Ligand Efficiency Driven Design of New Inhibitors of Mycobacterium tuberculosis Transcriptional Repressor EthR Using Fragment Growing, Merging, and Linking Approaches
Villemagne, Baptiste Villemagne, Baptiste Flipo, Marion Flipo, Marion Blondiaux, Nicolas Blondiaux, Nicolas Crauste, Celine Crauste, Celine Malaquin, Sandra Malaquin, Sandra Leroux, Florence Leroux, Florence Piveteau, Catherine Piveteau, Catherine Villeret, Vincent Villeret, Vincent Brodin, Priscille Brodin, Priscille Villoutreix, Bruno O. Villoutreix, Bruno O. Sperandio, Olivier Sperandio, Olivier Soror, Sameh H. Soror, Sameh H. Wohlkoenig, Alexandre Wohlkoenig, Alexandre Wintjens, Rene Wintjens, Rene Deprez, Benoit Deprez, Benoit Baulard, Alain R. Baulard, Alain R. Willand, Nicolas Willand, Nicolas
Journal of medicinal chemistry, 2014-6
https://doi.org/10.1021/jm500422b
Alexandre Wohlkonig
Wohlkonig Alexandre / Wohlkonig
ORCID: 0000-0003-3103-5022
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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
A general protocol for the generation of Nanobodies for structural biology. 10.1038/nprot.2014.039
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Baptiste Villemagne
Villemagne Baptiste
ORCID: 0000-0002-8416-5253
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Unconventional surface plasmon resonance signals reveal quantitative inhibition of transcriptional repressor EthR by synthetic ligands 10.1016/j.ab.2014.02.011
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Fragment-Based Optimized EthR Inhibitors with in Vivo Ethionamide Boosting Activity 10.1021/acsinfecdis.9b00277
Priscille Brodin
Brodin Priscille
ORCID: 0000-0003-0991-7344
Email: priscille.brodin@inserm.fr
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willand nicolas
nicolas willand
ORCID: 0000-0002-0784-0462
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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
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
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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
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
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Host-directed therapies offer novel opportunities for the fight against tuberculosis. 10.1016/j.drudis.2017.05.005
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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
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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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Increased protective efficacy of recombinant BCG strains expressing virulence-neutral proteins of the ESX-1 secretion system. 10.1016/j.vaccine.2015.03.083
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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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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
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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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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
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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
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Synthesis and antimycobacterial evaluation of benzofurobenzopyran analogues. 10.1016/j.bmc.2006.12.009
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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
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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
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Discovery of the first Mycobacterium tuberculosis MabA (FabG1) inhibitors through a fragment-based screening 10.1016/j.ejmech.2020.112440
olivier sperandio
sperandio olivier
ORCID: 0000-0001-6610-2729
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Villoutreix Bruno
ORCID: 0000-0002-6456-7730
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Targeting the Proangiogenic VEGF-VEGFR Protein-Protein Interface with Drug-like Compounds by In Silico and In Vitro Screening 10.1016/J.CHEMBIOL.2011.10.016
