A fragment merging approach towards the development of small molecule inhibitors of Mycobacterium tuberculosis EthR for use as ethionamide boosters
Nikiforov, Petar O. Surade, Sachin Blaszczyk, Michal Delorme, Vincent Brodin, Priscille Baulard, Alain R. Blundell, Tom L. Abell, Chris
Vincent Delorme
Delorme Vincent
ORCID: 0000-0001-5235-7069
Discovery of thienothiazolocarboxamide analogues as novel anti-tubercular agent. 10.1016/j.bmc.2020.115797
Drug Discovery Platform Targeting M. tuberculosis with Human Embryonic Stem Cell-Derived Macrophages. 10.1016/j.stemcr.2019.10.002
Oxadiazolone derivatives, new promising multi-target inhibitors against M. tuberculosis. 10.1016/j.bioorg.2018.08.025
Molecular Targets Related Drug Resistance Mechanisms in MDR-, XDR-, and TDR-Mycobacterium tuberculosis Strains. 10.3389/fcimb.2018.00114
Publisher Correction: Combination therapy for tuberculosis treatment: pulmonary administration of ethionamide and booster co-loaded nanoparticles. 10.1038/s41598-018-25177-2
Mycobacterium tuberculosis Infection and Innate Responses in a New Model of Lung Alveolar Macrophages. 10.3389/fimmu.2018.00438
ArfGAP1 restricts Mycobacterium tuberculosis entry by controlling the actin cytoskeleton. 10.15252/embr.201744371
Cyclipostins and Cyclophostin analogs as promising compounds in the fight against tuberculosis. 10.1038/s41598-017-11843-4
Mycobacterium tuberculosis Controls Phagosomal Acidification by Targeting CISH-Mediated Signaling. 10.1016/j.celrep.2017.08.101
Combination therapy for tuberculosis treatment: pulmonary administration of ethionamide and booster co-loaded nanoparticles. 10.1038/s41598-017-05453-3
Efflux Attenuates the Antibacterial Activity of Q203 in Mycobacterium tuberculosis. 10.1128/aac.02637-16
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
Reversion of antibiotic resistance in Mycobacterium tuberculosis by spiroisoxazoline SMARt-420. 10.1126/science.aag1006
High-Content Screening of Raw Actinomycete Extracts for the Identification of Antituberculosis Activities. 10.1177/1087057116675887
Identification of aminopyrimidine-sulfonamides as potent modulators of Wag31-mediated cell elongation in mycobacteria. 10.1111/mmi.13535
STAT3 Represses Nitric Oxide Synthesis in Human Macrophages upon Mycobacterium tuberculosis Infection. 10.1038/srep29297
A fragment merging approach towards the development of small molecule inhibitors of Mycobacterium tuberculosis EthR for use as ethionamide boosters. 10.1039/c5ob02630j
Testing chemical and genetic Modulators in Mycobacterium tuberculosis infected cells using phenotypic assays. 10.1007/978-1-4939-2450-9_24
2-Carboxyquinoxalines kill mycobacterium tuberculosis through noncovalent inhibition of DprE1. 10.1021/cb5007163
Supported inhibitor for fishing lipases in complex biological media and mass spectrometry identification. 10.1016/j.biochi.2014.07.015
A microscopic phenotypic assay for the quantification of intracellular mycobacteria adapted for high-throughput/high-content screening. 10.3791/51114
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MmPPOX inhibits Mycobacterium tuberculosis lipolytic enzymes belonging to the hormone-sensitive lipase family and alters mycobacterial growth. 10.1371/journal.pone.0046493
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Two cutinase-like proteins secreted by Mycobacterium tuberculosis show very different lipolytic activities reflecting their physiological function. 10.1096/fj.09-144766
Synthesis and kinetic evaluation of cyclophostin and cyclipostins phosphonate analogs as selective and potent inhibitors of microbial lipases. 10.1021/jm301216x
Phenotypic Screening for Drug Discovery in Tuberculosis https://doi.org/10.1039/9781839160721-00198
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
