcellulose tablets 10.1021/js9802291
Curing of aqueous polymeric film coatings: Importance of the coating level and type of plasticizer 10.1016/j.ejpb.2009.10.007
Deeper insight into the drug release mechanisms in Eudragit RL-based delivery systems 10.1016/j.ijpharm.2010.01.031
Drug release from PLGA-based microparticles: Effects of the "microparticle:bulk fluid" ratio 10.1016/j.ijpharm.2009.09.012
Enzymatically degraded Eurylon 6 HP-PG: ethylcellulose film coatings for colon targeting in inflammatory bowel disease patients 10.1111/j.2042-7158.2010.01165.x
Influence of urea and guanidine hydrochloride on lysozyme stability and thermal denaturation; a correlation between activity, protein dynamics and conformational changes 10.1039/c0cp00602e
Modeling drug release from PVAc/PVP matrix tablets 10.1016/j.jconrel.2009.08.027
Simulated food effects on drug release from ethylcellulose: PVA-PEG graft copolymer-coated pellets 10.3109/03639040903200706
Alginate-poloxamer microparticles for controlled drug delivery to mucosal tissue 10.1016/j.ejpb.2008.12.004
Characterisation of quaternary polymethacrylate films containing tartaric acid, metoprolol free base or metoprolol tartrate 10.1016/j.ejpb.2009.07.010
Characterization of ethylcellulose: starch-based film coatings for colon targeting 10.1080/03639040902858868
Characterization of Moisture-Protective Polymer Coatings Using Differential Scanning Calorimetry and Dynamic Vapor Sorption 10.1002/jps.21429
Colon targeting with bacteria-sensitive films adapted to the disease state 10.1016/j.ejpb.2009.04.003
Development of injection moulded matrix tablets based on mixtures of ethylcellulose and low-substituted hydroxypropylcellulose 10.1016/j.ejps.2009.02.006
Drug release from MCC- and carrageenan-based pellets: Experiment and theory 10.1016/j.ejpb.2009.05.007
Drug release mechanisms from ethylcellulose: PVA-PEG graft copolymer-coated pellets 10.1016/j.ejpb.2008.12.007
Effects of film coating thickness and drug layer uniformity on in vitro drug release from sustained-release coated pellets: A case study using terahertz pulsed imaging 10.1016/j.ijpharm.2009.08.025
Fenofibrate-loaded PLGA microparticles: Effects on ischemic stroke 10.1016/j.ejps.2008.12.016
Importance of glassy-to-rubbery state transitions in moisture-protective polymer coatings 10.1016/j.ejpb.2009.05.001
Improved long term stability of aqueous ethylcellulose film coatings: Importance of the type of drug and starter core 10.1016/j.ijpharm.2008.10.005
Modeling drug release from hot-melt extruded mini-matrices with constant and non-constant diffusivities 10.1016/j.ejpb.2009.06.010
Novel polymeric film coatings for colon targeting: Drug release from coated pellets 10.1016/j.ejps.2009.03.014
Novel polymeric film coatings for colon targeting: How to adjust desired membrane properties 10.1016/j.ijpharm.2008.12.014
Porous pellets as drug delivery system 10.1080/03639040802578103
Prediction of drug release from ethylcellulose coated pellets 10.1016/j.jconrel.2008.12.003
Protection of moisture-sensitive drugs with aqueous polymer coatings: Importance of coating and curing conditions 10.1016/j.ijpharm.2009.05.036
Towards More Realistic In Vitro Release Measurement Techniques for Biodegradable Microparticles 10.1007/s11095-008-9747-4
A novel mathematical model quantifying drug release from lipid implants 10.1016/j.jconrel.2008.03.009
How to improve the storage stability of aqueous polymeric film coatings 10.1016/j.jconrel.2007.10.018
Lipid implants as drug delivery systems 10.1517/17425247.5.3.291
Mathematical modeling of drug delivery 10.1016/j.ijpharm.2008.09.004
pH-sensitive film coatings: Towards a better understanding and facilitated optimization 10.1016/j.ejpb.2007.03.025
PLGA-based drug delivery systems: Importance of the type of drug and device geometry 10.1016/j.ijpharm.2007.10.030
