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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

Silva-Miranda, Mayra Ekaza, Euloge Breiman, Adrien Asehnoune, Karim Barros-Aguirre, David Pethe, Kevin Ewann, Fanny Brodin, Priscille Ballell-Pages, Llus Altare, Frederic

Antimicrobial agents and chemotherapy, 2015-1

https://doi.org/10.1128/aac.03705-14

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

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

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

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

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

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

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

Inactivation of Rv2525c, a substrate of the twin arginine translocation (Tat) system of Mycobacterium tuberculosis, increases beta-lactam susceptibility and virulence 10.1128/jb.00631-06

Evaluation of vaccines in the EU TB vaccine cluster using a guinea pig aerosol infection model of tuberculosis 10.1016/j.tube.2004.09.009

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

Enhanced protection against tuberculosis by vaccination with recombinant Mycobacterium microti vaccine that induces T cell immunity against region of difference 1 antigens 10.1086/421468

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

Macro-array and bioinformatic analyses reveal mycobacterial 'core' genes, variation in the ESAT-6 gene family and new phylogenetic markers for the Mycobacterium tuberculosis complex 10.1099/mic.0.26662-0

CD8(+)-T-cell responses of mycobacterium-infected mice to a newly identified major histocompatibility complex class I-restricted epitope shared by proteins of the ESAT-6 family 10.1128/iai.71.12.7173-7177.2003

Recombinant BCG exporting ESAT-6 confers enhanced protection against tuberculosis 10.1038/nm859

A new evolutionary scenario for the Mycobacterium tuberculosis complex 10.1073/pnas.052548299

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

Loss of RD1 contributed to the attenuation of the live tuberculosis vaccines Mycobacterium bovis BCG and Mycobacterium microti 10.1046/j.1365-2958.2002.03237.x

6-Oxocytidine containing oligonucleotides inhibit the HIV-1 integrase in vitro 10.1081/ncn-100002322

Determinants of Mg2+-dependent activities of recombinant human immunodeficiency virus type 1 integrase 10.1021/bi000398b

Inhibition of the human immunodeficiency virus type 1 DNA integration by modified oligonucleotides 10.1023/a:1026631910681

Branched oligonucleotide-intercalator conjugate forming a parallel stranded structure inhibits HIV-1 integrase 10.1016/s0014-5793(99)01350-2

Inhibition of HIV-1 integration by mono- & bi-functionalized triple helix forming oligonucleotides 10.1080/07328319908044831

Optimization of alternate-strand triple helix formation at the 5 '-TpA-3 ' and 5 '-ApT-3 ' junctions 10.1093/nar/27.15.3029

A truncated HIV-1 Tat protein basic domain rapidly translocates through the plasma membrane and accumulates in the cell nucleus 10.1074/jbc.272.25.16010

Mycobacterium tuberculosis inhibits human innate immune responses via the production of TLR2 antagonist glycolipids 10.1073/pnas.1707840114

ArfGAP1 restricts Mycobacterium tuberculosis entry by controlling the actin cytoskeleton 10.15252/embr.201744371

ArfGAP1 restricts Mycobacterium tuberculosis entry by controlling the actin cytoskeleton 10.15252/embr.201744371 10.15252/embr.201744371.

Combination therapy for tuberculosis treatment: pulmonary administration of ethionamide and booster co-loaded nanoparticles 10.1038/s41598-017-05453-3

Cyclipostins and Cyclophostin analogs as promising compounds in the fight against tuberculosis 10.1038/s41598-017-11843-4 10.1038/s41598-017-11843-4.

Fragment-Sized EthR Inhibitors Exhibit Exceptionally Strong Ethionamide Boosting Effect in Whole-Cell Mycobacterium tuberculosis Assays 10.1021/acschembio.7b00091

Host-pathogen systems for early drug discovery against tuberculosis 10.1016/j.mib.2017.11.017 10.1016/j.mib.2017.11.017.

Legionella pneumophila Modulates Mitochondrial Dynamics to Trigger Metabolic Repurposing of Infected Macrophages 10.1016/j.chom.2017.07.020 10.1016/j.chom.2017.07.020. Epub 2017 Aug 31.

