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Discovery of NovelN-Phenylphenoxyacetamide Derivatives as EthR Inhibitors and Ethionamide Boosters by Combining High-Throughput Screening and Synthesis

Marion Flipo Nicolas Willand Nathalie Lecat-Guillet Candide Hounsou Matthieu Desroses Florence Leroux Zoé Lens Vincent Villeret Alexandre Wohlkönig René Wintjens Thierry Christophe Hee Kyoung Jeon Camille Locht Priscille Brodin Alain R Baulard Benoit Déprez

Journal of medicinal chemistry, 2012-7

https://doi.org/10.1021/jm300377g

Alexandre Wohlkonig

Wohlkonig Alexandre / Wohlkonig

ORCID: 0000-0003-3103-5022

The Mycobacterium tuberculosis transcriptional repressor EthR is negatively regulated by Serine/Threonine phosphorylation 10.1016/j.bbrc.2014.03.074

Crystallization and initial crystallographic analysis of covalent DNA-cleavage complexes of Staphyloccocus aureus DNA gyrase with QPT-1, moxifloxacin and etoposide. 10.1107/S2053230X15015290

Production, crystallization and preliminary X-ray diffraction of the Gαs α-helical domain in complex with a nanobody. 10.1107/S2053230X14020962

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

Probing the N-terminal β-sheet conversion in the crystal structure of the human prion protein bound to a nanobody. 10.1021/ja407527p

Recombinant human prion protein inhibits prion propagation in vitro. 10.1038/srep02911

High-resolution structure of a papaya plant-defense barwin-like protein solved by in-house sulfur-SAD phasing. 10.1107/S0907444913018015

Characterization of the PAS domain in the sensor-kinase BvgS: mechanical role in signal transmission. 10.1186/1471-2180-13-172

The mannose-specific lectin domains of Flo1p from Saccharomyces cerevisiae and Lg-Flo1p from S. pastorianus: crystallization and preliminary X-ray diffraction analysis of the adhesin-carbohydrate complexes. 10.1107/S1744309113015030

Expression, purification, characterization, and solution nuclear magnetic resonance study of highly deuterated yeast cytochrome C peroxidase with enhanced solubility. 10.1021/bi400220w

Discovery of novel N-phenylphenoxyacetamide derivatives as EthR inhibitors and ethionamide boosters by combining high-throughput screening and synthesis. 10.1021/jm300377g

A novel expression system for production of soluble prion proteins in E. coli. 10.1186/1475-2859-11-6

Structural analysis of the interaction between spiroisoxazoline SMARt-420 and the Mycobacterium tuberculosis repressor EthR2 10.1016/j.bbrc.2017.04.074

Correction to Discovery, Structure-Activity Relationship, and Binding Mode of an Imidazo[1,2- a]pyridine Series of Autotaxin Inhibitors. 10.1021/acs.jmedchem.8b00579

Soluble polymorphic bank vole prion proteins induced by co-expression of quiescin sulfhydryl oxidase in E. coli and their aggregation behaviors. 10.1186/s12934-017-0782-x

Discovery, Structure-Activity Relationship, and Binding Mode of an Imidazo[1,2-a]pyridine Series of Autotaxin Inhibitors. 10.1021/acs.jmedchem.7b00647

Quiescin-sulfhydryl oxidase inhibits prion formation in vitro. 10.18632/aging.101132

Reversion of antibiotic resistance in Mycobacterium tuberculosis by spiroisoxazoline SMARt-420. 10.1126/science.aag1006

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

Structural relationships in the lysozyme superfamily: significant evidence for glycoside hydrolase signature motifs. 10.1371/journal.pone.0015388

Structural basis of quinolone inhibition of type IIA topoisomerases and target-mediated resistance. 10.1038/nsmb.1892

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

Type IIA topoisomerase inhibition by a new class of antibacterial agents. 10.1038/nature09197

Crystallization and preliminary X-ray diffraction analysis of the peptidylprolyl isomerase Par27 of Bordetella pertussis. 10.1107/S1744309108024731

The peptidyl-prolyl isomerase and chaperone Par27 of Bordetella pertussis as the prototype for a new group of parvulins. 10.1016/j.jmb.2007.10.088