Polymer blends for controlled release coatings 10.1016/j.conrel.2007.09.012
Carrageenan as an efficient drug release modifier for ethylcellulose-coated pharmaceutical dosage forms 10.1021/bm7009587
Cross-linking of chitosan and chitosan/poly(ethylene oxide) beads: A theoretical treatment 10.1016/j.ejpb.2007.02.012
How to adjust desired drug release patterns from ethylcellulose-coated dosage forms 10.1016/j.jconrel.2007.02.003
Mathematical modeling of drug release from lipid dosage forms 10.1016/j.ijpharm.2011.07.015
Methyl-β-cyclodextrin modified vascular prosthesis: Influence of the modification level on the drug delivery properties in different media 10.1016/j.actbio.2010.09.002
Non-coated multiparticulate matrix systems for colon targeting 10.3109/03639045.2011.562214
Peas Starch-Based Film Coatings for Site-Specific Drug Delivery to the Colon 10.1002/app.32802
Preparation and characterization of poly(lactic-co-glycolic acid) microspheres loaded with a labile antiparkinson prodrug 10.1016/j.ijpharm.2011.02.036
Simultaneous controlled vitamin release from multiparticulates: Theory and experiment 10.1016/j.ijpharm.2011.04.013
Unintended potential impact of perfect sink conditions on PLGA degradation in microparticles 10.1016/j.ijpharm.2010.10.054
Bone implants modified with cyclodextrin: Study of drug release in bulk fluid and into agarose gel 10.1016/j.ijpharm.2010.08.035
PLGA implants: How Poloxamer/PEO addition slows down or accelerates polymer degradation and drug release 10.1016/j.jconrel.2017.03.009
Development and evaluation of chitosan and chitosan derivative nanoparticles containing insulin for oral administration 10.3109/03639045.2015.1044904
Professor Alexander T. Florence: An exceptional scientist and man 10.1016/j.ijpharm.2016.10.004
Importance of PLGA microparticle swelling for the control of prilocaine release 10.1016/j.jddst.2015.10.009
Mathematical modeling of controlled drug delivery 10.1016/S0169-409X(01)00111-9
Fatty acids for controlled release applications: A comparison between prilling and solid lipid extrusion as manufacturing techniques 10.1016/j.ejpb.2015.09.011
Towards a better understanding of the different release phases from PLGA microparticles: Dexamethasone-loaded systems 10.1016/j.ijpharm.2016.08.032
Implants for drug substance delivery,Implants pour la délivrance de principes actifs 10.1051/medsci/20173301006
How to adjust dexamethasone mobility in silicone matrices: A quantitative treatment 10.1016/j.ejpb.2015.11.018
Controlled delivery of a new broad spectrum antibacterial agent against colitis: In vitro and in vivo performance 10.1016/j.ejpb.2015.07.012
In vitro release studies of insulin from lipid implants in solution and in a hydrogel matrix mimicking the subcutis 10.1016/j.ejps.2015.10.011
Novel insights into controlled drug release from coated pellets by confocal Raman microscopy 10.1002/jrs.4896
Series Preface 10.1002/9781118573983
Polymer blends for controlled release coatings 10.1016/j.jconrel.2007.09.012
Importance of air bubbles in the core of coated pellets: Synchrotron X-ray microtomography allows for new insights 10.1016/j.jconrel.2016.06.041
Ear Cubes for local controlled drug delivery to the inner ear 10.1016/j.ijpharm.2016.04.003
Physical key properties of antibiotic-free, PLGA/HPMC-based in-situ forming implants for local periodontitis treatment 10.1016/j.ijpharm.2017.02.039
Special JDDST issue in honour of Prof. Dominique Duchêne 10.1016/j.jddst.2015.07.015
Advances in Pharmaceutical Technology: Series Preface 10.1002/9781118734506
Preparation of polymeric fenofibrate formulations with accelerated drug release: Solvent evaporation versus co-grinding 10.1016/j.jddst.2015.07.013
The 6th world meeting on pharmaceutics, biopharmaceutics and pharmaceutical technology (PBP meeting) April 7-10, 2008, Barcelona, Spain 10.1208/s12249-008-9118-9