Mycobacterium tuberculosis Controls Phagosomal Acidification by Targeting CISH-Mediated Signaling 10.1016/j.celrep.2017.08.101 10.1016/j.celrep.2017.08.101.

Mycobacterium tuberculosis inhibits human innate immune responses via the production of TLR2 antagonist glycolipids 10.1073/pnas.1707840114 10.1073/pnas.1707840114.

Identification of Piperazinylbenzenesulfonamides as New Inhibitors of Claudin-1 Trafficking and Hepatitis C Virus Entry 10.1128/jvi.01982-17

Multiplexed Quantitation of Intraphagocyte Mycobacterium tuberculosis Secreted Protein Effectors 10.1016/j.celrep.2018.03.125

Oxadiazolone derivatives, new promising multi-target inhibitors against M. tuberculosis 10.1016/j.bioorg.2018.08.025

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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

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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

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

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T(oo)bAd. 10.1038/s41589-019-0347-x

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

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

frederic altare

altare frederic

ORCID: 0000-0002-5077-4616

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Author Correction: Alveolar macrophages are epigenetically altered after inflammation, leading to long-term lung immunoparalysis. 10.1038/s41590-020-0739-9

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Emergence in Western African countries of MDR-TB, focus on Côte d'Ivoire. 10.1155/2013/426709

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In a novel form of IFN-gamma receptor 1 deficiency, cell surface receptors fail to bind IFN-gamma. 10.1172/jci9166

Helicobacter pylori in children with peptic ulcer and their families. 10.1007/bf01297021

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A causative relationship between mutant IFNgR1 alleles and impaired cellular response to IFNgamma in a compound heterozygous child. 10.1086/301750

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Eighteen month follow up of Helicobacter pylori positive children treated with amoxycillin and tinidazole. 10.1136/gut.33.10.1328

Lluis Ballell

Ballell Lluis

ORCID: 0000-0002-3029-1860

In vivo Enhancement in Bioavailability of Atazanavir in the Presence of Proton-Pump Inhibitors using Mesoporous Materials 10.1002/cmdc.201100500

The antibiotic cyclomarin blocks arginine-phosphate–induced millisecond dynamics in the N-terminal domain of ClpC1 fromMycobacterium tuberculosis 10.1074/jbc.ra118.002251

In vivo potent BM635 analogue with improved drug-like properties 10.1016/j.ejmech.2017.12.075

Synthesis, antimycobacterial activity and influence on mycobacterial InhA and PknB of 12-membered cyclodepsipeptides 10.1016/j.bmc.2018.04.045

Antimycobacterial drug discovery using Mycobacteria-infected amoebae identifies anti-infectives and new molecular targets 10.1038/s41598-018-22228-6

A multitarget approach to drug discovery inhibiting Mycobacterium tuberculosis PyrG and PanK 10.1038/s41598-018-21614-4

Accelerating Early Antituberculosis Drug Discovery by Creating Mycobacterial Indicator Strains That Predict Mode of Action 10.1128/aac.00083-18

New Small-Molecule Synthetic Antimycobacterials 10.1128/aac.00399-07

A New Chemical Probe for Proteomics of Carbohydrate-Binding Proteins 10.1002/cbic.200400209

Author Correction: Prioritizing multiple therapeutic targets in parallel using automated DNA-encoded library screening 10.1038/ncomms16227

Inhibiting mycobacterial tryptophan synthase by targeting the inter-subunit interface 10.1038/s41598-017-09642-y

Pharmaceutical salt of BM635 with improved bioavailability 10.1016/j.ejps.2016.12.003

Design, synthesis and structure-activity relationship study of wollamide B; a new potential anti TB agent 10.1371/journal.pone.0176088

Target Identification of Mycobacterium tuberculosis Phenotypic Hits Using a Concerted Chemogenomic, Biophysical, and Structural Approach 10.3389/fphar.2017.00681

A Phenotypic Based Target Screening Approach Delivers New Antitubercular CTP Synthetase Inhibitors 10.1021/acsinfecdis.7b00006

Prioritizing multiple therapeutic targets in parallel using automated DNA-encoded library screening 10.1038/ncomms16081