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

Biphenyl 2,3',4,5',6-pentakisphosphate, a novel inositol polyphosphate surrogate, modulates Ca2+ responses in rat hepatocytes. 10.1096/fj.06-7691com

Purification of ArcR, an oxidation-sensitive regulatory protein from Bacillus licheniformis. 10.1016/j.pep.2004.05.006

An improved yeast surface display platform for the screening of nanobody immune libraries 10.1038/s41598-018-37212-3

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

Megabodies expand the nanobody toolkit for protein structure determination by single-particle cryo-EM 10.1101/812230

Constructing and purifying megabodies starting from individual nanobody sequences 10.21203/rs.3.pex-1033/v1

Camille Locht

Locht Camille

ORCID: 0000-0001-7295-7336

HBHA-Induced Polycytotoxic CD4+ T Lymphocytes Are Associated with the Control of Mycobacterium tuberculosis Infection in Humans 10.4049/jimmunol.1800840

Distinct virulence ranges for infection of mice by Bordetella pertussis revealed by engineering of the sensor-kinase BvgS 10.1371/journal.pone.0204861

Non-specific Effects of Live Attenuated Pertussis Vaccine Against Heterologous Infectious and Inflammatory Diseases 10.3389/fimmu.2018.02872

IL-17-dependent SIgA-mediated protection against nasal Bordetella pertussis infection by live attenuated BPZE1 vaccine 10.1038/s41385-018-0073-9

Rv0613c/MSMEG_1285 Interacts with HBHA and Mediates Its Proper Cell-Surface Exposure in Mycobacteria 10.3390/ijms19061673

Tuberculin skin test reaction is related to memory, but not naive CD4+ T cell responses to mycobacterial stimuli in BCG-vaccinated young adults 10.1016/j.vaccine.2018.05.068

Diversion of complement-mediated killing by Bordetella 10.1016/j.micinf.2018.02.002

TBVAC2020: Advancing Tuberculosis Vaccines from Discovery to Clinical Development 10.3389/fimmu.2017.01203

Characterization of a Bvg-regulated fatty acid methyl-transferase in Bordetella pertussis 10.1371/journal.pone.0176396

Heparin-Binding Hemagglutinin Adhesin (HBHA) Is Involved in Intracytosolic Lipid Inclusions Formation in Mycobacteria 10.3389/fmicb.2018.02258

In vivo imaging of bacterial colonization of the lower respiratory tract in a baboon model of Bordetella pertussis infection and transmission 10.1038/s41598-018-30896-7

Primary transcriptome analysis reveals importance of IS elements for the shaping of the transcriptional landscape of Bordetella pertussis 10.1080/15476286.2018.1462655

Bordetella pertussis pertactin knock-out strains reveal immunomodulatory properties of this virulence factor 10.1038/s41426-018-0039-8

Construction and evaluation of Bordetella pertussis live attenuated vaccine strain BPZE1 producing Fim3 10.1016/j.vaccine.2018.02.017

Will we have new pertussis vaccines? 10.1016/j.vaccine.2017.11.055

Assessing the reactogenicity of Tdap vaccine administered during pregnancy and antibodies to Bordetella pertussis antigens in maternal and cord sera of Thai women 10.1016/j.vaccine.2018.01.059

Conformational Changes of an Interdomain Linker Mediate Mechanical Signal Transmission in Sensor Kinase BvgS 10.1128/JB.00114-17

Coiled-Coil Antagonism Regulates Activity of Venus Flytrap-Domain-Containing Sensor Kinases of the BvgS Family 10.1128/mBio.02052-17

The Role of Mucosal Immunity in Pertussis 10.3389/fimmu.2018.03068

Live Attenuated Pertussis Vaccine BPZE1 Protects Baboons Against Bordetella pertussis Disease and Infection 10.1093/infdis/jix254

BCG and protection against inflammatory and auto-immune diseases 10.1080/14760584.2017.1333906

Age-Stratified T Cell Responses in Children Infected with Mycobacterium tuberculosis 10.3389/fimmu.2017.01059

Reversion of antibiotic resistance in Mycobacterium tuberculosis by spiroisoxazoline SMARt-420 10.1126/science.aag1006

Highlights of the 11th International Bordetella Symposium: from Basic Biology to Vaccine Development 10.1128/CVI.00388-16