PEO hot melt extrudates for controlled drug delivery: Importance of the molecular weight 10.1016/j.jddst.2016.09.003
Advances in Pharmaceutical Technology: Series Preface 10.1002/9781118943182
Series Preface 10.1002/9781118444726
Gastroretentive drug delivery systems 10.1517/17425247.3.2.217
Blends of aqueous polymer dispersions used for pellet coating: Importance of the particle size 10.1016/j.jconrel.2005.03.028
Gentamicin-loaded poly(lactic-co-glycolic acid) microparticles for the prevention of maxillofacial and orthopedic implant infections 10.1016/j.msec.2016.03.064
Limited drug solubility can be decisive even for freely soluble drugs in highly swollen matrix tablets 10.1016/j.ijpharm.2017.05.001
When drugs plasticize film coatings: Unusual formulation effects observed with metoprolol and Eudragit RS 10.1016/j.ijpharm.2018.01.014
Hybrid Ear Cubes for local controlled dexamethasone delivery to the inner ear 10.1016/j.ejps.2018.04.045
Often neglected: PLGA/PLA swelling orchestrates drug release: HME implants 10.1016/j.jconrel.2019.05.039
Process and formulation factors affecting drug release from pellets coated with the ethylcellulose- pseudolatex aquacoat 10.1201/9781315369938
Advances in pharmaceutical technology: Series preface 10.1002/9781118895238
Swelling controlled drug delivery systems 10.1007/978-1-4614-0881-9_7
Diffusion controlled drug delivery systems 10.1007/978-1-4614-0881-9_6
In-situ forming implants loaded with chlorhexidine and ibuprofen for periodontal treatment: Proof of concept study in vivo 10.1016/j.ijpharm.2019.118564
Crystalline Polymorphism Emerging From a Milling-Induced Amorphous Form: The Case of Chlorhexidine Dihydrochloride 10.1016/j.xphs.2017.07.003
Coloring of PLGA implants to better understand the underlying drug release mechanisms 10.1016/j.ijpharm.2019.118563
In-situ forming PLGA implants: How additives affect swelling and drug release 10.1016/j.jddst.2019.101180
Chitosan-clay nanocomposite microparticles for controlled drug delivery: Effects of the MAS content and TPP crosslinking 10.1016/j.jddst.2017.05.012
IJP's Editor for the Americas, Australia and New Zealand 10.1016/j.ijpharm.2017.12.017
In vitro and in vivo behavior of ground tadalafil hot-melt extrudates: How the carrier material can effectively assure rapid or controlled drug release 10.1016/j.ijpharm.2017.05.057
Using Milling to Explore Physical States: The Amorphous and Polymorphic Forms of Dexamethasone 10.1021/acs.cgd.7b01664
Controlled release tablets based on HPMC:lactose blends 10.1016/j.jddst.2019.05.028
Hot melt extruded polysaccharide blends for controlled drug delivery 10.1016/j.jddst.2019.101317
Lipids and polymers in pharmaceutical technology: Lifelong companions 10.1016/j.ijpharm.2018.12.080
Preparation and investigation of P28GST-loaded PLGA microparticles for immunomodulation of experimental colitis 10.1016/j.ijpharm.2017.09.037
In-situ forming PLGA implants for intraocular dexamethasone delivery 10.1016/j.ijpharm.2018.07.013
Towards a better understanding of the release mechanisms of caffeine from PLGA microparticles 10.1002/app.48710
Sink conditions do not guarantee the absence of saturation effects 10.1016/j.ijpharm.2019.119009
Eudragit RL-based film coatings: How to minimize sticking and adjust drug release using MAS 10.1016/j.ejpb.2020.01.011
Sincere thanks to Véronique Préat and Thorsteinn Loftsson and a Warm Welcome to Carmen Alvarez-Lorenzo and Juan Manuel Irache 10.1016/j.ijpharm.2020.119056
Mechanistic explanation of the (up to) 3 release phases of PLGA microparticles: Diprophylline dispersions 10.1016/j.ijpharm.2019.118819
Poorly soluble drugs 10.1016/j.ijpharm.2020.119055
Starch-based controlled release matrix tablets: Impact of the type of starch 10.1016/j.jddst.2020.102152
