Identification of aminopyrimidine-sulfonamides as potent modulators of Wag31-mediated cell elongation in mycobacteria
Vinayak Singh Neeraj Dhar János Pató Gaëlle S. Kolly Jana Korduláková Martin Forbak Joanna C. Evans Rita Székely Jan Rybniker Zuzana Palčeková Júlia Zemanová Isabella Santi François Signorino-Gelo Liliana Rodrigues Anthony Vocat Adrian S. Covarrubias Monica G. Rengifo Kai Johnsson Sherry Mowbray Joseph Buechler Vincent Delorme Priscille Brodin Graham W. Knott José A. Aínsa Digby F. Warner György Kéri Katarína Mikušová John D. McKinney Stewart T. Cole Valerie Mizrahi Ruben C. Hartkoorn
Graham W Knott
Knott Graham W
ORCID: 0000-0002-2956-9052
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Benzothiazinones Kill Mycobacterium tuberculosis by blocking Arabinan synthesis 10.1126/science.1171583
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Priscille Brodin
Brodin Priscille
ORCID: 0000-0003-0991-7344
Email: priscille.brodin@inserm.fr
How can nanoparticles contribute to antituberculosis therapy? 10.1016/j.drudis.2017.01.011
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Clofazimine encapsulation in nanoporous silica particles for the oral treatment of antibiotic-resistant Mycobacterium tuberculosis infections 10.2217/nnm-2016-0364
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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
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Identification of aminopyrimidine-sulfonamides as potent modulators of Wag31-mediated cell elongation in mycobacteria 10.1111/mmi.13535
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LppM impact on the colonization of macrophages by Mycobacterium tuberculosis 10.1111/cmi.12619
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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
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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
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
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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
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Impact of Mycobacterium ulcerans biofilm on transmissibility to ecological niches and Buruli ulcer pathogenesis 10.1371/journal.ppat.0030062
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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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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
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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
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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
Proteomics of Mycobacterium infection: Moving towards a Better Understanding of Pathogen-Driven immunomodulation 10.3389/fimmu.2018.00086
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
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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
José Antonio Aínsa Claver
Aínsa Claver José Antonio / José Antonio Aínsa
ORCID: 0000-0003-2076-844X
Selective Targeting of Human and Animal Pathogens of the Helicobacter Genus by Flavodoxin Inhibitors: Efficacy, Synergy, Resistance and Mechanistic Studies 10.3390/ijms221810137
Design, synthesis and inhibitory activity against Mycobacterium tuberculosis thymidine monophosphate kinase of acyclic nucleoside analogues with a distal imidazoquinolinone 10.1016/j.ejmech.2010.09.056
Transcriptional analysis of and resistance level conferred by the aminoglycoside acetyltransferase gene aac(2')-Id from Mycobacterium smegmatis. 10.1093/jac/dkm440
Aminoglycoside 2'-N-acetyltransferase genes are universally present in mycobacteria: Characterization of the aac(2')-lc gene from Mycobacterium tuberculosis and the aac(2')-ld gene from Mycobacterium smegmatis 10.1046/j.1365-2958.1997.3471717.x
Construction of a family of Mycobacterium/Escherichia coli shuttle vectors derived from pAL5000 and pACYC184: Their use for cloning an antibiotic-resistance gene from Mycobacterium fortuitum 10.1016/0378-1119(96)00202-8
Spectinamides: a new class of semisynthetic antituberculosis agents that overcome native drug efflux 10.1038/nm.3458
Analysis of Mutations in Streptomycin-Resistant Strains Reveals a Simple and Reliable Genetic Marker for Identification of the Mycobacterium tuberculosis Beijing Genotype 10.1128/JCM.01944-12
Zanthoxylum capense constituents with antimycobacterial activity against Mycobacterium tuberculosis in vitro and ex vivo within human macrophages 10.1016/j.jep.2013.01.013
Role of the Mmr Efflux Pump in Drug Resistance in Mycobacterium tuberculosis 10.1128/AAC.01482-12
Mycobacterial Shuttle Vectors Designed for High-Level Protein Expression in Infected Macrophages 10.1128/AEM.01674-12
Functional and Genetic Characterization of the Tap Efflux Pump in Mycobacterium bovis BCG 10.1128/AAC.05946-11
A Prodrug Approach for Improving Antituberculosis Activity of Potent Mycobacterium tuberculosis Type II Dehydroquinase Inhibitors 10.1021/jm2006063
Antimycobacterial evaluation and preliminary phytochemical investigation of selected medicinal plants traditionally used in Mozambique 10.1016/j.jep.2011.04.062
The complex whiJ locus mediates environmentally sensitive repression of development of Streptomyces coelicolor A3(2) 10.1007/s10482-010-9443-3
Role of the Mycobacterium tuberculosis P55 Efflux Pump in Intrinsic Drug Resistance, Oxidative Stress Responses, and Growth 10.1128/AAC.00550-09
Contribution of the Rv2333c efflux pump (the Stp protein) from Mycobacterium tuberculosis to intrinsic antibiotic resistance in Mycobacterium bovis BCG 10.1093/jac/dkl510
Novel streptomycin resistance gene from Mycobacterium fortuitum 10.1128/AAC.00223-06
Characterization of tetracycline resistance mediated by the efflux pump Tap from Mycobacterium fortuitum 10.1093/jac/dki436
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Characterization of P55, a multidrug efflux pump in Mycobacterium bovis and Mycobacterium tuberculosis 10.1128/AAC.45.3.800-804.2001
WhiA, a protein of unknown function conserved among gram-positive bacteria, is essential for sporulation in Streptomyces coelicolor A3(2) 10.1128/JB.182.19.5470-5478.2000
A response regulator-like protein that functions at an intermediate stage of sporulation in Streptomyces coelicolor A3(2) 10.1046/j.1365-2958.1999.01630.x
Inhibitors of mycobacterial efflux pumps as potential boosters for anti-tubercular drugs. 10.1586/eri.12.89