Novel inhibitors of Mycobacterium tuberculosis GuaB2 identified by a target based high-throughput phenotypic screen 10.1038/srep38986

Open Lab as a source of hits and leads against tuberculosis, malaria and kinetoplastid diseases 10.1038/nrd.2016.51

A new piperidinol derivative targeting mycolic acid transport inMycobacterium abscessus 10.1111/mmi.13406

Repurposing clinically approved cephalosporins for tuberculosis therapy 10.1038/srep34293

β-Lactams against Tuberculosis — New Trick for an Old Dog? 10.1056/nejmc1513236

New direct inhibitors of InhA with antimycobacterial activity based on a tetrahydropyran scaffold 10.1016/j.ejmech.2016.02.008

THPP target assignment reveals EchA6 as an essential fatty acid shuttle in mycobacteria 10.1038/nmicrobiol.2015.6

Searching for New Leads for Tuberculosis: Design, Synthesis, and Biological Evaluation of Novel 2-Quinolin-4-yloxyacetamides 10.1021/acs.jmedchem.6b00245

N-Benzyl-4-((heteroaryl)methyl)benzamides: A New Class of Direct NADH-Dependent 2-transEnoyl-Acyl Carrier Protein Reductase (InhA) Inhibitors with Antitubercular Activity 10.1002/cmdc.201600020

Antitubercular drugs for an old target: GSK693 as a promising InhA direct inhibitor 10.1016/j.ebiom.2016.05.006

Identification of KasA as the cellular target of an anti-tubercular scaffold 10.1038/ncomms12581

Essential but Not Vulnerable: Indazole Sulfonamides Targeting Inosine Monophosphate Dehydrogenase as Potential Leads against Mycobacterium tuberculosis 10.1021/acsinfecdis.6b00103

Non-absorbable mesoporous silica for the development of protein sequestration therapies 10.1016/j.bbrc.2015.09.071

Mycobacterial Dihydrofolate Reductase Inhibitors Identified Using Chemogenomic Methods and In Vitro Validation 10.1371/journal.pone.0121492

Hydrolysis of Clavulanate by Mycobacterium tuberculosis β-Lactamase BlaC Harboring a Canonical SDN Motif 10.1128/aac.00598-15

A Focused Screen Identifies Antifolates with Activity on Mycobacterium tuberculosis 10.1021/acsinfecdis.5b00063

Combinations of β-Lactam Antibiotics Currently in Clinical Trials Are Efficacious in a DHP-I-Deficient Mouse Model of Tuberculosis Infection 10.1128/aac.01063-15

Mycobacterium tuberculosis Gyrase Inhibitors as a New Class of Antitubercular Drugs 10.1128/aac.03913-14

Whole Cell Target Engagement Identifies Novel Inhibitors of Mycobacterium tuberculosis Decaprenylphosphoryl-β-d-ribose Oxidase 10.1021/acsinfecdis.5b00065

Carbamoyl Triazoles, Known Serine Protease Inhibitors, Are a Potent New Class of Antimalarials 10.1021/acs.jmedchem.5b00434

A Developability-Focused Optimization Approach Allows Identification of in Vivo Fast-Acting Antimalarials: N-[3-[(Benzimidazol-2-yl)amino]propyl]amides 10.1021/acs.jmedchem.5b00114

Release of 50 new, drug-like compounds and their computational target predictions for open source anti-tubercular drug discovery 10.1371/journal.pone.0142293

Large pore mesoporous silica induced weight loss in obese mice 10.2217/nnm.13.138

Rapid Cytolysis of Mycobacterium tuberculosis by Faropenem, an Orally Bioavailable β-Lactam Antibiotic 10.1128/aac.03461-14

Collaborative approaches for Target ID in neglected diseases: identifying new antimalarial targets 10.1186/1475-2875-13-s1-p54

Encapsulation of Anti-Tuberculosis Drugs within Mesoporous Silica and Intracellular Antibacterial Activities 10.3390/nano4030813

Biochemical and Structural Characterization of Mycobacterial Aspartyl-tRNA Synthetase AspS, a Promising TB Drug Target 10.1371/journal.pone.0113568