Evaluation of the Efficacy of Dexamethasone-Eluting Electrode Array on the Post-Implant Cochlear Fibrotic Reaction by Three-Dimensional Immunofluorescence Analysis in Mongolian Gerbil Cochlea 10.3390/jcm10153315
Marion Flipo
Flipo Marion
ORCID: 0000-0003-2863-5721
A comprehensive analysis of the protein-ligand interactions in crystal structures of Mycobacterium tuberculosis EthR 10.1016/j.bbapap.2018.12.003
Structural rearrangements occurring upon cofactor binding in the Mycobacterium smegmatis beta-ketoacyl-acyl carrier protein reductase MabA 10.1107/S2059798318002917
Combination therapy for tuberculosis treatment: pulmonary administration of ethionamide and booster co-loaded nanoparticles 10.1038/s41598-017-05453-3
Reversion of antibiotic resistance in Mycobacterium tuberculosis by spiroisoxazoline SMARt-420 10.1126/science.aag1006
Microwave-assisted synthesis of functionalized spirohydantoins as 3-D privileged fragments for scouting the chemical space 10.1016/j.tetlet.2016.05.065
Synthesis of functionalized 2-isoxazolines as three-dimensional fragments for fragment-based drug discovery 10.1016/j.tetlet.2015.05.035
Imidazole-derived 2-[N-carbamoylmethyl-alkylamino]acetic acids, substrate-dependent modulators of insulin-degrading enzyme in amyloid-beta hydrolysis 10.1016/j.ejmech.2014.04.009
Ligand Efficiency Driven Design of New Inhibitors of Mycobacterium tuberculosis Transcriptional Repressor EthR Using Fragment Growing, Merging, and Linking Approaches 10.1021/jm500422b
Unconventional surface plasmon resonance signals reveal quantitative inhibition of transcriptional repressor EthR by synthetic ligands 10.1016/j.ab.2014.02.011
On the Mechanism of Degradation of Oxytocin and its Analogues in Aqueous Solution 10.1002/bip.22260
Discovery of Novel N-Phenylphenoxyacetamide Derivatives as EthR Inhibitors and Ethionamide Boosters by Combining High-Throughput Screening and Synthesis 10.1021/jm3003779
Ethionamide Boosters. 2. Combining Bioisosteric Replacement and Structure-Based Drug Design To Solve Pharmacokinetic Issues in a Series of Potent 1,2,4-Oxadiazole EthR Inhibitors 10.1021/jm200825u
Structure-Activity Relationships and Blood Distribution of Antiplasmodial Aminopeptidase-1 Inhibitors 10.1021/jm301506h
Tuberculosis: The drug development pipeline at a glance 10.1016/j.ejmech.2012.02.033
Ethionamide Boosters: Synthesis, Biological Activity, and Structure-Activity Relationships of a Series of 1,2,4-Oxadiazole EthR Inhibitors 10.1021/jm200076a
Hydroxamates: Relationships between Structure and Plasma Stability 10.1021/jm900648x
A library of novel hydroxamic acids targeting the metallo-protease family: Design, parallel synthesis and screening 10.1016/j.bmc.2006.10.010
Novel selective inhibitors of the zinc plasmodial aminopeptidase PfA-M1 as potential antimalarial agents 10.1021/jm061169b
Design, synthesis and antimalarial activity of novel, quinoline-based, zinc metallo-aminopeptidase inhibitors 10.1016/S0960-894X(03)00550-X
Intrinsic Antibacterial Activity of Nanoparticles Made of β-Cyclodextrins Potentiates Their Effect as Drug Nanocarriers against Tuberculosis 10.1021/acsnano.8b07902
A fragment-based approach towards the discovery of N-substituted tropinones as inhibitors of Mycobacterium tuberculosis transcriptional regulator EthR2 10.1016/j.ejmech.2019.02.023
Recent advances in the design of inhibitors of mycobacterial transcriptional regulators to boost thioamides anti-tubercular activity and circumvent acquired-resistance 10.1016/bs.armc.2019.06.003
Fragment-Based Optimized EthR Inhibitors with in Vivo Ethionamide Boosting Activity 10.1021/acsinfecdis.9b00277
Discovery of the first Mycobacterium tuberculosis MabA (FabG1) inhibitors through a fragment-based screening 10.1016/j.ejmech.2020.112440
florence leroux
leroux florence
ORCID: 0000-0003-0554-873X
Synthetic EthR inhibitors boost antituberculous activity of ethionamide 10.1038/NM.1950