Lipid transport in Mycobacterium tuberculosis and its implications in virulence and drug development 10.1016/j.bcp.2015.05.001
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Antituberculosis drugs: reducing efflux = increasing activity 10.1016/j.drudis.2017.01.002
Discovery of antimicrobial compounds targeting bacterial type FAD synthetases 10.1080/14756366.2017.1411910
The EU approved antimalarial pyronaridine shows antitubercular activity and synergy with rifampicin, targeting RNA polymerase. 10.1016/j.tube.2018.08.004
Total Synthesis of Ripostatin B and Structure-Activity Relationship Studies on Ripostatin Analogs. 10.1021/acs.joc.8b00193
Ionophore A23187 shows anti-tuberculosis activity and synergy with tebipenem. 10.1016/j.tube.2017.09.001
Structure Guided Lead Generation toward Nonchiral M. tuberculosis Thymidylate Kinase Inhibitors. 10.1021/acs.jmedchem.7b01570
Identification of aminopyrimidine-sulfonamides as potent modulators of Wag31-mediated cell elongation in mycobacteria. 10.1111/mmi.13535
Structure-Activity Relationships of Spectinamide Antituberculosis Agents: A Dissection of Ribosomal Inhibition and Native Efflux Avoidance Contributions. 10.1021/acsinfecdis.6b00158
How can nanoparticles contribute to antituberculosis therapy? 10.1016/j.drudis.2017.01.011
Boldine-Derived Alkaloids Inhibit the Activity of DNA Topoisomerase I and Growth of Mycobacterium tuberculosis. 10.3389/fmicb.2018.01659
Synergy between Circular Bacteriocin AS-48 and Ethambutol against Mycobacterium tuberculosis. 10.1128/aac.00359-18
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Polypeptidic Micelles Stabilized with Sodium Alginate Enhance the Activity of Encapsulated Bedaquiline 10.1002/mabi.201800397
Co-delivery of free vancomycin and transcription factor decoy-nanostructured lipid carriers can enhance inhibition of methicillin resistant Staphylococcus aureus (MRSA) 10.1371/journal.pone.0220684
In silico discovery and biological validation of ligands of FAD synthase, a promising new antimicrobial target 10.1371/journal.pcbi.1007898
Nanotechnology‐Based Targeted Drug Delivery: An Emerging Tool to Overcome Tuberculosis 10.1002/adtp.202000113
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
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Comparison of chlorine and peroxyacetic-based disinfectant to inactivate Feline calicivirus, Murine norovirus and Hepatitis A virus on lettuce. 10.1016/j.ijfoodmicro.2011.08.011
Direct detection of highly pathogenic avian influenza A/H5N1 virus from mud specimens. 10.1016/j.jviromet.2011.06.002
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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
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Cyclodextrin-based nanocarriers containing a synergic drug combination: A potential formulation for pulmonary administration of antitubercular drugs. 10.1016/j.ijpharm.2017.05.030
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Clofazimine encapsulation in nanoporous silica particles for the oral treatment of antibiotic-resistant Mycobacterium tuberculosis infections. 10.2217/nnm-2016-0364
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How can nanoparticles contribute to antituberculosis therapy? 10.1016/j.drudis.2017.01.011
Genome-wide, high-content siRNA screening identifies the Alzheimer's genetic risk factor FERMT2 as a major modulator of APP metabolism. 10.1007/s00401-016-1652-z
Identification of aminopyrimidine-sulfonamides as potent modulators of Wag31-mediated cell elongation in mycobacteria. 10.1111/mmi.13535
Mycobacterium tuberculosis LppM Displays an Original Structure and Domain Composition Linked to a Dual Localization. 10.1016/j.str.2016.07.009
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A fragment merging approach towards the development of small molecule inhibitors of Mycobacterium tuberculosis EthR for use as ethionamide boosters. 10.1039/c5ob02630j
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
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Testing chemical and genetic Modulators in Mycobacterium tuberculosis infected cells using phenotypic assays. 10.1007/978-1-4939-2450-9_24
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High-content screening technology combined with a human granuloma model as a new approach to evaluate the activities of drugs against Mycobacterium tuberculosis. 10.1128/aac.03705-14
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
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Ethionamide boosters: synthesis, biological activity, and structure-activity relationships of a series of 1,2,4-oxadiazole EthR inhibitors. 10.1021/jm200076a
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
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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
Functional analysis of early secreted antigenic target-6, the dominant T-cell antigen of Mycobacterium tuberculosis, reveals key residues involved in secretion, complex formation, virulence, and immunogenicity. 10.1074/jbc.m503515200
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
Macro-array and bioinformatic analyses reveal mycobacterial 'core' genes, variation in the ESAT-6 gene family and new phylogenetic markers for the Mycobacterium tuberculosis complex. 10.1099/mic.0.26662-0
CD8+-T-cell responses of Mycobacterium-infected mice to a newly identified major histocompatibility complex class I-restricted epitope shared by proteins of the ESAT-6 family. 10.1128/iai.71.12.7173-7177.2003
Recombinant BCG exporting ESAT-6 confers enhanced protection against tuberculosis. 10.1038/nm859
Loss of RD1 contributed to the attenuation of the live tuberculosis vaccines Mycobacterium bovis BCG and Mycobacterium microti. 10.1046/j.1365-2958.2002.03237.x
Bacterial artificial chromosome-based comparative genomic analysis identifies Mycobacterium microti as a natural ESAT-6 deletion mutant. 10.1128/iai.70.10.5568-5578.2002
Disruption of HIV-1 integrase-DNA complexes by short 6-oxocytosine-containing oligonucleotides. 10.1021/bi015732y
IRG1 controls immunometabolic host response and restricts intracellular Mycobacterium tuberculosis infection 10.1101/761551
Large scale screening discovers clofoctol as an inhibitor of SARS-CoV-2 replication that reduces COVID-19-like pathology 10.1101/2021.06.30.450483
Vinayak Singh
Singh Vinayak / Vin
ORCID: 0000-0001-9002-2489