Erratum for Carbonetti et al., "Highlights of the 11th International Bordetella Symposium: from Basic Biology to Vaccine Development" 10.1128/CVI.00071-17

Human isotype-dependent inhibitory antibody responses against Mycobacterium tuberculosis 10.15252/emmm.201606330

Live pertussis vaccines: will they protect against carriage and spread of pertussis? 10.1016/j.cmi.2016.05.029

The multifaceted RisA regulon of Bordetella pertussis 10.1038/srep32774

LppM impact on the colonization of macrophages by Mycobacterium tuberculosis 10.1111/cmi.12619

Added Value of Long-Term Cytokine Release Assays to Detect Mycobacterium tuberculosis Infection in HIV-Infected Subjects in Uganda 10.1097/QAI.0000000000000980

[Tuberculosis, a story still relevant] 10.1051/medsci/20163206001

STAT3 Represses Nitric Oxide Synthesis in Human Macrophages upon Mycobacterium tuberculosis Infection 10.1038/srep29297

Pertussis: Where did we go wrong and what can we do about it? 10.1016/j.jinf.2016.04.020

Pertussis: acellular, whole-cell, new vaccines, what to choose? 10.1586/14760584.2016.1161511

Balance between Coiled-Coil Stability and Dynamics Regulates Activity of BvgS Sensor Kinase in Bordetella 10.1128/mBio.02089-15

Reciprocal interference of maternal and infant immunization in protection against pertussis 10.1016/j.vaccine.2016.01.011

Signal transduction by BvgS sensor kinase. Binding of modulator nicotinate affects the conformation and dynamics of the entire periplasmic moiety 10.1074/jbc.A115.655720

Integrating knowledge of Mycobacterium tuberculosis pathogenesis for the design of better vaccines 10.1586/14760584.2015.1102638

Dendritic Cell Activity Driven by Recombinant Mycobacterium bovis BCG Producing Human IL-18, in Healthy BCG Vaccinated Adults 10.1155/2015/359153

Lower Pre-Treatment T Cell Activation in Early- and Late-Onset Tuberculosis-Associated Immune Reconstitution Inflammatory Syndrome 10.1371/journal.pone.0133924

Dynamic interplay of membrane-proximal POTRA domain and conserved loop L6 in Omp85 transporter FhaC 10.1111/mmi.13137

Signal Transduction by BvgS Sensor Kinase: BINDING OF MODULATOR NICOTINATE AFFECTS THE CONFORMATION AND DYNAMICS OF THE ENTIRE PERIPLASMIC MOIETY 10.1074/jbc.M115.655720

Virulence regulation with Venus flytrap domains: structure and function of the periplasmic moiety of the sensor-kinase BvgS 10.1371/journal.ppat.1004700

Investigating pertussis toxin and its impact on vaccination 10.2217/fmb.14.123

Contribution of a heparin-binding haemagglutinin interferon-gamma release assay to the detection of Mycobacterium tuberculosis infection in HIV-infected patients: comparison with the tuberculin skin test and the QuantiFERON-TB Gold In-tube 10.1186/s12879-015-0796-0

Early cellular immune response to a new candidate mycobacterial vaccine antigen in childhood tuberculosis 10.1016/j.vaccine.2014.12.011

Unconventional, adenosine-producing suppressor T cells induced by dendritic cells exposed to BPZE1 pertussis vaccine 10.1189/jlb.3a0315-101r

Translocation path of a substrate protein through its Omp85 transporter 10.1038/ncomms6271

Antigen-specific interferon-gamma responses and innate cytokine balance in TB-IRIS 10.1371/journal.pone.0113101

HBHA vaccination may require both Th1 and Th17 immune responses to protect mice against tuberculosis 10.1016/j.vaccine.2014.09.024

Toward Understanding the Essence of Post-Translational Modifications for the Mycobacterium tuberculosis Immunoproteome 10.3389/fimmu.2014.00361

Live attenuated B. pertussis BPZE1 rescues the immune functions of Respiratory Syncytial virus infected human dendritic cells by promoting Th1/Th17 responses 10.1371/journal.pone.0100166

Live attenuated vaccines against pertussis 10.1586/14760584.2014.942222

Human dendritic cell maturation and cytokine secretion upon stimulation with Bordetella pertussis filamentous haemagglutinin 10.1016/j.micinf.2014.04.003