Designing Focused Chemical Libraries Enriched in Protein-Protein Interaction Inhibitors using Machine-Learning Methods 10.1371/JOURNAL.PCBI.1000695
Synthesis of a 200-member library of squaric acid N-hydroxylamide amides (vol 18, pg 4968, 2008) 10.1016/J.BMCL.2008.08.116
New non-hydroxamic ADAMTS-5 inhibitors based on the 1,2,4-triazole-3-thiol scaffold 10.1016/J.BMCL.2010.08.108
Ethionamide Boosters: Synthesis, Biological Activity, and Structure-Activity Relationships of a Series of 1,2,4-Oxadiazole EthR Inhibitors 10.1021/JM200076A
Drug-to-Genome-to-Drug, Step 2: Reversing Selectivity in a Series of Antiplasmodial Compounds 10.1021/JM201422E
Drug to Genome to Drug: Discovery of New Antiplasmodial Compounds 10.1021/JM1014617
Ethionamide Boosters. 2. Combining Bioisosteric Replacement and Structure-Based Drug Design To Solve Pharmacokinetic Issues in a Series of Potent 1,2,4-Oxadiazole EthR Inhibitors 10.1021/JM200825U
Discovery of Novel N-Phenylphenoxyacetamide Derivatives as EthR Inhibitors and Ethionamide Boosters by Combining High-Throughput Screening and Synthesis 10.1021/JM3003779
Novel selective inhibitors of neutral endopeptidase: discovery by screening and hit-to-lead optimisation 10.1039/C2MD00287F
Structure-Activity Relationships and Blood Distribution of Antiplasmodial Aminopeptidase-1 Inhibitors 10.1021/JM301506H
Imidazole-derived 2-[N-carbamoylmethyl-alkylamino]acetic acids, substrate-dependent modulators of insulin-degrading enzyme in amyloid-beta hydrolysis 10.1016/J.EJMECH.2014.04.009
Inhibition of aggrecanases as a therapeutic strategy in osteoarthritis 10.4155/FMC.14.84
Identification of Small Inhibitory Molecules Targeting the Bfl-1 Anti-Apoptotic Protein That Alleviates Resistance to ABT-737 10.1177/1087057114534070
Aggrecanase-2 inhibitors based on the acylthiosemicarbazide zinc-binding group 10.1016/J.EJMECH.2013.08.027
Ligand Efficiency Driven Design of New Inhibitors of Mycobacterium tuberculosis Transcriptional Repressor EthR Using Fragment Growing, Merging, and Linking Approaches 10.1021/JM500422B
Topical Intestinal Aminoimidazole Agonists of G-Protein-Coupled Bile Acid Receptor 1 Promote Glucagon Like Peptide-1 Secretion and Improve Glucose Tolerance 10.1021/ACS.JMEDCHEM.6B01873
Structure-activity relationships of imidazole-derived 2-[N-carbamoylmethyl-alkylamino]acetic acids, dual binders of human insulin-degrading enzyme 10.1016/J.EJMECH.2014.12.005
Genome-wide, high-content siRNA screening identifies the Alzheimer's genetic risk factor FERMT2 as a major modulator of APP metabolism 10.1007/S00401-016-1652-Z
Catalytic site inhibition of insulin-degrading enzyme by a small molecule induces glucose intolerance in mice 10.1038/NCOMMS9250
ADAM30 Downregulates APP-Linked Defects Through Cathepsin D Activation in Alzheimer's Disease 10.1016/J.EBIOM.2016.06.002
Fragment-Based Optimized EthR Inhibitors with in Vivo Ethionamide Boosting Activity 10.1021/ACSINFECDIS.9B00277
Drug Target Engagement Using Coupled Cellular Thermal Shift Assay-Acoustic Reverse-Phase Protein Array 10.1177/2472555219897256
Controlling Plasma Stability of Hydroxamic Acids: A MedChem Toolbox 10.1021/ACS.JMEDCHEM.7B01444
A fragment-based approach towards the discovery of N-substituted tropinones as inhibitors of Mycobacterium tuberculosis transcriptional regulator EthR2 10.1016/J.EJMECH.2019.02.023
BIN1 recovers tauopathy-induced long-term memory deficits in mice and interacts with Tau through Thr(348) phosphorylation 10.1007/S00401-019-02017-9
Identification of ebselen as a potent inhibitor of insulin degrading enzyme by a drug repurposing screening 10.1016/J.EJMECH.2019.06.057
HIGH-PERFORMANCE LIQUID-CHROMATOGRAPHIC DETERMINATION OF CYCLIC 3',5'-AMP WITH FLUORESCENCE DETECTION - VASOACTIVE INTESTINAL PEPTIDE-INDUCED MODIFICATION OF ITS CONCENTRATION IN NEUROBLASTOMA-CELLS 10.1016/0378-4347(94)80086-3