Identification and validation of novel drug targets in Mycobacterium tuberculosis 10.1016/j.drudis.2016.09.010
The Inosine Monophosphate Dehydrogenase, GuaB2, Is a Vulnerable New Bactericidal Drug Target for Tuberculosis 10.1021/acsinfecdis.6b00102
Overexpression of Rv3097c in Mycobacterium bovis BCG abolished the efficacy of BCG vaccine to protect against Mycobacterium tuberculosis infection in mice 10.1016/j.vaccine.2011.04.086
Downregulation of Rv0189c, encoding a dihydroxyacid dehydratase, affects growth of Mycobacterium tuberculosis in vitro and in mice 10.1099/mic.0.042358-0
3D-QSAR and molecular modeling studies on 2,3-dideoxy hexenopyranosid-4-uloses as anti-tubercular agents targeting alpha-mannosidase 10.1016/j.bioorg.2015.02.001
Predictive modeling targets thymidylate synthase ThyX in Mycobacterium tuberculosis 10.1038/srep27792
Deoxysugars as antituberculars and alpha-mannosidase inhibitors 10.1128/AAC.02715-13
Biochemical and transcription analysis of acetohydroxyacid synthase isoforms in Mycobacterium tuberculosis identifies these enzymes as potential targets for drug development 10.1099/mic.0.041343-0
Identification of Aminopyrimidine-Sulfonamides as Potent Modulators of Wag31-mediated Cell Elongation in Mycobacteria 10.1111/mmi.13535
The complex mechanism of antimycobacterial action of 5-fluorouracil 10.1016/j.chembiol.2014.11.006
Genome-Wide Transposon Mutagenesis in Mycobacterium tuberculosis and Mycobacterium smegmatis 10.1007/978-1-4939-6472-7_21
N-Acetylglucosamine-1-phosphate transferase, WecA, as a validated drug target in Mycobacterium tuberculosis. 10.1128/aac.01310-17
Detection of Mycobacterium tuberculosis bacilli in bio-aerosols from untreated TB patients 10.12688/gatesopenres.12758.1
Fragment-Based Approach to Targeting Inosine-5′-monophosphate Dehydrogenase (IMPDH) from Mycobacterium tuberculosis 10.1021/acs.jmedchem.7b01622
Hit discovery of Mycobacterium tuberculosis inosine 5′-monophosphate dehydrogenase, GuaB2, inhibitors 10.1016/j.bmcl.2018.04.045
Expanding Benzoxazole-Based Inosine 5′-Monophosphate Dehydrogenase (IMPDH) Inhibitor Structure-Activity As Potential Antituberculosis Agents 10.1021/acs.jmedchem.7b01839
Detection of Mycobacterium tuberculosis bacilli in bio-aerosols from untreated TB patients 10.12688/gatesopenres.12758.2
Synthesis and Structure–Activity relationship of 1-(5-isoquinolinesulfonyl)piperazine analogues as inhibitors of Mycobacterium tuberculosis IMPDH 10.1016/j.ejmech.2019.04.027
Drug-resistance in Mycobacterium tuberculosis: where we stand 10.1039/c9md00057g
Synergistic enhancement of beta-lactam antibiotics by modified tunicamycin analogs TunR1 and TunR2 10.1038/s41429-019-0220-x
Real-time investigation of tuberculosis transmission: Developing the respiratory aerosol sampling chamber (RASC) 10.1371/journal.pone.0146658
The quest for the holy grail: new antitubercular chemical entities, targets and strategies 10.1016/j.drudis.2020.02.003
Synthesis, Structure–Activity Relationship, and Mechanistic Studies of Aminoquinazolinones Displaying Antimycobacterial Activity 10.1021/acsinfecdis.0c00252
Design, synthesis and characterization of novel 2-(2, 3-dichlorophenyl)-5-aryl-1,3,4-oxadiazole derivatives for their anti-tubercular activity against Mycobacterium tuberculosis 10.1016/j.cdc.2020.100431
Current Scenario and Future Prospect in the Management of COVID-19 10.2174/0929867327666200908113642
6,11-Dioxobenzo[f]pyrido[1,2-a]indoles Kill Mycobacterium tuberculosis by Targeting Iron–Sulfur Protein Rv0338c (IspQ), A Putative Redox Sensor 10.1021/acsinfecdis.0c00531
Current advances in the clinical development of anti-tubercular agents. 10.1016/j.tube.2020.101989
Antitubercular 2-Pyrazolylpyrimidinones: Structure–Activity Relationship and Mode-of-Action Studies 10.1021/acs.jmedchem.0c01727
Tuberculosis: An Update on Pathophysiology, Molecular Mechanisms of Drug Resistance, Newer Anti-TB Drugs, Treatment Regimens and Host-Di-rected Therapies. 10.2174/1568026621999201211200447
Developing Synergistic Drug Combinations To Restore Antibiotic Sensitivity in Drug-Resistant Mycobacterium tuberculosis 10.1128/AAC.02554-20
An ABC transporter Wzm–Wzt catalyzes translocation of lipid-linked galactan across the plasma membrane in mycobacteria 10.1073/pnas.2023663118
Strategies to Combat Multi-Drug Resistance in Tuberculosis 10.1021/acs.accounts.0c00878
Rv0684/fusA1, an Essential Gene, Is the Target of Fusidic Acid and Its Derivatives in Mycobacterium tuberculosis 10.1021/acsinfecdis.1c00195
Current strategies in targeted anticancer drug delivery systems to brain 10.1016/b978-0-323-85503-7.00038-9
Benzoheterocyclic Oxime Carbamates Active against Mycobacterium tuberculosis: Synthesis, Structure–Activity Relationship, Metabolism, and Biology Triaging 10.1021/acs.jmedchem.1c00707
Perspectives on RNA Vaccine Candidates for COVID-19 10.3389/fmolb.2021.635245
Neurological Consequences of SARS-CoV-2 Infection and Concurrence of Treatment-Induced Neuropsychiatric Adverse Events in COVID-19 Patients: Navigating the Uncharted 10.3389/fmolb.2021.627723
Joanna Evans
Evans Joanna
ORCID: 0000-0002-4139-9527
Email: Joanna.evans@crick.ac.uk
Blocking Bacterial Naphthohydroquinone Oxidation and ADP-Ribosylation Improves Activity of Rifamycins against Mycobacterium abscessus 10.1128/aac.00978-21
A novel insertion sequence, ISPA26, in oprD of Pseudomonas aeruginosa is associated with carbapenem resistance. 10.1128/AAC.00837-07
Recent and rapid emergence of W-Beijing strains of Mycobacterium tuberculosis in Cape Town, South Africa. 10.1086/592575
Rapid genotypic assays to identify drug-resistant Mycobacterium tuberculosis in South Africa. 10.1093/jac/dkn433
Novel multiplex allele-specific PCR assays for the detection of resistance to second-line drugs in Mycobacterium tuberculosis. 10.1093/jac/dkq047
Reaction intermediate analogues as bisubstrate inhibitors of pantothenate synthetase. 10.1016/j.bmc.2014.01.017
The complex mechanism of antimycobacterial action of 5-fluorouracil. 10.1016/j.chembiol.2014.11.006
Nucleotide Metabolism and DNA Replication. 10.1128/microbiolspec.mgm2-0001-2013
The application of tetracyclineregulated gene expression systems in the validation of novel drug targets in Mycobacterium tuberculosis. 10.3389/fmicb.2015.00812
Validation of CoaBC as a Bactericidal Target in the Coenzyme A Pathway of Mycobacterium tuberculosis. 10.1021/acsinfecdis.6b00150
Identification of aminopyrimidine-sulfonamides as potent modulators of Wag31-mediated cell elongation in mycobacteria. 10.1111/mmi.13535