Testing Tuberculosis Drug Efficacy in a Zebrafish High-Throughput Translational Medicine Screen 10.1128/aac.03588-14

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

Design, Synthesis, and Evaluation of New Thiadiazole-Based Direct Inhibitors of Enoyl Acyl Carrier Protein Reductase (InhA) for the Treatment of Tuberculosis 10.1021/jm501029r

Encoded Library Technology as a Source of Hits for the Discovery and Lead Optimization of a Potent and Selective Class of Bactericidal Direct Inhibitors of Mycobacterium tuberculosis InhA 10.1021/jm401326j

In vivo oral toxicological evaluation of mesoporous silica particles 10.2217/nnm.12.77

Discovery of novel InhA reductase inhibitors: application of pharmacophore- and shape-based screening approach 10.4155/fmc.12.211

Improved BM212 MmpL3 Inhibitor Analogue Shows Efficacy in Acute Murine Model of Tuberculosis Infection 10.1371/journal.pone.0056980

Tetrahydropyrazolo[1,5-a]Pyrimidine-3-Carboxamide and N-Benzyl-6′,7′-Dihydrospiro[Piperidine-4,4′-Thieno[3,2-c]Pyran] Analogues with Bactericidal Efficacy against Mycobacterium tuberculosis Targeting MmpL3 10.1371/journal.pone.0060933

Fueling Open-Source Drug Discovery: 177 Small-Molecule Leads against Tuberculosis 10.1002/cmdc.201200428

Identification of Novel Imidazo[1,2-a]pyridine Inhibitors Targeting M. tuberculosis QcrB 10.1371/journal.pone.0052951

4-Substituted Thioquinolines and Thiazoloquinolines: Potent, Selective, and Tween-80 in vitro Dependent Families of Antitubercular Agents with Moderate in vivo Activity 10.1002/cmdc.201100309

Synthesis and Evaluation of New Thiodigalactoside-Based Chemical Probes to Label Galectin-3 10.1002/cbic.200900198

New thiopyrazolo[3,4-d]pyrimidine derivatives as anti-mycobacterial agents 10.1016/j.bmcl.2006.12.066

New Thiopyrazolo[3,4-d]pyrimidine Derivatives as Antimycobacterial Agents. 10.1002/chin.200730194

A new chemical probe for the detection of the cancer-linked galectin-3 10.1039/b611050a

New Small-Molecule Synthetic Antimycobacterials 10.1128/aac.49.6.2153-2163.2005

Synthesis and evaluation of mimetics of UDP and UDP-α-d-galactose, dTDP and dTDP-α-d-glucose with monosaccharides replacing the key pyrophosphate unit 10.1039/b500418g

Microwave-assisted, tin-mediated, regioselective 3-O-alkylation of galactosides 10.1016/j.tetlet.2004.06.113

Amino alditols as inhibitors of mycobacterial cell wall biosynthesis 10.1042/bst030a027a

An open toolkit for tracking open science partnership implementation and impact [version 1; peer review: awaiting peer review] 10.12688/gatesopenres.12958.1

An open toolkit for tracking open science partnership implementation and impact [version 2; peer review: 2 approved] 10.12688/gatesopenres.12958.2

Kevin Pethe

Pethe Kevin

ORCID: 0000-0003-0916-8873

Bedaquiline inhibits the ATP synthase in mycobacterium abscessus and is effective in infected zebrafish 10.1128/AAC.01225-17

Biosynthesis and recycling of nicotinamide cofactors in Mycobacterium tuberculosis: An essential role for NAD in nonreplicating bacilli 10.1074/jbc.M800694200

Nanoparticles of Short Cationic Peptidopolysaccharide Self-Assembled by Hydrogen Bonding with Antibacterial Effect against Multidrug-Resistant Bacteria 10.1021/acsami.7b12120

Gluconeogenic carbon flow of tricarboxylic acid cycle intermediates is critical for Mycobacterium tuberculosis to establish and maintain infection 10.1073/pnas.1000715107

Discovery of tetrahydropyrazolopyrimidine carboxamide derivatives as potent and orally active antitubercular agents 10.1021/ml400071a