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Genetic, molecular and functional analysis of complement factor I deficiency 10.1016/J.MOLIMM.2007.06.033
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Two Clusters of Charged Residues Located in the Electropositive Face of the Von Willebrand Factor A1 Domain Are Essential for Heparin Binding † 10.1021/BI020044F
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Characterization and Structural Impact of Five Novel PROS1 Mutations in Eleven Protein S-deficient Families 10.1055/S-0037-1616741
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Factor VIII Inhibitors in Two Families with Mild Haemophilia A: Structural Analysis of the Mutations 10.1159/000054143
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Prothrombin deficiency caused by compound heterozygosity for two novel mutations in the prothrombin gene associated with a bleeding tendency 10.1055/S-0037-1612584
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The N-terminal Epidermal Growth Factor-like Domain of Coagulation Factor IX 10.1074/JBC.M205930200
Defining the Factor Xa-binding Site on Factor Va by Site-directed Glycosylation 10.1074/JBC.M205609200
Antithrombin Phe229Leu: a new homozygous variant leading to spontaneous antithrombin polymerization in vivo associated with severe childhood thrombosis 10.1182/BLOOD-2002-11-3391
Functional analysis of the EGF-like domain mutations Pro55Ser and Pro55Leu, which cause mild hemophilia B 10.1046/J.1538-7836.2003.00187.X
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Structural basis for type I and type II deficiencies of antithrombotic plasma protein C: Patterns revealed by three-dimensional molecular modelling of mutations of the protease domain 10.1002/PROT.340180407
Analysis of protein S C4b-binding protein interactions by homology modeling and inhibitory antibodies 10.1021/BI00203A003
A structural model for the prostate disease marker, human prostate-specific antigen 10.1002/PRO.5560031116
A Two-Allele Polymorphism in Protein C Inhibitor with Varying Frequencies in Different Ethnic Populations 10.1055/S-0038-1650222
Mutations in a potential phospholipid binding loop in the C2 domain of factor V affecting the assembly of the prothrombinase complex 10.1097/00001721-200011010-00010
Partial Glycosylation of Asn 2181 in Human Factor V as a Cause of Molecular and Functional Heterogeneity. Modulation of Glycosylation Efficiency by Mutagenesis of the Consensus Sequence for N-Linked Glycosylation † 10.1021/BI991165R
Amino acid residues in thrombin-sensitive region and first epidermal growth factor domain of vitamin K-dependent protein S determining specificity of the activated protein C cofactor function 10.1074/JBC.273.42.27449
Mutations within the cyclooxygenase-1 gene in aspirin non-responders with recurrence of stroke 10.1016/J.THROMRES.2003.12.005
Structural modeling and electrostatic properties of aspartate transcarbamylase fromSaccharomyces cerevisiae 10.1002/PROT.340190307
Probing the activation of protein C by the thrombin-thrombomodulin complex using structural analysis, site-directed mutagenesis, and computer modeling 10.1002/(SICI)1097-0134(19990501)35:2<218::AID-PROT8>3.0.CO;2-2
Structural investigation of the A domains of human blood coagulation factor V by molecular modeling 10.1002/PRO.5560070607
Investigation of C4b-binding protein by molecular modeling 10.1016/S0161-5890(98)90569-7
Molecular Models for the two Discoidin Domains of Human Blood Coagulation Factor V 10.1007/S008940050084
Interspecies Loop Grafting in the Protease Domain of Human Protein C Yielding Enhanced Catalytic and Anticoagulant Activity 10.1055/S-0037-1614332
Calcium binding to tandem repeats of EGF-like modules. Expression and characterization of the EGF-like modules of human Notch-1 implicated in receptor-ligand interactions 10.1002/PRO.5560061002
Molecular Model for the C-type Lectin Domain of Human Thrombomodulin 10.1007/S008940050088