Conformational dynamics of protein transporter FhaC: large-scale motions of plug helix 10.1111/mmi.12585

B-cell responses after intranasal vaccination with the novel attenuated Bordetella pertussis vaccine strain BPZE1 in a randomized phase I clinical trial 10.1016/j.vaccine.2014.04.048

Possible options for new pertussis vaccines 10.1093/infdis/jit531

A phase I clinical study of a live attenuated Bordetella pertussis vaccine--BPZE1; a single centre, double-blind, placebo-controlled, dose-escalating study of BPZE1 given intranasally to healthy adult male volunteers 10.1371/journal.pone.0083449

Mucosal delivery of antigen-coated nanoparticles to lungs confers protective immunity against tuberculosis infection in mice 10.1002/eji.201343887

Pertussis toxin improves immune responses to a combined pneumococcal antigen and leads to enhanced protection against Streptococcus pneumoniae 10.1128/CVI.00134-14

Heterologous prime-boost immunization with live attenuated B. pertussis BPZE1 followed by acellular pertussis vaccine in mice 10.1016/j.vaccine.2014.06.019

Key role of effector memory CD4+ T lymphocytes in a short-incubation heparin-binding hemagglutinin gamma interferon release assay for the detection of latent tuberculosis 10.1128/CVI.00651-13

LPS-binding protein and IL-6 mark paradoxical tuberculosis immune reconstitution inflammatory syndrome in HIV patients 10.1371/journal.pone.0081856

Attenuated Bordetella pertussis vaccine protects against respiratory syncytial virus disease via an IL-17-dependent mechanism 10.1164/rccm.201307-1227OC

Protective role of adenylate cyclase in the context of a live pertussis vaccine candidate 10.1016/j.micinf.2013.10.002

Different T cell memory in preadolescents after whole-cell or acellular pertussis vaccination 10.1016/j.vaccine.2013.10.056

Heparin-binding haemagglutinin, a new tool for the detection of latent Mycobacterium tuberculosis infection in hemodialysis patients 10.1371/journal.pone.0071088

Novel feature of Mycobacterium avium subsp. paratuberculosis, highlighted by characterization of the heparin-binding hemagglutinin adhesin 10.1128/JB.00671-13

Characterization of the PAS domain in the sensor-kinase BvgS: mechanical role in signal transmission 10.1186/1471-2180-13-172

Modulation of the complement system in monocytes contributes to tuberculosis-associated immune reconstitution inflammatory syndrome 10.1097/qad.0b013e328361648b

The role of monocytes in the development of Tuberculosis-associated Immune Reconstitution Inflammatory Syndrome 10.1016/j.imbio.2013.07.004

Immunogenicity of live attenuated B. pertussis BPZE1 producing the universal influenza vaccine candidate M2e 10.1371/journal.pone.0059198

Purification of native HBHA from Mycobacterium avium subsp. paratuberculosis 10.1186/1756-0500-6-55

Genomic analysis of smooth tubercle bacilli provides insights into ancestry and pathoadaptation of Mycobacterium tuberculosis 10.1038/ng.2517

Persistence at one year of age of antigen-induced cellular immune responses in preterm infants vaccinated against whooping cough: comparison of three different vaccines and effect of a booster dose 10.1016/j.vaccine.2013.02.004

Low prevalence of vitamin D deficiency in Ugandan HIV-infected patients with and without tuberculosis 10.5588/ijtld.11.0146

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Attenuated Bordetella pertussis BPZE1 protects against allergic airway inflammation and contact dermatitis in mouse models 10.1111/j.1398-9995.2012.02884.x

Dual mechanism of protection by live attenuated Bordetella pertussis BPZE1 against Bordetella bronchiseptica in mice 10.1016/j.vaccine.2012.07.005

New pertussis vaccination approaches: en route to protect newborns? 10.1111/j.1574-695x.2012.00988.x

Discovery of novel N-phenylphenoxyacetamide derivatives as EthR inhibitors and ethionamide boosters by combining high-throughput screening and synthesis 10.1021/jm300377g

Differential contribution of the repeats to heparin binding of HBHA, a major adhesin of Mycobacterium tuberculosis 10.1371/journal.pone.0032421