A NEW VASOACTIVE-INTESTINAL-PEPTIDE ANTAGONIST DISCRIMINATES VIP RECEPTORS ON GUINEA-PIG TRACHEA AND HUMAN NEUROBLASTOMA-CELLS 10.1016/0167-0115(94)90044-2
Tracheal Relaxant Effect of Triazine Derivatives: Correlation with Phosphodiesterase 4 Inhibitory Activity 10.1211/146080899128734613
Use of a low-density microarray for studying gene expression patterns induced by hepatotoxicants on primary cultures of rat hepatocytes 10.1093/TOXSCI/KFG196
High-Throughput Image-Based Aggresome Quantification 10.1177/2472555220919708
Matthieu Desroses
Desroses Matthieu
ORCID: 0000-0003-4152-3855
Synthesis of Unsymmetrical Dialkoxy Quinazolines. 10.1002/chin.200510156
A microwave-assisted, propylphosphonic anhydride (T3P®) mediated one-pot Fischer indole synthesis 10.1016/j.tetlet.2011.06.053
Sugar-based ethenyl ethers: stereoselective dipolar cycloadditions of nitrile oxides 10.1016/s0957-4166(02)00709-7
Synthesis of sugar-based ethenyl ethers through a vinyl bis-sulfone methodology 10.1016/s0040-4020(03)00661-6
Crystal structure, biochemical and cellular activities demonstrate separate functions of MTH1 and MTH2 10.1038/ncomms8871
Synthetic EthR inhibitors boost antituberculous activity of ethionamide 10.1038/nm.1950
A facile and efficient synthesis of tetrahydro-β-carbolines 10.1016/j.tetlet.2013.04.107
A Convenient Microwave-Assisted Propylphosphonic Anhydride (T3P ® ) Mediated One-Pot Pyrazolone Synthesis 10.1002/ejoc.201300380
Derivatives of Iressa, a Specific Epidermal Growth Factor Receptor Inhibitor, are Powerful Apoptosis Inducers in PC3 Prostatic Cancer Cells 10.1002/cmdc.200600128
DXR Inhibition by Potent Mono- and Disubstituted Fosmidomycin Analogues 10.1021/jm4006498
Crystal structure of human MTH1 and the 8-oxo-dGMP product complex 10.1016/j.febslet.2011.07.017
Exploring Drug Target Flexibility Usingin SituClick Chemistry: Application to a Mycobacterial Transcriptional Regulator 10.1021/cb100177g
dUTPase inhibition augments replication defects of 5-Fluorouracil 10.18632/oncotarget.15785
Vinylic MIDA Boronates: New Building Blocks for the Synthesis of Aza-Heterocycles 10.1002/chem.201406549
Discovery of NovelN-Phenylphenoxyacetamide Derivatives as EthR Inhibitors and Ethionamide Boosters by Combining High-Throughput Screening and Synthesis 10.1021/jm300377g
Ethionamide Boosters: Synthesis, Biological Activity, and Structure−Activity Relationships of a Series of 1,2,4-Oxadiazole EthR Inhibitors 10.1021/jm200076a
Ethionamide Boosters. 2. Combining Bioisosteric Replacement and Structure-Based Drug Design To Solve Pharmacokinetic Issues in a Series of Potent 1,2,4-Oxadiazole EthR Inhibitors 10.1021/jm200825u
MTH1 inhibition eradicates cancer by preventing sanitation of the dNTP pool 10.1038/nature13181
Reversion of antibiotic resistance in Mycobacterium tuberculosis by spiroisoxazoline SMARt-420 10.1126/science.aag1006
Data from: Reversion of antibiotic resistance in Mycobacterium tuberculosis by spiroisoxazoline SMARt-420 10.5061/DRYAD.MB463
Structural analysis of the interaction between spiroisoxazoline SMARt-420 and the Mycobacterium tuberculosis repressor EthR2 10.1016/j.bbrc.2017.04.074
A new concise synthesis of 2,3-dihydroquinazolin-4(1H)-one derivatives 10.1039/c3nj00618b
Structure–metabolism-relationships in the microsomal clearance of piperazin-1-ylpyridazines 10.1039/C7MD00230K
The Next Step Forward in Ubiquitin-Specific Protease 7 Selective Inhibition. 10.1016/j.chembiol.2017.12.003
Piperazin-1-ylpyridazine Derivatives Are a Novel Class of Human dCTP Pyrophosphatase 1 Inhibitors. 10.1021/acs.jmedchem.7b00182
BCG_BDM41906.fastq 10.5061/dryad.mb463/2
STAT3 differential scanning fluorimetry and differential scanning light scattering assays: Addressing a missing link in the characterization of STAT3 inhibitor interactions 10.1016/j.jpba.2018.07.018