Plant extracts from Cameroonian medicinal plants strongly inhibit hepatitis C virus infection in vitro 10.3389/fmicb.2015.00438
Polyphenols Inhibit Hepatitis C Virus Entry by a New Mechanism of Action 10.1128/jvi.01473-15
Testing chemical and genetic Modulators in Mycobacterium tuberculosis infected cells using phenotypic assays 10.1007/978-1-4939-2450-9_24
A Microscopic Phenotypic Assay for the Quantification of Intracellular Mycobacteria Adapted for High-throughput/High-content Screening 10.3791/51114
Ligand Efficiency Driven Design of New Inhibitors of Mycobacterium tuberculosis Transcriptional Repressor EthR Using Fragment Growing, Merging, and Linking Approaches 10.1021/jm500422b
Mycobacterial Toxin Induces Analgesia in Buruli Ulcer by Targeting the Angiotensin Pathways 10.1016/j.cell.2014.04.040
Potent antiviral activity of Solanum rantonnetii and the isolated compounds against hepatitis C virus in vitro 10.1016/j.jff.2014.09.022
A novel specific edge effect correction method for RNA interference screenings 10.1093/bioinformatics/btr648
Discovery of Novel N-Phenylphenoxyacetamide Derivatives as EthR Inhibitors and Ethionamide Boosters by Combining High-Throughput Screening and Synthesis 10.1021/jm3003779
Ethionamide Boosters. 2. Combining Bioisosteric Replacement and Structure-Based Drug Design To Solve Pharmacokinetic Issues in a Series of Potent 1,2,4-Oxadiazole EthR Inhibitors 10.1021/jm200825u
The Balance of Apoptotic and Necrotic Cell Death in Mycobacterium tuberculosis Infected Macrophages Is Not Dependent on Bacterial Virulence 10.1371/journal.pone.0047573
Analogous Mechanisms of Resistance to Benzothiazinones and Dinitrobenzamides in Mycobacterium smegmatis 10.1371/journal.pone.0026675
Ethionamide Boosters: Synthesis, Biological Activity, and Structure-Activity Relationships of a Series of 1,2,4-Oxadiazole EthR Inhibitors 10.1021/jm200076a
High-content screening in infectious diseases 10.1016/j.cbpa.2011.05.023
Functional characterization of the Mycobacterium tuberculosis serine/threonine kinase PknJ 10.1099/mic.0.038133-0
High Content Phenotypic Cell-Based Visual Screen Identifies Mycobacterium tuberculosis Acyltrehalose-Containing Glycolipids Involved in Phagosome Remodeling 10.1371/journal.ppat.1001100
High-content imaging of Mycobacterium tuberculosis-infected macrophages: an in vitro model for tuberculosis drug discovery 10.4155/fmc.10.223
Long-circulating DNA lipid nanocapsules as new vector for passive tumor targeting 10.1016/j.biomaterials.2009.09.044
Automated High-Throughput siRNA Transfection in Raw 264.7 Macrophages: A Case Study for Optimization Procedure 10.1177/1087057108328762
Benzothiazinones Kill Mycobacterium tuberculosis by Blocking Arabinan Synthesis 10.1126/science.1171583
High Content Screening Identifies Decaprenyl-Phosphoribose 2 ' Epimerase as a Target for Intracellular Antimycobacterial Inhibitors 10.1371/journal.ppat.1000645
Systematic Genetic Nomenclature for Type VII Secretion Systems 10.1371/journal.ppat.1000507
Control of M-tuberculosis ESAT-6 secretion and specific T cell recognition by PhoP 10.1371/journal.ppat.0040033
Aquatic insects and transmission of Mycobacterium ulcerans 10.1051/medsci/20072367572
ESAT-6 from Mycobacterium tuberculosis dissociates from its putative chaperone CFP-10 under acidic conditions and exhibits membrane-lysing activity 10.1128/jb.00469-07
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Mycobacterium tuberculosis inhibits human innate immune responses via the production of TLR2 antagonist glycolipids 10.1073/pnas.1707840114
ArfGAP1 restricts Mycobacterium tuberculosis entry by controlling the actin cytoskeleton 10.15252/embr.201744371
ArfGAP1 restricts Mycobacterium tuberculosis entry by controlling the actin cytoskeleton 10.15252/embr.201744371 10.15252/embr.201744371.