Clinical spectrum, risk factors and outcome of immune reconstitution inflammatory syndrome in patients with tuberculosis-HIV coinfection 10.3851/imp2108

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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

The ins and outs of pertussis toxin 10.1111/j.1742-4658.2011.08237.x

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[New antituberculosis vaccines] 10.1016/j.arcped.2011.05.003

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Substrate recognition by the POTRA domains of TpsB transporter FhaC 10.1111/j.1365-2958.2011.07680.x

Membrane-associated DegP in Bordetella chaperones a repeat-rich secretory protein 10.1111/j.1365-2958.2011.07672.x

Detection of small RNAs in Bordetella pertussis and identification of a novel repeated genetic element 10.1186/1471-2164-12-207

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Attenuated Bordetella pertussis vaccine candidate BPZE1 promotes human dendritic cell CCL21-induced migration and drives a Th1/Th17 response 10.4049/jimmunol.1003765

Ethionamide boosters: synthesis, biological activity, and structure-activity relationships of a series of 1,2,4-oxadiazole EthR inhibitors 10.1021/jm200076a

Characterization of the Mycobacterium avium subsp. paratuberculosis laminin-binding/histone-like protein (Lbp/Hlp) which reacts with sera from patients with Crohn's disease 10.1016/j.micinf.2011.02.002

Chips from chips: application to the study of antibody responses to methylated proteins 10.1021/pr100707t

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

Long-term immunity against pertussis induced by a single nasal administration of live attenuated B. pertussis BPZE1 10.1016/j.vaccine.2010.08.017

Report of the 2nd "French Clinical Vaccinology Meeting Jean-Gerard Guillet": immunization and respiratory diseases 10.1016/j.vaccine.2010.07.038

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Boosting BCG to protect against TB 10.1586/ers.10.25

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Boosting with mycobacterial heparin-binding haemagglutinin enhances protection of Mycobacterium bovis BCG-vaccinated newborn mice against M. tuberculosis 10.1016/j.vaccine.2010.04.062

T- and B-cell-mediated protection induced by novel, live attenuated pertussis vaccine in mice. Cross protection against parapertussis 10.1371/journal.pone.0010178

Attenuated Bordetella pertussis vaccine strain BPZE1 modulates allergen-induced immunity and prevents allergic pulmonary pathology in a murine model 10.1111/j.1365-2222.2010.03459.x

Heparin-binding, hemagglutinin-specific IFN-gamma synthesis at the site of infection during active tuberculosis in humans 10.1164/rccm.201001-0083oc

Impact of HIV infection on the recurrence of tuberculosis in South India 10.1086/650528

Dose response of attenuated Bordetella pertussis BPZE1-induced protection in mice 10.1128/CVI.00322-09

Cellular immune responses of preterm infants after vaccination with whole-cell or acellular pertussis vaccines 10.1128/CVI.00328-09

Correction: Molecular Evolution of the Two-Component System BvgAS Involved in Virulence Regulation in Bordetella 10.1371/annotation/ae7f86ff-0aca-4411-aed3-3eeea9303abb

Monocyte-derived interleukin-10 depresses the Bordetella pertussis- specific gamma interferon response in vaccinated infants 10.1128/CVI.00314-09

In situ chemical modification of peptide microarrays: application to the study of the antibody responses to methylated antigens 10.1007/978-1-60761-845-4_11

Molecular evolution of the two-component system BvgAS involved in virulence regulation in Bordetella 10.1371/journal.pone.0006996

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Cytokine and antibody profiles in 1-year-old children vaccinated with either acellular or whole-cell pertussis vaccine during infancy 10.1016/j.vaccine.2009.07.075

Genomic island excisions in Bordetella petrii 10.1186/1471-2180-9-141

Subcutaneous boosting with heparin binding haemagglutinin increases BCG-induced protection against tuberculosis 10.1016/j.micinf.2009.07.005

Synthetic EthR inhibitors boost antituberculous activity of ethionamide 10.1038/nm.1950

A live attenuated Bordetella pertussis candidate vaccine does not cause disseminating infection in gamma interferon receptor knockout mice 10.1128/CVI.00082-09

Biomarkers for tuberculosis disease status and diagnosis 10.1097/mcp.0b013e328326f42c