Inhibitors of energy metabolism interfere with antibiotic-induced death in mycobacteria 10.1074/jbc.RA118.005732

Microbiomes in respiratory health and disease: An Asia-Pacific perspective 10.1111/resp.12971

Next-generation antimicrobials: From chemical biology to first-in-class drugs 10.1007/s12272-015-0645-0

Characterization of Phosphofructokinase Activity in Mycobacterium tuberculosis Reveals That a Functional Glycolytic Carbon Flow Is Necessary to Limit the Accumulation of Toxic Metabolic Intermediates under Hypoxia 10.1371/journal.pone.0056037

Transient requirement of the PrrA-PrrB two-component system for early intracellular multiplication of Mycobacterium tuberculosis 10.1128/IAI.70.5.2256-2263.2002

New 2-Ethylthio-4-methylaminoquinazoline derivatives inhibiting two subunits of cytochrome bc1 in Mycobacterium tuberculosis 10.1371/journal.ppat.1008270

Targeting the Mycobacterium ulcerans cytochrome bc 1 :aa 3 for the treatment of Buruli ulcer 10.1038/s41467-018-07804-8

Target Engagement and Binding Mode of an Antituberculosis Drug to Its Bacterial Target Deciphered in Whole Living Cells by NMR 10.1021/acs.biochem.8b00975

Oxidative phosphorylation as a target space for tuberculosis: Success, caution, and future directions 10.1128/microbiolspec.TBTB2-0014-2016

EthA/R-independent killing of Mycobacterium tuberculosis by ethionamide 10.3389/fmicb.2017.00710

Isolation of Mycobacterium tuberculosis mutants defective in the arrest of phagosome maturation 10.1073/pnas.0401657101

Para-aminosalicylic acid is a prodrug targeting dihydrofolate reductase in mycobacterium tuberculosis 10.1074/jbc.M113.475798

Indolcarboxamide is a preclinical candidate for treating multidrug-resistant tuberculosis 10.1126/scitranslmed.3007355

The heparin-binding haemagglutinin of M. tuberculosis is required for extrapulmonary dissemination 10.1038/35084083

Mycobacterium smegmatis laminin-binding glycoprotein shares epitopes with Mycobacterium tuberculosis heparin-binding haemagglutinin 10.1046/j.1365-2958.2001.02206.x

The protonmotive force is required for maintaining ATP homeostasis and viability of hypoxic, nonreplicating Mycobacterium tuberculosis 10.1073/pnas.0711697105

M. tuberculosis Rv2252 encodes a diacylglycerol kinase involved in the biosynthesis of phosphatidylinositol mannosides (PIMs) 10.1111/j.1365-2958.2006.05174.x

The role of acute and chronic respiratory colonization and infections in the pathogenesis of COPD 10.1111/resp.13032

Triacylglycerol utilization is required for regrowth of in vitro hypoxic nonreplicating Mycobacterium bovis bacillus Calmette-Guerin 10.1128/JB.00530-09

Lead optimization of a novel series of imidazo[1,2-a]pyridine amides leading to a clinical candidate (Q203) as a multi- and extensively-drug- resistant anti-tuberculosis agent 10.1021/jm5003606

A chemical genetic screen in Mycobacterium tuberculosis identifies carbon-source-dependent growth inhibitors devoid of in vivo efficacy 10.1038/ncomms1060

Naturally-Occurring Polymorphisms in QcrB Are Responsible for Resistance to Telacebec in Mycobacterium abscessus 10.1021/acsinfecdis.9b00322

Arylvinylpiperazine amides, a new class of potent inhibitors targeting QcrB of mycobacterium tuberculosis 10.1128/mBio.01276-18

Nitrate respiration protects hypoxic Mycobacterium tuberculosisagainst acid- and reactive nitrogen species stresses 10.1371/journal.pone.0013356

The natural product cyclomarin kills mycobacterium tuberculosis by targeting the ClpC1 subunit of the caseinolytic protease 10.1002/anie.201101740

Active pulmonary targeting against tuberculosis (TB) via triple-encapsulation of Q203, bedaquiline and superparamagnetic iron oxides (SPIOs) in nanoparticle aggregates 10.1080/10717544.2019.1676841