Combination therapy for tuberculosis treatment: pulmonary administration of ethionamide and booster co-loaded nanoparticles 10.1038/s41598-017-05453-3
Cyclipostins and Cyclophostin analogs as promising compounds in the fight against tuberculosis 10.1038/s41598-017-11843-4 10.1038/s41598-017-11843-4.
Fragment-Sized EthR Inhibitors Exhibit Exceptionally Strong Ethionamide Boosting Effect in Whole-Cell Mycobacterium tuberculosis Assays 10.1021/acschembio.7b00091
Host-pathogen systems for early drug discovery against tuberculosis 10.1016/j.mib.2017.11.017 10.1016/j.mib.2017.11.017.
Legionella pneumophila Modulates Mitochondrial Dynamics to Trigger Metabolic Repurposing of Infected Macrophages 10.1016/j.chom.2017.07.020 10.1016/j.chom.2017.07.020. Epub 2017 Aug 31.
Mycobacterium tuberculosis Controls Phagosomal Acidification by Targeting CISH-Mediated Signaling 10.1016/j.celrep.2017.08.101 10.1016/j.celrep.2017.08.101.
Mycobacterium tuberculosis inhibits human innate immune responses via the production of TLR2 antagonist glycolipids 10.1073/pnas.1707840114 10.1073/pnas.1707840114.
Identification of Piperazinylbenzenesulfonamides as New Inhibitors of Claudin-1 Trafficking and Hepatitis C Virus Entry 10.1128/jvi.01982-17
Multiplexed Quantitation of Intraphagocyte Mycobacterium tuberculosis Secreted Protein Effectors 10.1016/j.celrep.2018.03.125
Oxadiazolone derivatives, new promising multi-target inhibitors against M. tuberculosis 10.1016/j.bioorg.2018.08.025
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Synergy between circular bacteriocin AS-48 and ethambutol against Mycobacterium tuberculosis 10.1128/aac.00359-18
The EU approved antimalarial pyronaridine shows antitubercular activity and synergy with rifampicin, targeting RNA polymerase 10.1016/j.tube.2018.08.004
Cyclipostins and Cyclophostin analogs as promising compounds in the fight against tuberculosis 10.1038/s41598-017-11843-4
Cyclodextrin-based nanocarriers containing a synergic drug combination: A potential formulation for pulmonary administration of antitubercular drugs 10.1016/j.ijpharm.2017.05.030
Host-pathogen systems for early drug discovery against tuberculosis 10.1016/j.mib.2017.11.017
Legionella pneumophila Modulates Mitochondrial Dynamics to Trigger Metabolic Repurposing of Infected Macrophages 10.1016/j.chom.2017.07.020
Mycobacterium tuberculosis Controls Phagosomal Acidification by Targeting CISH-Mediated Signaling 10.1016/j.celrep.2017.08.101
Phenotypic assays for Mycobacterium tuberculosis infection 10.1002/cyto.a.23129
A fast, fully automated cell segmentation algorithm for high-throughput and high-content screening 10.1002/cyto.a.20627
Compartmentalized Encapsulation of Two Antibiotics in Porous Nanoparticles: an Efficient Strategy to Treat Intracellular Infections 10.1002/ppsc.201800360
Spatiotemporal Changes of the Phagosomal Proteome in Dendritic Cells in Response to LPS Stimulation 10.1074/mcp.RA119.001316
Mycolactone as Analgesic: Subcutaneous Bioavailability Parameters 10.3389/fphar.2019.00378
Intrinsic Antibacterial Activity of Nanoparticles Made of β-Cyclodextrins Potentiates Their Effect as Drug Nanocarriers against Tuberculosis 10.1021/acsnano.8b07902
Mitochondrial Dynamics and Activity in Legionella-Infected Cells 10.1007/978-1-4939-9048-1_13
Heparin-Binding Hemagglutinin Adhesin (HBHA) Is Involved in Intracytosolic Lipid Inclusions Formation in Mycobacteria 10.3389/fmicb.2018.02258