Interaction of the mycobacterial heparin-binding hemagglutinin with actin, as evidenced by single-molecule force spectroscopy 10.1128/JB.00974-08

Origin, spread and demography of the Mycobacterium tuberculosis complex 10.1371/journal.ppat.1000160

Genetic stability of the live attenuated Bordetella pertussis vaccine candidate BPZE1 10.1016/j.vaccine.2008.08.018

The coiled-coil N-terminal domain of the heparin-binding haemagglutinin is required for the humoral and cellular immune responses in mice 10.1016/j.molimm.2008.07.009

Bordetella pertussis filamentous hemagglutinin delivered by mucosal routes enhances immunoglobulin levels in serum and mucosal fluids 10.1111/j.1574-695x.2008.00460.x

A common vaccination strategy to solve unsolved problems of tuberculosis and pertussis? 10.1016/j.micinf.2008.07.008

How a different look at latency can help to develop novel diagnostics and vaccines against tuberculosis 10.1517/14712598.7.11.1665

The peptidyl-prolyl isomerase and chaperone Par27 of Bordetella pertussis as the prototype for a new group of parvulins 10.1016/j.jmb.2007.10.088

Highly attenuated Bordetella pertussis strain BPZE1 as a potential live vehicle for delivery of heterologous vaccine candidates 10.1128/IAI.00795-07

Structure-based mechanism of ligand binding for periplasmic solute-binding protein of the Bug family 10.1016/j.jmb.2007.08.006

Heparin-binding-hemagglutinin-induced IFN-gamma release as a diagnostic tool for latent tuberculosis 10.1371/journal.pone.0000926

Single-molecule force spectroscopy of mycobacterial adhesin-adhesin interactions 10.1128/JB.01299-07

Structure of the membrane protein FhaC: a member of the Omp85-TpsB transporter superfamily 10.1126/science.1143860

In vitro expansion of CD4+CD25highFOXP3+CD127low/- regulatory T cells from peripheral blood lymphocytes of healthy Mycobacterium tuberculosis-infected humans 10.1016/j.micinf.2007.06.004

Regulatory T cells depress immune responses to protective antigens in active tuberculosis 10.1164/rccm.200701-084oc

Macrophage-specific Mycobacterium tuberculosis genes: identification by green fluorescent protein and kanamycin resistance selection 10.1099/mic.0.2006/000547-0

Enzymatic methylation of the Mycobacterium tuberculosis heparin-binding haemagglutinin 10.1111/j.1574-6968.2007.00636.x

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

IL-18 does not increase allergic airway disease in mice when produced by BCG 10.1155/2007/67276

Antibody response in pulmonary tuberculosis against recombinant 27kDa (MPT51, Rv3803c) protein of Mycobacterium tuberculosis 10.1080/00365540701402954

Mycobacterium smegmatis produces an HBHA homologue which is not involved in epithelial adherence 10.1016/j.micinf.2006.11.007

Combined RNAseq and ChIPseq Analyses of the BvgA Virulence Regulator of Bordetella pertussis 10.1128/mSystems.00208-20

Good old BCG – what a century‐old vaccine can contribute to modern medicine 10.1111/joim.13195

The History of Pertussis Toxin 10.3390/toxins13090623

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

Host-directed therapies offer novel opportunities for the fight against tuberculosis 10.1016/j.drudis.2017.05.005

A Bacterial Toxin with Analgesic Properties: Hyperpolarization of DRG Neurons by Mycolactone 10.3390/toxins9070227

A Bacterial Toxin with Analgesic Properties: Hyperpolarization of DRG Neurons by Mycolactone 10.3390/toxins9070227 10.3390/toxins9070227.

Clofazimine encapsulation in nanoporous silica particles for the oral treatment of antibiotic-resistant Mycobacterium tuberculosis infections 10.2217/nnm-2016-0364

Cyclodextrin-based nanocarriers containing a synergic drug combination: a potential formulation for pulmonary administration of antitubercular drugs 10.1016/j.ijpharm.2017.05.030 10.1016/j.ijpharm.2017.05.030.

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

Host-directed therapies offer novel opportunities for the fight against tuberculosis 10.1016/j.drudis.2017.05.005 10.1016/j.drudis.2017.05.005.