The Influence of HIV on the Evolution of Mycobacterium tuberculosis. 10.1093/molbev/msx107
Priming the tuberculosis drug pipeline: new antimycobacterial targets and agents. 10.1016/j.mib.2018.02.006
In vitro efficacies, ADME, and pharmacokinetic properties of phenoxazine derivatives active against Mycobacterium tuberculosis. 10.1128/aac.01010-19
Inhibiting Mycobacterium tuberculosis CoaBC by targeting an allosteric site. 10.1038/s41467-020-20224-x
Targeting Mycobacterium tuberculosis CoaBC through Chemical Inhibition of 4′-Phosphopantothenoyl-L-cysteine Synthetase (CoaB) Activity 10.1021/acsinfecdis.0c00904
Chemical validation of Mycobacterium tuberculosis phosphopantetheine adenylyltransferase using fragment linking and CRISPR interference 10.1101/2020.09.04.280388
Ruben Hartkoorn
Hartkoorn Ruben / Ruben C. Hartkoorn
ORCID: 0000-0001-7315-1553
A druggable secretory protein maturase of Toxoplasma essential for invasion and egress 10.7554/eLife.27480
Discovery and Biosynthesis of Gladiolin: A Burkholderia gladioli Antibiotic with Promising Activity against Mycobacterium tuberculosis 10.1021/jacs.7b03382
Identification of aminopyrimidine-sulfonamides as potent modulators of Wag31-mediated cell elongation in mycobacteria 10.1111/mmi.13535
MoS2/TiO2/SiNW surface as an effective substrate for LDI-MS detection of glucose and glutathione in real samples 10.1016/j.talanta.2017.04.061
The Inosine Monophosphate Dehydrogenase, GuaB2, Is a Vulnerable New Bactericidal Drug Target for Tuberculosis 10.1021/acsinfecdis.6b00102
Micrococcin P1-A bactericidal thiopeptide active against Mycobacterium tuberculosis 10.1016/j.tube.2016.07.011
2-Carboxyquinoxalines Kill Mycobacterium tuberculosis through Noncovalent Inhibition of DprE1 10.1021/cb5007163
Bioluminescence for Assessing Drug Potency against Nonreplicating Mycobacterium tuberculosis 10.1128/aac.00528-15
Lead selection and characterization of antitubercular compounds using the Nested Chemical Library 10.1016/j.tube.2015.02.028
The 8-Pyrrole-Benzothiazinones Are Noncovalent Inhibitors of DprE1 from Mycobacterium tuberculosis 10.1128/aac.00778-15
Thiophenecarboxamide Derivatives Activated by EthA Kill Mycobacterium tuberculosis by Inhibiting the CTP Synthetase PyrG 10.1016/j.chembiol.2015.05.016
Whole cell screen based identification of spiropiperidines with potent antitubercular properties 10.1016/j.bmcl.2015.05.087
Anticytolytic Screen Identifies Inhibitors of Mycobacterial Virulence Protein Secretion 10.1016/j.chom.2014.09.008
Assessing the essentiality of the decaprenyl-phospho-D-arabinofuranose pathway in Mycobacterium tuberculosis using conditional mutants 10.1111/mmi.12546
Cross-Resistance between Clofazimine and Bedaquiline through Upregulation of MmpL5 in Mycobacterium tuberculosis 10.1128/aac.00037-14
Mechanism of Action of 5-Nitrothiophenes against Mycobacterium tuberculosis 10.1128/aac.02693-13
Rv2466c Mediates the Activation of TP053 To Kill Replicating and Non-replicating Mycobacterium tuberculosis 10.1021/cb500149m
Towards a new combination therapy for tuberculosis with next generation benzothiazinones 10.1002/emmm.201303575
Synthesis and Antimycobacterial Activity of 2,1 '-Dihydropyridomycins 10.1021/ml300385q
Genome-Wide Definition of the SigF Regulon in Mycobacterium tuberculosis 10.1128/jb.06692-11
In Vitro Combination Studies of Benzothiazinone Lead Compound BTZ043 against Mycobacterium tuberculosis 10.1128/aac.01476-12
Streptomycin-Starved Mycobacterium tuberculosis 18b, a Drug Discovery Tool for Latent Tuberculosis 10.1128/aac.01125-12
Towards a new tuberculosis drug: pyridomycin - nature's isoniazid 10.1002/emmm.201201689
Virulence Regulator EspR of Mycobacterium tuberculosis Is a Nucleoid-Associated Protein 10.1371/journal.ppat.1002621
Tuberculosis drugs: new candidates and how to find more 10.2217/fmb.11.46
HIV protease inhibitors are substrates for OATP1A2, OATP1B1 and OATP1B3 and lopinavir plasma concentrations are influenced by SLCO1B1 polymorphisms 10.1097/FPC.0b013e328335b02d
Leads for antitubercular compounds from kinase inhibitor library screens 10.1016/j.tube.2010.09.001
Sigma Factor F Does Not Prevent Rifampin Inhibition of RNA Polymerase or Cause Rifampin Tolerance in Mycobacterium tuberculosis 10.1128/jb.00687-10
Simple Model for Testing Drugs against Nonreplicating Mycobacterium tuberculosis 10.1128/aac.00821-10
Intracellular 'boosting' of darunavir using known transport inhibitors in primary PBMC 10.1111/j.1365-2125.2009.03462.x
Intracellular accumulation of efavirenz and nevirapine is independent of P-glycoprotein activity in cultured CD4 T cells and primary human lymphocytes 10.1093/jac/dkp335
Cultured CD4T cells and primary human lymphocytes express hOATPs: intracellular accumulation of saquinavir and lopinavir 10.1038/bjp.2008.320
A rapid and sensitive HPLC-MS method for the detection of plasma and cellular rifampicin 10.1016/j.jchromb.2007.07.005
Differential drug susceptibility of intracellular and extracellular tuberculosis, and the impact of P-glycoprotein 10.1016/j.tube.2006.12.001
Tacrine-induced liver damage: an analysis of 19 candidate genes 10.1097/FPC.0b013e3282f1f12b
Down regulation of multidrug resistance protein-1 expression in patients with early rheumatoid arthritis exposed to methotrexate as a first disease-modifying antirheumatic drug 10.1136/ard.2005.049189
Low levels of pyrazinamide and ethambutol in children with tuberculosis and impact of age, nutritional status, and human immunodeficiency virus infection 10.1128/aac.50.2.407-413.2006
In vitro synergy and enhanced murine brain penetration of saquinavir coadministered with mefloquine 10.1124/jpet..105.086272
Modulation of the intracellular accumulation of saquinavir in peripheral blood mononuclear cells by inhibitors of MRP1, MRP2, P-gp and BCRP 10.1097/01.aids.0000194793.36175.40
Expression of P-glycoprotein, multidrug-resistance proteins 1 and 2 in CEM, CEMVBL, CEME1000, MDCKIIMRP1 and MDCKIIMRP2 cell lines 10.1097/01.aids.0000088212.77946.65
Pyrrolomycins Are Potent Natural Protonophores 10.1128/AAC.01450-19
Intragenic Distribution of IS 6110 in Clinical Mycobacterium tuberculosis Strains: Bioinformatic Evidence for Gene Disruption Leading to Underdiagnosed Antibiotic Resistance 10.1128/Spectrum.00019-21
Liliana Rodrigues
Rodrigues Liliana
ORCID: 0000-0002-2094-2666
Measuring efflux and permeability in mycobacteria. 10.1007/978-1-4939-2450-9_13
Role of the Mmr efflux pump in drug resistance in Mycobacterium tuberculosis. 10.1128/aac.01482-12