Interaction between C4B-binding protein and protein S is hydrophobic in nature 10.1016/S0161-5890(98)90568-5
Analysis of solvent-exposed and buried co-crystallized ligands: a case study to support the design of novel protein-protein interaction inhibitors 10.1016/J.DRUDIS.2018.11.013
Rigorous sampling of docking poses unveils binding hypothesis for the halogenated ligands of L-type Amino acid Transporter 1 (LAT1) 10.1038/s41598-019-51455-8
Analysis of protein missense alterations by combining sequence‐ and structure‐based methods 10.1002/mgg3.1166
Virtual screening web servers: designing chemical probes and drug candidates in the cyberspace 10.1093/bib/bbaa034
Gly197Arg mutation in protein C causes recurrent thrombosis in a heterozygous carrier 10.1111/jth.14777
Anti-Factor B Antibodies and Acute Postinfectious GN in Children. 10.1681/asn.2019080851
Prevention of COVID-19 by drug repurposing: rationale from drugs prescribed for mental disorders 10.1016/j.drudis.2020.06.022
FastTargetPred: a program enabling the fast prediction of putative protein targets for input chemical databases 10.1093/bioinformatics/btaa494
Structure-based drug repositioning over the human TMPRSS2 protease domain: search for chemical probes able to repress SARS-CoV-2 Spike protein cleavages 10.1016/j.ejps.2020.105495
Fast Rescoring Protocols to Improve the Performance of Structure-Based Virtual Screening Performed on Protein–Protein Interfaces 10.1021/acs.jcim.0c00545
Strategies in the Search for New Lead Compounds or Original Working Hypotheses 10.1016/B978-0-12-417205-0.00004-3
Application Strategies for the Primary Structure-Activity Relationship Exploration 10.1016/B978-0-12-417205-0.00012-2
Structure-based virtual screening 10.2174/978160805142711101010020
In Silico ADME/Tox Predictions 10.1002/9780470915110.ch2
Fr-PPIChem: An Academic Compound Library Dedicated to Protein-Protein Interactions 10.1021/acschembio.0c00179
Demystifying the Molecular Basis of Pyrazoloquinolinones Recognition at the Extracellular α1+/β3- Interface of the GABAA Receptor by Molecular Modeling 10.3389/fphar.2020.561834
A leap into the chemical space of protein-protein interaction inhibitors 10.2174/138161212802651571
Online structure-based screening of purchasable approved drugs and natural compounds: Retrospective examples of drug repositioning on cancer targets 10.18632/oncotarget.25966
Efficiency of a hierarchical docking protocol for computational ligand screening against homology models 10.4015/S1016237214500240
Thr90Ser Mutation in Antithrombin is Associated with Recurrent Thrombosis in a Heterozygous Carrier 10.1055/s-0040-1710590
Mutations in a potential phospholipid binding loop in the C2 domain of factor V affecting the assembly of the prothrombinase complex 10.1097/00001721-200001000-00010
Lattice protein folding with two and four-body statistical potentials 10.1002/1097-0134(20010501)43:2<161::AID-PROT1028>3.0.CO;2-F
Chemical libraries dedicated to protein-protein interactions,Les chimiothèques ciblant les interactions protéine-protéine 10.1051/medsci/20153103017
Protein C deficiency caused by homozygosity for a novel PROC D180G mutation - In vitro expression and structural analysis of the mutation 10.1055/s-0037-1613267
Involvement of Lys 62(217) and lys 63(218) of human anticoagulant protein C in heparin stimulation of inhibition by the protein C inhibitor 10.1055/s-0037-1614632
DG-AMMOS: A New tool to generate 3D conformation of small molecules using Distance Geometry and Automated Molecular Mechanics Optimization for in silico Screening 10.1186/1472-6769-9-6
Ile73Asn mutation in protein C introduces a new N-linked glycosylation site on the first EGF-domain of protein C and causes thrombosis 10.3324/haematol.2019.227033
Combining bioinformatics, chemoinformatics and experimental approaches to design chemical probes: Applications in the field of blood coagulation 10.1016/j.pharma.2016.03.006
A free web-based protocol to assist structure-based virtual screening experiments 10.3390/ijms20184648
ELA/APELA precursor cleaved by furin displays tumor suppressor function in renal cell carcinoma through mTORC1 activation 10.1172/JCI.INSIGHT.129070