Identification of aminopyrimidine-sulfonamides as potent modulators of Wag31-mediated cell elongation in mycobacteria 10.1111/mmi.13535

Impact of pe_ pgrs33 Gene Polymorphisms on Mycobacterium tuberculosis Infection and Pathogenesis 10.3389/fcimb.2017.00137

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

High content screening in chemical biology: overview and main challenges 10.1051/medsci/20153102016

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

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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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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

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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

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A novel codrug made of the combination of ethionamide and its potentiating booster: synthesis, self-assembly into nanoparticles and antimycobacterial evaluation 10.1039/C9OB00680J

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Fragment-Based Optimized EthR Inhibitors with in Vivo Ethionamide Boosting Activity. 10.1021/acsinfecdis.9b00277

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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

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Automated HTS/HCS for antivirals using visual HIV full replication assays. 10.1186/1742-4690-6-s2-p82

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willand nicolas

nicolas willand

ORCID: 0000-0002-0784-0462

http://www.deprezlab.fr

http://www.sct-asso.fr

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Synthesis of functionalized 2-isoxazolines as three-dimensional fragments for fragment-based drug discovery 10.1016/j.tetlet.2015.05.035

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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

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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

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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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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

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

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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

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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

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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

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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

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

High content screening identifies decaprenyl-phosphoribose 2' epimerase as a target for intracellular antimycobacterial inhibitors. 10.1371/journal.ppat.1000645

Systematic genetic nomenclature for type VII secretion systems. 10.1371/journal.ppat.1000507

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

[Aquatic insects and transmission of Mycobacterium ulcerans]. 10.1051/medsci/20072367572

Impact of Mycobacterium ulcerans biofilm on transmissibility to ecological niches and Buruli ulcer pathogenesis. 10.1371/journal.ppat.0030062

Protection against Mycobacterium ulcerans lesion development by exposure to aquatic insect saliva. 10.1371/journal.pmed.0040064

Synthesis and antimycobacterial evaluation of benzofurobenzopyran analogues. 10.1016/j.bmc.2006.12.009

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

High frequency of CD4+ T cells specific for the TB10.4 protein correlates with protection against Mycobacterium tuberculosis infection. 10.1128/iai.02086-05

Benzofuro[3,2-f][1]benzopyrans: a new class of antitubercular agents. 10.1016/j.bmc.2006.03.033

An increase in antimycobacterial Th1-cell responses by prime-boost protocols of immunization does not enhance protection against tuberculosis. 10.1128/iai.74.4.2128-2137.2006

Dissection of ESAT-6 system 1 of Mycobacterium tuberculosis and impact on immunogenicity and virulence. 10.1128/iai.74.1.88-98.2006

Tuberculosis: from genome to vaccine. 10.1586/14760584.4.4.541

Immunogenic membrane-associated proteins of Mycobacterium tuberculosis revealed by proteomics. 10.1099/mic.0.27799-0

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

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

ESAT-6 proteins: protective antigens and virulence factors? 10.1016/j.tim.2004.09.007

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

Cell envelope protein PPE68 contributes to Mycobacterium tuberculosis RD1 immunogenicity independently of a 10-kilodalton culture filtrate protein and ESAT-6. 10.1128/iai.72.4.2170-2176.2004

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

http://www.deprezlab.fr

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

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

Corrigendum to "Synthesis of a 200-member library of squaric acid N-hydroxylamide amides" [Bioorg. Med. Chem. Lett. 18 (2008) 4968-4971] (DOI:10.1016/j.bmcl.2008.08.025) 10.1016/j.bmcl.2008.08.116

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

Probing the role of oligomerization in the high thermal stability of Pyrococcus furiosus ornithine carbamoyltransferase by site-specific mutants. 10.1046/j.1432-1327.2001.02302.x

Crystal structure of isopentenyl diphosphate:dimethylallyl diphosphate isomerase. 10.1093/emboj/20.7.1530

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Crystal structure of a D-aminopeptidase from Ochrobactrum anthropi, a new member of the 'penicillin-recognizing enzyme' family. 10.1016/s0969-2126(00)00188-x

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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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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

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Take Your PIC 10.1016/j.tibs.2021.05.008

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

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Synthesis of sugar-based ethenyl ethers through a vinyl bis-sulfone methodology 10.1016/s0040-4020(03)00661-6

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