Inhibitors of mycobacterial efflux pumps as potential boosters for anti-tubercular drugs. 10.1586/eri.12.89
Contribution of efflux to the emergence of isoniazid and multidrug resistance in Mycobacterium tuberculosis. 10.1371/journal.pone.0034538
Genetic response of Salmonella enterica serotype Enteritidis to thioridazine rendering the organism resistant to the agent. 10.1016/j.ijantimicag.2011.08.013
Contribution of efflux activity to isoniazid resistance in the Mycobacterium tuberculosis complex. 10.1016/j.meegid.2011.08.009
Inhibition of drug efflux in mycobacteria with phenothiazines and other putative efflux inhibitors. 10.2174/157489111796064579
Ethidium bromide transport across Mycobacterium smegmatis cell-wall: correlation with antibiotic resistance. 10.1186/1471-2180-11-35
Physiological characterisation of the efflux pump system of antibiotic-susceptible and multidrug-resistant Enterobacter aerogenes. 10.1016/j.ijantimicag.2010.06.036
Molecular tools for rapid identification and novel effective therapy against MDRTB/XDRTB infections. 10.1586/eri.10.20
Evaluation of efflux activity of bacteria by a semi-automated fluorometric system. 10.1007/978-1-60327-279-7_12
Fluorometric determination of ethidium bromide efflux kinetics in Escherichia coli. 10.1186/1754-1611-3-18
Identification of nontuberculous mycobacteria in clinical samples using molecular methods: a 3-year study. 10.1111/j.1469-0691.2009.03076.x
The role of efflux pumps in macrolide resistance in Mycobacterium avium complex. 10.1016/j.ijantimicag.2009.07.010
An AcrAB-mediated multidrug-resistant phenotype is maintained following restoration of wild-type activities by efflux pump genes and their regulators. 10.1016/j.ijantimicag.2009.06.029
pH Modulation of efflux pump activity of multi-drug resistant Escherichia coli: protection during its passage and eventual colonization of the colon. 10.1371/journal.pone.0006656
New methods for the identification of efflux mediated MDR bacteria, genetic assessment of regulators and efflux pump constituents, characterization of efflux systems and screening for inhibitors of efflux pumps. 10.2174/138945008785747734
Demonstration of intrinsic efflux activity of Escherichia coli K-12 AG100 by an automated ethidium bromide method. 10.1016/j.ijantimicag.2007.12.015
Thioridazine and chlorpromazine inhibition of ethidium bromide efflux in Mycobacterium avium and Mycobacterium smegmatis. 10.1093/jac/dkn070
Antibiotic stress, genetic response and altered permeability of E. coli. 10.1371/journal.pone.0000365
Direct application of the INNO-LiPA Rif.TB line-probe assay for rapid identification of Mycobacterium tuberculosis complex strains and detection of rifampin resistance in 360 smear-positive respiratory specimens from an area of high incidence of multidrug-resistant tuberculosis. 10.1128/jcm.43.9.4880-4884.2005
Antituberculosis drugs: reducing efflux=increasing activity. 10.1016/j.drudis.2017.01.002
Identification of aminopyrimidine-sulfonamides as potent modulators of Wag31-mediated cell elongation in mycobacteria. 10.1111/mmi.13535
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
Boldine-Derived Alkaloids Inhibit the Activity of DNA Topoisomerase I and Growth of Mycobacterium tuberculosis. 10.3389/fmicb.2018.01659
Total Synthesis of Ripostatin B and Structure-Activity Relationship Studies on Ripostatin Analogs. 10.1021/acs.joc.8b00193
Mycobacterial Aminoglycoside Acetyltransferases: A Little of Drug Resistance, and a Lot of Other Roles. 10.3389/fmicb.2019.00046
Design, Synthesis, and Efficacy Testing of Nitroethylene- and 7-Nitrobenzoxadiazol-Based Flavodoxin Inhibitors against Helicobacter pylori Drug-Resistant Clinical Strains and in Helicobacter pylori-Infected Mice 10.1021/acs.jmedchem.9b00355
O contributo dos serviços de diagnóstico laboratorial para o acesso universal à saúde nos países da Comunidade de Língua Portuguesa 10.25761/ANAISIHMT.337
Katarina Mikusova
Mikusova Katarina
ORCID: 0000-0002-0100-4877
Time-adjusted Analysis Shows Weak Associations Between BCG Vaccination Policy and COVID-19 Disease Progression 10.1101/2020.05.01.20087809
Synthesis, docking study and biological evaluation of ᴅ-fructofuranosyl and ᴅ-tagatofuranosyl sulfones as potential inhibitors of the mycobacterial galactan synthesis targeting the galactofuranosyltransferase GlfT2 10.3762/bjoc.16.152
Synthesis of the Arabinose Donor .beta.-D-Arabinofuranosyl-1-monophosphoryldecaprenol, Development of a Basic Arabinosyl-Transferase Assay, and Identification of Ethambutol as an Arabinosyl Transferase Inhibitor 10.1021/ja00153a002
Fragment-Based Design of Mycobacterium tuberculosis InhA Inhibitors 10.1021/acs.jmedchem.0c00007
Development of Macozinone for TB treatment: An Update 10.3390/app10072269
Design, synthesis and evaluation of covalent inhibitors of DprE1 as antitubercular agents 10.1016/j.ejmech.2020.112773
Biosynthesis of Galactan in Mycobacterium tuberculosis as a Viable TB Drug Target? 10.3390/antibiotics9010020
New Insights into the Mechanism of Action of the Thienopyrimidine Antitubercular Prodrug TP053 10.1021/acsinfecdis.9b00388
Development of 3,5-Dinitrophenyl-Containing 1,2,4-Triazoles and Their Trifluoromethyl Analogues as Highly Efficient Antitubercular Agents Inhibiting Decaprenylphosphoryl-β-d-ribofuranose 2′-Oxidase 10.1021/acs.jmedchem.9b00912
Drugging the Folate Pathway in Mycobacterium tuberculosis: The Role of Multi-targeting Agents 10.1016/j.chembiol.2019.02.013
New lipophilic isoniazid derivatives and their 1,3,4-oxadiazole analogues: Synthesis, antimycobacterial activity and investigation of their mechanism of action 10.1016/j.ejmech.2018.04.017
Copper-related toxicity in replicating and dormantMycobacterium tuberculosiscaused by 1-hydroxy-5-R-pyridine-2(1H)-thiones 10.1039/c8mt00067k
The EU approved antimalarial pyronaridine shows antitubercular activity and synergy with rifampicin, targeting RNA polymerase 10.1016/j.tube.2018.08.004
A multitarget approach to drug discovery inhibiting Mycobacterium tuberculosis PyrG and PanK 10.1038/s41598-018-21614-4
Identification of aminopyrimidine-sulfonamides as potent modulators of Wag31-mediated cell elongation in mycobacteria 10.1111/mmi.13535
Learning from the past for TB drug discovery in the future 10.1016/j.drudis.2016.09.025
N-Acetylglucosamine-1-Phosphate Transferase, WecA, as a Validated Drug Target in Mycobacterium tuberculosis 10.1128/aac.01310-17