Dehydrojuncusol, a Natural Phenanthrene Compound Extracted from Juncus maritimus, Is a New Inhibitor of Hepatitis C Virus RNA Replication 10.1128/jvi.02009-18
A novel codrug made of the combination of ethionamide and its potentiating booster: synthesis, self-assembly into nanoparticles and antimycobacterial evaluation 10.1039/C9OB00680J
Could Mycolactone Inspire New Potent Analgesics? Perspectives and Pitfalls 10.3390/toxins11090516
Paradoxical Roles of the MAL/Tirap Adaptor in Pathologies. 10.3389/fimmu.2020.569127
Fragment-Based Optimized EthR Inhibitors with in Vivo Ethionamide Boosting Activity. 10.1021/acsinfecdis.9b00277
Intracellular and in vivo evaluation of imidazo[2,1-b]thiazole-5-carboxamide anti-tuberculosis compounds. 10.1371/journal.pone.0227224
Preclinical assessment of a new live attenuated Mycobacterium tuberculosis Beijing-based vaccine for tuberculosis. 10.1016/j.vaccine.2019.11.085
IRG1 controls immunometabolic host response and restricts intracellular Mycobacterium tuberculosis infection 10.1101/761551
Worms' Antimicrobial Peptides. 10.3390/md17090512
Theaflavins, polyphenols of black tea, inhibit entry of hepatitis C virus in cell culture. 10.1371/journal.pone.0198226
Plant extracts from Cameroonian medicinal plants strongly inhibit hepatitis C virus infection in vitro. 10.3389/fmicb.2015.00488
Discovery of Q203, a potent clinical candidate for the treatment of tuberculosis. 10.1038/nm.3262
Discovery of novel N-phenylphenoxyacetamide derivatives as EthR inhibitors and ethionamide boosters by combining high-throughput screening and synthesis. 10.1021/jm300377g
Shortening the drug discovery pipeline: small molecule high content screening for lead discovery in neglected disease. 10.1186/1753-6561-5-s1-p38
Automated HTS/HCS for antivirals using visual HIV full replication assays. 10.1186/1742-4690-6-s2-p82
Influence of ESAT-6 secretion system 1 (RD1) of Mycobacterium tuberculosis on the interaction between mycobacteria and the host immune system. 10.4049/jimmunol.174.6.3570
Cell microbiology interview 10.1111/cmi.13288
Pathogenomic analyses of Mycobacterium microti, an ESX-1-deleted member of the Mycobacterium tuberculosis complex causing disease in various hosts 10.1099/mgen.0.000505
Nathalie deboosere
deboosere Nathalie
ORCID: 0000-0002-2873-5485
ArfGAP1 restricts Mycobacterium tuberculosis entry by controlling the actin cytoskeleton. 10.15252/embr.201744371
Mycobacterium tuberculosis Controls Phagosomal Acidification by Targeting CISH-Mediated Signaling. 10.1016/j.celrep.2017.08.101
A Bacterial Toxin with Analgesic Properties: Hyperpolarization of DRG Neurons by Mycolactone. 10.3390/toxins9070227
Phenotypic assays for Mycobacterium tuberculosis infection. 10.1002/cyto.a.23129
Fragment-Sized EthR Inhibitors Exhibit Exceptionally Strong Ethionamide Boosting Effect in Whole-Cell Mycobacterium tuberculosis Assays. 10.1021/acschembio.7b00091
STAT3 Represses Nitric Oxide Synthesis in Human Macrophages upon Mycobacterium tuberculosis Infection. 10.1038/srep29297
LppM impact on the colonization of macrophages by Mycobacterium tuberculosis. 10.1111/cmi.12619
A microscopic phenotypic assay for the quantification of intracellular mycobacteria adapted for high-throughput/high-content screening. 10.3791/51114
Adhesion of human pathogenic enteric viruses and surrogate viruses to inert and vegetal food surfaces. 10.1016/j.fm.2012.04.007