Editorial: Virtual screening 10.2174/157340908785747429
Antihistamine and cationic amphiphilic drugs, old molecules as new tools against the COVID-19? 10.1016/j.mehy.2021.110508
In Silico Investigation of the New UK (B.1.1.7) and South African (501Y.V2) SARS-CoV-2 Variants with a Focus at the ACE2-Spike RBD Interface. 10.3390/ijms22041695
Chemoinformatic Analysis of Psychotropic and Antihistaminic Drugs in the Light of Experimental Anti-SARS-CoV-2 Activities 10.26434/chemrxiv.13643690.v4
Chemoinformatic Analysis of Psychotropic and Antihistaminic Drugs in the Light of Experimental Anti-SARS-CoV-2 Activities 10.2147/AABC.S304649
PAK1-Dependent Antitumor Effect of AAC-11‒Derived Peptides on Sézary Syndrome Malignant CD4+ T Lymphocytes 10.1016/j.jid.2021.01.033
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
Céline Crauste
Crauste Céline
ORCID: 0000-0002-5714-8749
Extra Virgin Olive Oil Reduced Polyunsaturated Fatty Acid and Cholesterol Oxidation in Rodent Liver: Is This Accounted for Hydroxytyrosol-Fatty Acid Conjugation? 10.1021/acs.chemrestox.6b00214
Phloroglucinol protects retinal pigment epithelium and photoreceptor against all-trans-retinal-induced toxicity and inhibits A2E formation. 10.1111/jcmm.12857
Omega-3 polyunsaturated lipophenols, how and why? 10.1016/j.biochi.2015.07.018
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
Tuberculosis: the drug development pipeline at a glance. 10.1016/j.ejmech.2012.02.033
Synthesis of 2',3'-dideoxynucleoside phosphoesters using H-phosphonate chemistry on soluble polymer support. 10.1021/jo1022958
Insights into the soluble PEG-supported synthesis of cytosine-containing nucleoside 5'-mono-, di-, and triphosphates. 10.1021/jo901931z
Development of a sensitive and selective LC/MS/MS method for the simultaneous determination of intracellular 1-beta-D-arabinofuranosylcytosine triphosphate (araCTP), cytidine triphosphate (CTP) and deoxycytidine triphosphate (dCTP) in a human follicular lymphoma cell line. 10.1016/j.jchromb.2009.02.071
Magnesium(II)-coordinated Claisen rearrangement: a direct approach towards ulosonic acid derivatives 10.1016/j.tetlet.2006.07.022
Asymmetric Synthesis of New β-Lactam Lipopeptides as Bacterial Signal Peptidase I Inhibitors 10.1002/ejoc.201100148
Total Syntheses of Two bis-Allylic-Deuterated DHA Analogues 10.1002/ajoc.201600565
Synthesis and Evaluation of Polyunsaturated Fatty Acid-Phenol Conjugates as Anti-Carbonyl-Stress Lipophenols 10.1002/ejoc.201402282
Resveratrol formulated with a natural deep eutectic solvent inhibits active matrix metalloprotease-9 in hormetic conditions 10.1002/ejlt.201700171
Oxadiazolone derivatives, new promising multi-target inhibitors against M. tuberculosis 10.1016/j.bioorg.2018.08.025
LipG a bifunctional phospholipase/thioesterase involved in mycobacterial envelope remodeling 10.1042/bsr20181953
New Lipophenol Antioxidants Reduce Oxidative Damage in Retina Pigment Epithelial Cells 10.3390/antiox7120197
Resveratrol-Linoleate protects from exacerbated endothelial permeability via a drastic inhibition of the MMP-9 activity 10.1042/bsr20171712
Bis-allylic Deuterated DHA Alleviates Oxidative Stress in Retinal Epithelial Cells 10.3390/antiox8100447
Isopropyl-phloroglucinol-DHA protects outer retinal cells against lethal dose of all-trans-retinal. 10.1111/jcmm.15135
Combination of Lutein and Zeaxanthin, and DHA Regulated Polyunsaturated Fatty Acid Oxidation in H2O2-Stressed Retinal Cells. 10.1007/s11064-020-02994-4
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
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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
Summary of the Sussex-Huawei locomotion-transportation recognition challenge
Observation of a manifold in the chaotic phase space of an asymmetric optical microcavity
Localized temporal variation of Earth's inner-core boundary from high-quality waveform doublets
Off-axis multi-wavelength dispersion controlling metalens for multi-color imaging
Impact of United States political sanctions on international collaborations and research in Iran