A Phenotypic Based Target Screening Approach Delivers New Antitubercular CTP Synthetase Inhibitors 10.1021/acsinfecdis.7b00006
Design, Syntheses, and Anti-TB Activity of 1,3-Benzothiazinone Azide and Click Chemistry Products Inspired by BTZ043 10.1021/acsmedchemlett.5b00424
Development of 3,5-Dinitrobenzylsulfanyl-1,3,4-oxadiazoles and Thiadiazoles as Selective Antitubercular Agents Active Against Replicating and Nonreplicating Mycobacterium tuberculosis 10.1021/acs.jmedchem.5b00608
Assembling of theMycobacterium tuberculosisCell Wall Core 10.1074/jbc.m116.739227
Structural basis for selective recognition of acyl chains by the membrane-associated acyltransferase PatA 10.1038/ncomms10906
Lead selection and characterization of antitubercular compounds using the Nested Chemical Library 10.1016/j.tube.2015.02.028
The Complex Mechanism of Antimycobacterial Action of 5-Fluorouracil 10.1016/j.chembiol.2014.11.006
Thiophenecarboxamide Derivatives Activated by EthA Kill Mycobacterium tuberculosis by Inhibiting the CTP Synthetase PyrG 10.1016/j.chembiol.2015.05.016
The 8-Pyrrole-Benzothiazinones Are Noncovalent Inhibitors of DprE1 from Mycobacterium tuberculosis 10.1128/aac.00778-15
GtrA Protein Rv3789 Is Required for Arabinosylation of Arabinogalactan in Mycobacterium tuberculosis 10.1128/jb.00628-15
DprE1 Is a Vulnerable Tuberculosis Drug Target Due to Its Cell Wall Localization 10.1021/acschembio.5b00237
Purification and characterization of the acyltransferase involved in biosynthesis of the major mycobacterial cell envelope glycolipid – Monoacylated phosphatidylinositol dimannoside 10.1016/j.pep.2014.04.014
DprE1 - from the Discovery to the Promising Tuberculosis Drug Target 10.2174/138161282027140630122724
The Phosphatidyl-myo-Inositol Mannosyltransferase PimA Is Essential for Mycobacterium tuberculosis Growth In Vitro and In Vivo 10.1128/jb.01346-13
AnethA-ethR-Deficient Mycobacterium bovis BCG Mutant Displays Increased Adherence to Mammalian Cells and Greater PersistenceIn Vivo, Which Correlate with Altered Mycolic Acid Composition 10.1128/iai.01332-13
Identification of a small molecule with activity against drug-resistant and persistent tuberculosis 10.1073/pnas.1309171110
Novel synthetic (1 → 6)-α-d-mannodisaccharide substrates support processive mannosylation catalysed by the mycobacterial cell envelope enzyme fraction 10.1039/c3ra43575j
Benzothiazinones Are Suicide Inhibitors of Mycobacterial Decaprenylphosphoryl-β-d-ribofuranose 2′-Oxidase DprE1 10.1021/ja211042r
A Small Multidrug Resistance-like Transporter Involved in the Arabinosylation of Arabinogalactan and Lipoarabinomannan in Mycobacteria 10.1074/jbc.m112.400986
Protein Separation and Enzyme Purification by Preparative Capillary Isotachophoresis 10.1007/s10337-012-2348-8
Synthesis of 1,2,3-Triazolo-Linked Octyl (1→6)-α-d-Oligomannosides and Their Evaluation in Mycobacterial Mannosyltransferase Assay 10.1021/bc100421g
Investigation of ABC transporter from mycobacterial arabinogalactan biosynthetic cluster 10.4149/gpb_2011_03_239
Biosynthetic Origin of the Galactosamine Substituent of Arabinogalactan inMycobacterium tuberculosis 10.1074/jbc.m110.188110
Synthesis of alkyl and cycloalkyl α-d-mannopyranosides and derivatives thereof and their evaluation in the mycobacterial mannosyltransferase assay 10.1016/j.carres.2010.03.011
Synthetic UDP-Furanoses as Potent Inhibitors of Mycobacterial Galactan Biogenesis 10.1016/j.chembiol.2010.10.014
Biological and structural characterization of the Mycobacterium smegmatis nitroreductase NfnB, and its role in benzothiazinone resistance 10.1111/j.1365-2958.2010.07277.x
Benzothiazinones Kill Mycobacterium tuberculosis by Blocking Arabinan Synthesis 10.1126/science.1171583
Stereoselective syntheses of heptaprenylphosphoryl β-d-arabino-and β-d-ribo-furanoses 10.1016/j.tetlet.2009.02.188
Galactosyl Transferases in Mycobacterial Cell Wall Synthesis 10.1128/jb.01326-07
Identification of promoters recognized by RNA polymerase containing Mycobacterium tuberculosis stress-response sigma factor σF 10.1007/s00203-006-0185-6
Molecular Recognition and Interfacial Catalysis by the Essential Phosphatidylinositol Mannosyltransferase PimA from Mycobacteria 10.1074/jbc.m702087200
Identification of a Novel Galactosyl Transferase Involved in Biosynthesis of the Mycobacterial Cell Wall 10.1128/jb.00489-06
Decaprenylphosphoryl Arabinofuranose, the Donor of the d-Arabinofuranosyl Residues of Mycobacterial Arabinan, Is Formed via a Two-Step Epimerization of Decaprenylphosphoryl Ribose 10.1128/jb.187.23.8020-8025.2005
Polymerization of Mycobacterial Arabinogalactan and Ligation to Peptidoglycan 10.1074/jbc.m302216200
Identification of the Required Acyltransferase Step in the Biosynthesis of the Phosphatidylinositol Mannosides ofMycobacteriumSpecies 10.1074/jbc.m303639200
Definition of the First Mannosylation Step in Phosphatidylinositol Mannoside Synthesis 10.1074/jbc.m204060200
Biosynthesis of the Galactan Component of the Mycobacterial Cell Wall 10.1074/jbc.m006875200
Interaction of Human Mannose‐Binding Protein withMycobacterium avium 10.1086/520354
Hydride-induced Meisenheimer complex formation reflects activity of nitro aromatic anti-tuberculosis compounds 10.1039/D0MD00390E
Design and Synthesis of Pyrano[3,2-b]indolones Showing Antimycobacterial Activity 10.1021/acsinfecdis.0c00622
An ABC transporter Wzm-Wzt catalyzes translocation of lipid-linked galactan across the plasma membrane in mycobacteria. 10.1073/pnas.2023663118
Digby Warner
Warner Digby
ORCID: 0000-0002-4146-0930
Antimycobacterial, cytotoxic, and antioxidant activities of abietane diterpenoids isolated from plectranthus madagascariensis 10.3390/plants10010175
Easy-to-access quinolone derivatives exhibiting antibacterial and anti-parasitic activities 10.3390/molecules26041141
Mutation rate and the emergence of drug resistance in Mycobacterium tuberculosis 10.1093/jac/dkt364
Detection of Mycobacterium tuberculosis bacilli in bio-aerosols from untreated TB patients [version 1; referees: awaiting peer review] 10.12688/gatesopenres.12758.1
Bioluminescent Reporters for Rapid Mechanism of Action Assessment in Tuberculosis Drug Discovery 10.1128/AAC.01178-16
Antimicrobial activity of organometallic isonicotinyl and pyrazinyl ferrocenyl-derived complexes 10.1039/C7DT01952A
Susceptibility of Mycobacterium tuberculosis Cytochrome bd Oxidase Mutants to Compounds Targeting the Terminal Respiratory Oxidase, Cytochrome c 10.1128/AAC.01338-17
