Ethionamide Boosters: Synthesis, Biological Activity, and Structure-Activity Relationships of a Series of 1,2,4-Oxadiazole EthR Inhibitors
Flipo, Marion Desroses, Matthieu Lecat-Guillet, Nathalie Dirie, Bertrand Carette, Xavier Leroux, Florence Piveteau, Catherine Demirkaya, Fatma Lens, Zoe Rucktooa, Prakash Villeret, Vincent Christophe, Thierry Jeon, Hee Kyoung Locht, Camille Brodin, Priscille Deprez, Benoit Baulard, Alain R. Willand, Nicolas
Journal of Medicinal Chemistry, 2011
https://doi.org/10.1021/jm200076a
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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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
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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
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Ethionamide Boosters: Synthesis, Biological Activity, and Structure-Activity Relationships of a Series of 1,2,4-Oxadiazole EthR Inhibitors 10.1021/jm200076a
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Benzothiazinones Kill Mycobacterium tuberculosis by Blocking Arabinan Synthesis 10.1126/science.1171583
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Discovery of novel N-phenylphenoxyacetamide derivatives as EthR inhibitors and ethionamide boosters by combining high-throughput screening and synthesis. 10.1021/jm300377g
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ORCID: 0000-0003-2050-7389
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Characterization of ERM transactivation domain binding to the ACID/PTOV domain of the Mediator subunit MED25. 10.1093/nar/gkv650
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Structural characterization of binding mode of smoking cessation drugs to nicotinic acetylcholine receptors through study of ligand complexes with acetylcholine-binding protein. 10.1074/jbc.M112.360347
Dimeric α-cobratoxin X-ray structure: localization of intermolecular disulfides and possible mode of binding to nicotinic acetylcholine receptors. 10.1074/jbc.M111.322313
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Crystal structures of the human neurokinin 1 receptor in complex with clinically used antagonists. 10.1038/s41467-018-07939-8
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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
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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
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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
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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
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A facile and rapid synthesis of N-benzyl-2-substituted piperazines 10.1016/j.tetlet.2011.02.011
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A comprehensive analysis of the protein-ligand interactions in crystal structures of Mycobacterium tuberculosis EthR 10.1016/j.bbapap.2018.12.003
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Structural analysis of the interaction between spiroisoxazoline SMARt-420 and the Mycobacterium tuberculosis repressor EthR2 10.1016/j.bbrc.2017.04.074
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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
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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
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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
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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
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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
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A fragment merging approach towards the development of small molecule inhibitors of Mycobacterium tuberculosis EthR for use as ethionamide boosters. 10.1039/c5ob02630j
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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
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Testing chemical and genetic Modulators in Mycobacterium tuberculosis infected cells using phenotypic assays. 10.1007/978-1-4939-2450-9_24
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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
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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
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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
High content screening identifies decaprenyl-phosphoribose 2' epimerase as a target for intracellular antimycobacterial inhibitors. 10.1371/journal.ppat.1000645
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Long-circulating DNA lipid nanocapsules as new vector for passive tumor targeting. 10.1016/j.biomaterials.2009.09.044
Automated HTS/HCS for antivirals using visual HIV full replication assays. 10.1186/1742-4690-6-s2-p82
Benzothiazinones kill Mycobacterium tuberculosis by blocking arabinan synthesis. 10.1126/science.1171583
Automated high-throughput siRNA transfection in raw 264.7 macrophages: a case study for optimization procedure. 10.1177/1087057108328762
Control of M. tuberculosis ESAT-6 secretion and specific T cell recognition by PhoP. 10.1371/journal.ppat.0040033
ESAT-6 from Mycobacterium tuberculosis dissociates from its putative chaperone CFP-10 under acidic conditions and exhibits membrane-lysing activity. 10.1128/jb.00469-07
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Synthesis and antimycobacterial evaluation of benzofurobenzopyran analogues. 10.1016/j.bmc.2006.12.009
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Macro-array and bioinformatic analyses reveal mycobacterial 'core' genes, variation in the ESAT-6 gene family and new phylogenetic markers for the Mycobacterium tuberculosis complex. 10.1099/mic.0.26662-0
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
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
Bacterial artificial chromosome-based comparative genomic analysis identifies Mycobacterium microti as a natural ESAT-6 deletion mutant. 10.1128/iai.70.10.5568-5578.2002
Disruption of HIV-1 integrase-DNA complexes by short 6-oxocytosine-containing oligonucleotides. 10.1021/bi015732y
IRG1 controls immunometabolic host response and restricts intracellular Mycobacterium tuberculosis infection 10.1101/761551
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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A new variant of the Ntn hydrolase fold revealed by the crystal structure of L-aminopeptidase D-ala-esterase/amidase from Ochrobactrum anthropi. 10.1016/s0969-2126(00)00091-5
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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
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florence leroux
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ORCID: 0000-0003-0554-873X
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Xavier Carette
Carette Xavier
ORCID: 0000-0003-4490-5752
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Impact of United States political sanctions on international collaborations and research in Iran