Viral elution and concentration method for detection of influenza A viruses in mud by real-time RT-PCR. 10.1016/j.jviromet.2011.10.013
Comparison of chlorine and peroxyacetic-based disinfectant to inactivate Feline calicivirus, Murine norovirus and Hepatitis A virus on lettuce. 10.1016/j.ijfoodmicro.2011.08.011
Direct detection of highly pathogenic avian influenza A/H5N1 virus from mud specimens. 10.1016/j.jviromet.2011.06.002
Development and validation of a concentration method for the detection of influenza a viruses from large volumes of surface water. 10.1128/aem.02484-10
A predictive microbiology approach for thermal inactivation of Hepatitis A virus in acidified berries. 10.1016/j.fm.2010.05.018
Assessment of the removal and inactivation of influenza viruses H5N1 and H1N1 by drinking water treatment. 10.1016/j.watres.2010.01.013
Intra-laboratory validation of a concentration method adapted for the enumeration of infectious F-specific RNA coliphage, enterovirus, and hepatitis A virus from inoculated leaves of salad vegetables. 10.1016/j.ijfoodmicro.2005.11.007
Modelling effect of physical and chemical parameters on heat inactivation kinetics of hepatitis A virus in a fruit model system. 10.1016/j.ijfoodmicro.2003.10.015
Host-pathogen systems for early drug discovery against tuberculosis. 10.1016/j.mib.2017.11.017
Mycobacterium tuberculosis inhibits human innate immune responses via the production of TLR2 antagonist glycolipids. 10.1073/pnas.1707840114
Cyclipostins and Cyclophostin analogs as promising compounds in the fight against tuberculosis. 10.1038/s41598-017-11843-4
Legionella pneumophila Modulates Mitochondrial Dynamics to Trigger Metabolic Repurposing of Infected Macrophages. 10.1016/j.chom.2017.07.020
Combination therapy for tuberculosis treatment: pulmonary administration of ethionamide and booster co-loaded nanoparticles. 10.1038/s41598-017-05453-3
Host-directed therapies offer novel opportunities for the fight against tuberculosis. 10.1016/j.drudis.2017.05.005
Cyclodextrin-based nanocarriers containing a synergic drug combination: A potential formulation for pulmonary administration of antitubercular drugs. 10.1016/j.ijpharm.2017.05.030
Impact of pe_pgrs33 Gene Polymorphisms on Mycobacterium tuberculosis Infection and Pathogenesis. 10.3389/fcimb.2017.00137
Clofazimine encapsulation in nanoporous silica particles for the oral treatment of antibiotic-resistant Mycobacterium tuberculosis infections. 10.2217/nnm-2016-0364
Reversion of antibiotic resistance in Mycobacterium tuberculosis by spiroisoxazoline SMARt-420. 10.1126/science.aag1006
How can nanoparticles contribute to antituberculosis therapy? 10.1016/j.drudis.2017.01.011
Genome-wide, high-content siRNA screening identifies the Alzheimer's genetic risk factor FERMT2 as a major modulator of APP metabolism. 10.1007/s00401-016-1652-z
Identification of aminopyrimidine-sulfonamides as potent modulators of Wag31-mediated cell elongation in mycobacteria. 10.1111/mmi.13535
Mycobacterium tuberculosis LppM Displays an Original Structure and Domain Composition Linked to a Dual Localization. 10.1016/j.str.2016.07.009
Khaya grandifoliola C.DC: a potential source of active ingredients against hepatitis C virus in vitro. 10.1007/s00705-016-2771-5
[Mycolactone: the amazing analgesic mycobacterial toxin]. 10.1051/medsci/20163202007
A fragment merging approach towards the development of small molecule inhibitors of Mycobacterium tuberculosis EthR for use as ethionamide boosters. 10.1039/c5ob02630j