Detection of Mycobacterium tuberculosis bacilli in bio-aerosols from untreated TB patients [version 2; referees: 2 approved, 1 approved with reservations] 10.12688/gatesopenres.12758.2
Drug permeation and metabolism in Mycobacterium tuberculosis: Prioritising local exposure as essential criterion in new TB drug development 10.1002/iub.1866
CRISPRi-Seq for the Identification and Characterisation of Essential Mycobacterial Genes and Transcriptional Units 10.1101/358275
Versatility of 7-Substituted Coumarin Molecules as Antimycobacterial Agents, Neuronal Enzyme Inhibitors and Neuroprotective Agents 10.20944/preprints201709.0070.v1
Cinnamoyl-Oxaborole Amides: Synthesis and Their in Vitro Biological Activity 10.3390/molecules23082038
Death of Mycobacterium tuberculosis by l-arginine starvation 10.1073/pnas.1813587115
Quinolone-isoniazid hybrids: synthesis and preliminary in vitro cytotoxicity and anti-tuberculosis evaluation 10.1039/C8MD00480C
New Quinolone-Based Thiosemicarbazones Showing Activity Against Plasmodium falciparum and Mycobacterium tuberculosis 10.3390/molecules24091740
Detection, survival and infectious potential of Mycobacterium tuberculosis in the environment: a review of the evidence and epidemiological implications 10.1183/13993003.02302-2018
Design, synthesis, and antimycobacterial activity of novel ciprofloxacin derivatives 10.1111/cbdd.13534
Targeting DNA replication and repair for the development of novel therapeutics against tuberculosis 10.3389/fmolb.2017.00075
Erratum: Aminopyrazolo[1,5-a]pyrimidines as potential inhibitors of Mycobacterium tuberculosis: Structure activity relationships and ADME characterization (Bioorg. Med. Chem. (2015) 23 (7240-7250)) 10.1016/j.bmc.2015.12.015
Diversity and disease pathogenesis in mycobacterium tuberculosis 10.1016/j.tim.2014.10.005
2-Mercapto-Quinazolinones as Inhibitors of Type II NADH Dehydrogenase and Mycobacterium tuberculosis: Structure-Activity Relationships, Mechanism of Action and Absorption, Distribution, Metabolism, and Excretion Characterization 10.1021/acsinfecdis.7b00275
Pharmacologically active metabolites, combination screening and target identification-driven drug repositioning in antituberculosis drug discovery 10.1016/j.bmc.2014.06.012
Mono- and polynuclear ferrocenylthiosemicarbazones: Synthesis, characterisation and antimicrobial evaluation 10.1016/j.jorganchem.2016.06.032
Nucleotide metabolism and DNA replication 10.1128/microbiolspec.MGM2-0001-2013
Pyrrolo[3,4-c]pyridine-1,3(2H)-diones: A novel antimycobacterial class targeting mycobacterial respiration 10.1021/acs.jmedchem.5b01542
Targeted gene knockout and essentiality testing by homologous recombination 10.1007/978-1-4939-2450-9_8
Synthesis and biological evaluation of (E)-cinnamic acid, (E)-2-styrylthiazole and (E)-2-[2-(naphthalen-1-yl)vinyl]thiazole derivatives 10.24820/ark.5550190.p009.905
Novel Antitubercular 6-Dialkylaminopyrimidine Carboxamides from Phenotypic Whole-Cell High Throughput Screening of a SoftFocus Library: Structure-Activity Relationship and Target Identification Studies 10.1021/acs.jmedchem.7b01347
DNA replication fidelity in the mycobacterium tuberculosis complex 10.1007/978-3-319-64371-7_13
DNA Replication in Mycobacterium tuberculosis 10.1128/microbiolspec.TBTB2-0027-2016
Mycobacterium tuberculosis metabolism 10.1101/cshperspect.a021121
The complex mechanism of antimycobacterial action of 5-fluorouracil 10.1016/j.chembiol.2014.11.006
Editorial overview: Tuberculosis, malaria and schistosomiasis; understanding resistance and development of new drugs 10.1016/j.coph.2018.09.002
The Influence of HIV on the Evolution of Mycobacterium tuberculosis 10.1093/molbev/msx107
Synthesis and biological evaluation of 2-chloro-3-[(thiazol-2-yl)amino]-1,4-naphthoquinones 10.1016/j.bmcl.2019.05.001
Synthesis and biological evaluation of (E)-cinnamic acid, (E)-2-styrylthiazole and (E)-2-[2-(naphthalen-1-yl)vinyl]thiazole derivatives 10.3998/ark.5550190.p009.905
Expanding the anti-TB arsenal 10.1126/science.aaw5224
Proteomic comparison of three clinical diarrhoeagenic drug-resistant Escherichia coli isolates grown on CHROMagar™STEC media 10.1016/j.jprot.2017.09.003
Azaaurones as Potent Antimycobacterial Agents Active against MDR- and XDR-TB 10.1002/cmdc.201900289
Design, Synthesis, and Evaluation of Novel Hybrid Efflux Pump Inhibitors for Use against Mycobacterium tuberculosis 10.1021/acsinfecdis.6b00111
Genome-wide transposon mutagenesis in Mycobacterium tuberculosis and Mycobacterium smegmatis 10.1007/978-1-4939-6472-7_21
Aminopyrazolo[1,5-a]pyrimidines as potential inhibitors of Mycobacterium tuberculosis: Structure activity relationships and ADME characterization 10.1016/j.bmc.2015.10.021
Beyond the lab: Eh!woza and knowing tuberculosis 10.1136/medhum-2018-011479
Bioisosteric ferrocenyl aminoquinoline-benzimidazole hybrids: Antimicrobial evaluation and mechanistic insights 10.1016/j.ejmech.2019.06.069
Real-time investigation of tuberculosis transmission: Developing the respiratory aerosol sampling chamber (RASC) 10.1371/journal.pone.0146658
Effective visualization of tuberculosis three-drug assays: A design study 10.1145/2987491.2987501
Defining a diagnostic gene signature for tuberculosis 10.1016/S2213-2600(16)00063-1
Versatility of 7-substituted coumarin molecules as antimycobacterial agents, neuronal enzyme inhibitors and neuroprotective agents 10.3390/molecules22101644
Synthesis, characterization and antimicrobial evaluation of mono- and polynuclear ferrocenyl-derived amino and imino complexes 10.1016/j.jorganchem.2016.02.033
Synthesis and biological screening of diethyl [N-(thiazol-2-yl)carbamoyl]methylphosphonates 10.24820/ark.5550190.p010.534
The inosine monophosphate dehydrogenase, GuaB2, is a vulnerable new bactericidal drug target for tuberculosis 10.1021/acsinfecdis.6b00102
Identification of aminopyrimidine-sulfonamides as potent modulators of Wag31-mediated cell elongation in mycobacteria 10.1111/mmi.13535
In Vitro Efficacies, ADME, and Pharmacokinetic Properties of Phenoxazine Derivatives Active against Mycobacterium tuberculosis 10.1128/AAC.01010-19
Synthesis and antimycobacterial activity of disubstituted benzyltriazoles 10.1007/s00044-019-02458-7
Developing synergistic drug combinations to restore antibiotic sensitivity in drug-resistant Mycobacterium tuberculosis 10.1101/860288
Arrayed CRISPRi and Quantitative Imaging Describe the Morphotypic Landscape of Essential Mycobacterial Genes 10.1101/2020.03.20.000372