Validating Signal Transducer and Activator of Transcription (STAT) Protein–Inhibitor Interactions Using Biochemical and Cellular Thermal Shift Assays 10.1021/acschembio.0c00046
Development of a chemical probe against NUDT15 10.1038/s41589-020-0592-z
Sameh Soror
Soror Sameh / Sameh H. Soror / Sameh Soror
ORCID: 0000-0001-6474-8884
Discovery, Structure-Activity Relationship, and Binding Mode of an Imidazo[1,2-a]pyridine Series of Autotaxin Inhibitors. 10.1021/acs.jmedchem.7b00647
Design, synthesis, assessment, and molecular docking of novel pyrrolopyrimidine (7-deazapurine) derivatives as non-nucleoside hepatitis C virus NS5B polymerase inhibitors. 10.1016/j.bmc.2016.03.046
Novel antiviral compounds against gastroenteric viral infections. 10.1002/ardp.201400387
Ligand efficiency driven design of new inhibitors of Mycobacterium tuberculosis transcriptional repressor EthR using fragment growing, merging, and linking approaches. 10.1021/jm500422b
Probing the N-terminal β-sheet conversion in the crystal structure of the human prion protein bound to a nanobody. 10.1021/ja407527p
High-resolution structure of a papaya plant-defense barwin-like protein solved by in-house sulfur-SAD phasing. 10.1107/s0907444913018015
Expression, purification, characterization, and solution nuclear magnetic resonance study of highly deuterated yeast cytochrome C peroxidase with enhanced solubility. 10.1021/bi400220w
A novel expression system for production of soluble prion proteins in E. coli. 10.1186/1475-2859-11-6
Structural activation of the transcriptional repressor EthR from Mycobacterium tuberculosis by single amino acid change mimicking natural and synthetic ligands. 10.1093/nar/gkr1113
Ethionamide boosters. 2. Combining bioisosteric replacement and structure-based drug design to solve pharmacokinetic issues in a series of potent 1,2,4-oxadiazole EthR inhibitors. 10.1021/jm200825u
Crystallization and preliminary X-ray diffraction analysis of kanamycin-binding β-lactamase in complex with its ligand. 10.1107/s1744309111013832
Combining in-situ proteolysis and microseed matrix screening to promote crystallization of PrPc-nanobody complexes. 10.1093/protein/gzr017
Crystallization and preliminary X-ray diffraction analysis of a specific VHH domain against mouse prion protein. 10.1107/s1744309110042168
A llama-derived gelsolin single-domain antibody blocks gelsolin-G-actin interaction. 10.1007/s00018-010-0266-1
A cold-active esterase of Streptomyces coelicolor A3(2): from genome sequence to enzyme activity. 10.1007/s10295-007-0224-6
Mining the genome sequence for novel enzyme activity: characterisation of an unusual member of the hormone-sensitive lipase family of esterases from the genome of Streptomyces coelicolor A3 (2). 10.1093/protein/gzp009
Evaluation of novel pyrrolopyrimidine derivatives as antiviral against gastroenteric viral infections 10.1016/j.ejps.2018.10.022
Inflammasome Genes’ Polymorphisms in Egyptian Chronic Hepatitis C Patients: Influence on Vulnerability to Infection and Response to Treatment 10.1155/2019/3273645
Structural evidence for the critical role of the prion protein hydrophobic region in forming an infectious prion 10.1371/journal.ppat.1008139
1H-Imidazole-2,5-Dicarboxamides as NS4A Peptidomimetics: Identification of a New Approach to Inhibit HCV-NS3 Protease 10.3390/biom10030479
1H-Imidazole-2,5-Dicarboxamides as NS4A Peptidomimetics: Identification of a New Venue to Inhibit HCV-NS3 Protease 10.20944/preprints202001.0279.v1
Targeting NUPR1 for Cancer Treatment: A Risky Endeavor 10.2174/1568009620666200703152523
Revealing the Potential Application of EC-Synthetic Retinoid Analogues in Anticancer Therapy 10.3390/molecules26020506
Restoring NK cells functionality via cytokine activation enhances cetuximab-mediated NK-cell ADCC: A promising therapeutic tool for HCC patients 10.1016/j.molimm.2021.07.008