Polyphenols Inhibit Hepatitis C Virus Entry by a New Mechanism of Action. 10.1128/jvi.01473-15
Plant extracts from Cameroonian medicinal plants strongly inhibit hepatitis C virus infection in vitro. 10.3389/fmicb.2015.00488
Increased protective efficacy of recombinant BCG strains expressing virulence-neutral proteins of the ESX-1 secretion system. 10.1016/j.vaccine.2015.03.083
Cytosolic access of Mycobacterium tuberculosis: critical impact of phagosomal acidification control and demonstration of occurrence in vivo. 10.1371/journal.ppat.1004650
[High content screening in chemical biology: overview and main challenges]. 10.1051/medsci/20153102016
Testing chemical and genetic Modulators in Mycobacterium tuberculosis infected cells using phenotypic assays. 10.1007/978-1-4939-2450-9_24
2-Carboxyquinoxalines kill mycobacterium tuberculosis through noncovalent inhibition of DprE1. 10.1021/cb5007163
High-content screening technology combined with a human granuloma model as a new approach to evaluate the activities of drugs against Mycobacterium tuberculosis. 10.1128/aac.03705-14
Mycobacterial toxin induces analgesia in buruli ulcer by targeting the angiotensin pathways. 10.1016/j.cell.2014.04.040
Ligand efficiency driven design of new inhibitors of Mycobacterium tuberculosis transcriptional repressor EthR using fragment growing, merging, and linking approaches. 10.1021/jm500422b
Discovery of Q203, a potent clinical candidate for the treatment of tuberculosis. 10.1038/nm.3262
The balance of apoptotic and necrotic cell death in Mycobacterium tuberculosis infected macrophages is not dependent on bacterial virulence. 10.1371/journal.pone.0047573
Discovery of novel N-phenylphenoxyacetamide derivatives as EthR inhibitors and ethionamide boosters by combining high-throughput screening and synthesis. 10.1021/jm300377g
Ethionamide boosters. 2. Combining bioisosteric replacement and structure-based drug design to solve pharmacokinetic issues in a series of potent 1,2,4-oxadiazole EthR inhibitors. 10.1021/jm200825u
A novel specific edge effect correction method for RNA interference screenings. 10.1093/bioinformatics/btr648
Analogous mechanisms of resistance to benzothiazinones and dinitrobenzamides in Mycobacterium smegmatis. 10.1371/journal.pone.0026675
High-content screening in infectious diseases. 10.1016/j.cbpa.2011.05.023
Ethionamide boosters: synthesis, biological activity, and structure-activity relationships of a series of 1,2,4-oxadiazole EthR inhibitors. 10.1021/jm200076a
Shortening the drug discovery pipeline: small molecule high content screening for lead discovery in neglected disease. 10.1186/1753-6561-5-s1-p38
High content phenotypic cell-based visual screen identifies Mycobacterium tuberculosis acyltrehalose-containing glycolipids involved in phagosome remodeling. 10.1371/journal.ppat.1001100
High-content imaging of Mycobacterium tuberculosis-infected macrophages: an in vitro model for tuberculosis drug discovery. 10.4155/fmc.10.223
Functional characterization of the Mycobacterium tuberculosis serine/threonine kinase PknJ. 10.1099/mic.0.038133-0
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
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Control of M. tuberculosis ESAT-6 secretion and specific T cell recognition by PhoP. 10.1371/journal.ppat.0040033
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