Contribution of high-content imaging technologies to the development of anti-infective drugs 10.1002/cyto.a.22885

Role of the CD137 ligand (CD137L) signaling pathway during Mycobacterium tuberculosis infection 10.1016/j.imbio.2013.08.009

Nutrient-starved, non-replicating Mycobacterium tuberculosis requires respiration, ATP synthase and isocitrate lyase for maintenance of ATP homeostasis and viability 10.1099/mic.0.033084-0

Differential T and B cell responses against Mycobacterium tuberculosis heparin-binding hemagglutinin adhesin in infected healthy individuals and patients with tuberculosis 10.1086/338833

A rheostat mechanism governs the bifurcation of carbon flux in mycobacteria 10.1038/ncomms12527

Mycobacterial heparin-binding hemagglutinin and laminin-binding protein share antigenic methyllysines that confer resistance to proteolysis 10.1073/pnas.162246899

Discovery of Q203, a potent clinical candidate for the treatment of tuberculosis 10.1038/nm.3262

Sensitive profiling of chemically diverse bioactive lipids 10.1194/jlr.M700060-JLR200

Lysosomal killing of Mycobacterium mediated by ubiquitin-derived peptides is enhanced by autophagy 10.1073/pnas.0700036104

Eighty-kilodalton N-terminal moiety of Bordetella pertussis filamentous hemagglutinin: Adherence, immunogenicity, and protective role 10.1128/IAI.70.8.4142-4147.2002

Interaction of human Tamm-Horsfall glycoprotein with Bordetella pertussis toxin 10.1099/00221287-148-4-1193

Enantiomeric glycosylated cationic block co-beta-peptides eradicate Staphylococcus aureus biofilms and antibiotic-tolerant persisters 10.1038/s41467-019-12702-8

Carbon metabolism modulates the efficacy of drugs targeting the cytochrome bc 1 :aa 3 in Mycobacterium tuberculosis 10.1038/s41598-019-44887-9

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

Methylation-dependent T cell immunity to Mycobacterium tuberculosis heparin-binding hemagglutinin 10.1038/nm1090

Recombinase-based reporter system and antisense technology to study gene expression and essentiality in hypoxic nonreplicating mycobacteria 10.1111/j.1574-6968.2008.01193.x

Isolation and characterization of a hybrid respiratory supercomplex consisting of mycobacterium tuberculosis cytochrome bcc and mycobacterium smegmatis cytochrome aa3 10.1074/jbc.M114.624312

Urease activity represents an alternative pathway for Mycobacterium tuberculosis nitrogen metabolism 10.1128/IAI.06195-11

Targeting bacterial central metabolism for drug development 10.1016/j.chembiol.2014.08.020

Role of ADP-ribosyltransferase activity of pertussis toxin in toxin-adhesin redundancy with filamentous hemagglutinin during Bordetella pertussis infection 10.1128/IAI.69.10.6038-6043.2001

Therapeutic potential of promiscuous targets in Mycobacterium tuberculosis 10.1016/j.coph.2018.06.006

Enhanced bacterial virulence through exploitation of host glycosaminoglycans 10.1046/j.1365-2958.2002.02841.x

Characterization of the heparin-binding site of the mycobacterial heparin-binding hemagglutinin adhesin 10.1074/jbc.275.19.14273

An ethA-ethR-deficient Mycobacterium bovis BCG mutant displays increased adherence to mammalian cells and greater persistence in vivo, which correlate with altered mycolic acid composition 10.1128/IAI.01332-13

Exploiting the synthetic lethality between terminal respiratory oxidases to kill Mycobacterium tuberculosis and clear host infection 10.1073/pnas.1706139114

A high-throughput screen to identify inhibitors of ATP homeostasis in non-replicating mycobacterium tuberculosis 10.1021/cb2004884

Tuberculose, la porte vers la dissémination extra-pulmonaire 10.1051/medsci/200117111220

Mycobacterium tuberculosis with disruption in genes encoding the phosphate binding proteins PstS1 and PstS2 is deficient in phosphate uptake and demonstrates reduced in vivo virulence 10.1128/IAI.73.3.1898-1902.2005