Single-step synthesis and in vitro anti-mycobacterial activity of novel nitrofurantoin analogues 10.1016/j.bioorg.2020.103587
Novel South African Rare Actinomycete Kribbella speibonae Strain SK5: A Prolific Producer of Hydroxamate Siderophores Including New Dehydroxylated Congeners 10.3390/molecules25132979
Antimicrobial evaluation of neutral and cationic iridium(III) and rhodium(III) aminoquinoline-benzimidazole hybrid complexes 10.1016/j.ejmech.2020.112694
Synthesis and in vitro antimycobacterial and antileishmanial activities of hydroquinone-triazole hybrids https://doi.org/10.1007/s00044-020-02553-0
Novel approach to estimate tuberculosis transmission in primary care clinics in sub-Saharan Africa: protocol of a prospective study 10.1136/bmjopen-2019-036214
Sensitivity optimisation of tuberculosis bioaerosol sampling 10.1371/journal.pone.0238193
Bioaerosol sampling of patients with suspected pulmonary tuberculosis: a study protocol 10.1186/s12879-020-05278-y
Arrayed CRISPRi and quantitative imaging describe the morphotypic landscape of essential mycobacterial genes 10.7554/eLife.60083
De novo cobalamin biosynthesis, transport and assimilation and cobalamin-mediated regulation of methionine biosynthesis in Mycobacterium smegmatis 10.1101/2020.11.04.369181
Addressing Latent Tuberculosis: New Advances in Mimicking the Disease, Discovering Key Targets, and Designing Hit Compounds 10.3390/ijms21228854
Synthesis and antimicrobial study of organoiridium amido-sulfadoxine complexes 10.1016/j.ica.2020.120175
Biological Profiling Enables Rapid Mechanistic Classification of Phenotypic Screening Hits and Identification of KatG Activation-Dependent Pyridine Carboxamide Prodrugs With Activity Against Mycobacterium tuberculosis 10.3389/fcimb.2020.582416
De Novo Cobalamin Biosynthesis, Transport, and Assimilation and Cobalamin-Mediated Regulation of Methionine Biosynthesis in Mycobacterium smegmatis 10.1128/JB.00620-20
Synthesis and biological evaluation of 2-aminothiazole derivatives as antimycobacterial and antiplasmodial agents doi.org/10.1016/j.bmcl.2019.126911
Capture and visualization of live Mycobacterium tuberculosis bacilli from tuberculosis patient bioaerosols 10.1371/journal.ppat.1009262
Developing Synergistic Drug Combinations To Restore Antibiotic Sensitivity in Drug-Resistant Mycobacterium tuberculosis 10.1128/AAC.02554-20
Translating genomics research into control of tuberculosis: lessons learned and future prospects 10.1186/s13059-014-0514-z
Physiology of Mycobacterium tuberculosis 10.1002/9783527611614.ch3
The impact of drug resistance onMycobacterium tuberculosisphysiology: what can we learn from rifampicin? 10.1038/emi.2014.17
Shortening Treatment for Tuberculosis — Back to Basics 10.1056/nejme1410977
Synthesis and synergistic antimycobacterial screening of chlorpromazine and its metabolites 10.1039/c3md00387f
Vitamin B12metabolism inMycobacterium tuberculosis 10.2217/fmb.13.113
A vitamin B 12 transporter in Mycobacterium tuberculosis 10.1098/rsob.120175
DNA Metabolism in Mycobacterial Pathogenesis 10.1007/82_2013_328
Detection and treatment of subclinical tuberculosis 10.1016/j.tube.2012.06.004
Tuberculosis Drug Discovery: Target Identification and Validation 10.1007/978-3-642-28175-4_3
Essential roles for imuA'- and imuB-encoded accessory factors in DnaE2-dependent mutagenesis in Mycobacterium tuberculosis 10.1073/pnas.1002614107
The role of DNA repair in M. tuberculosis pathogenesis 10.1016/j.ddmec.2010.08.002
A Riboswitch Regulates Expression of the Coenzyme B12-Independent Methionine Synthase in Mycobacterium tuberculosis: Implications for Differential Methionine Synthase Function in Strains H37Rv and CDC1551 10.1128/jb.00040-07
Tuberculosis Chemotherapy: the Influence of Bacillary Stress and Damage Response Pathways on Drug Efficacy 10.1128/cmr.00060-05
Mechanisms of stationary-phase mutagenesis in bacteria and their relevance to antibiotic resistance 10.1017/cbo9780511546242.006
Flow cytometry method for absolute counting and single-cell phenotyping of mycobacteria 10.1101/2021.05.01.442251
Antimycobacterial Activity, Synergism, and Mechanism of Action Evaluation of Novel Polycyclic Amines against Mycobacterium tuberculosis 10.1155/2021/5583342
Arylquinolinecarboxamides: Synthesis, in vitro and in silico studies against Mycobacterium tuberculosis 10.1002/jhet.4340
Isolation and characterization of new phenolic siderophores with antimicrobial properties from Pseudomonas sp. UIAU-6B 10.3762/bjoc.17.156
Kai Johnsson
Johnsson Kai
ORCID: 0000-0002-8002-1981
A synergistic strategy to develop photostable and bright dyes with long Stokes shift for super-resolution microscopy 10.21203/rs.3.rs-885436/v1
Fluorescence microscopy: strategic blinking. 10.1038/nchem.2020
Fluorogenic probes for live-cell imaging of the cytoskeleton. 10.1038/nmeth.2972
Bioluminescent sensor proteins for point-of-care therapeutic drug monitoring. 10.1038/nchembio.1554
A fluorogenic probe for SNAP-tagged plasma membrane proteins based on the solvatochromic molecule Nile Red. 10.1021/cb400819c
Sensing acetylcholine and anticholinesterase compounds. 10.1002/anie.201307754
Yeast three-hybrid screening for identifying anti-tuberculosis drug targets. 10.1002/cbic.201300472
Computational design of ligand-binding proteins with high affinity and selectivity. 10.1038/nature12443
Identification of a small molecule with activity against drug-resistant and persistent tuberculosis. 10.1073/pnas.1309171110
Tetrahydrobiopterin biosynthesis as an off-target of sulfa drugs. 10.1126/science.1232972
Selective chemical crosslinking reveals a Cep57-Cep63-Cep152 centrosomal complex. 10.1016/j.cub.2012.12.030
A near-infrared fluorophore for live-cell super-resolution microscopy of cellular proteins. 10.1038/nchem.1546
Investigating endocytic pathways to the endoplasmic reticulum and to the cytosol using SNAP-trap. 10.1111/tra.12018
Protein tag-mediated conjugation of oligonucleotides to recombinant affinity binders for proximity ligation. 10.1016/j.nbt.2012.05.005
Substrates for improved live-cell fluorescence labeling of SNAP-tag. 10.2174/1381612811319300011
A fluorescent sensor for GABA and synthetic GABA(B) receptor ligands. 10.1021/ja306320s
Liver-specific ablation of Kruppel-associated box-associated protein 1 in mice leads to male-predominant hepatosteatosis and development of liver adenoma. 10.1002/hep.25767
WhiB5, a transcriptional regulator that contributes to Mycobacterium tuberculosis virulence and reactivation. 10.1128/IAI.06328-11
A semisynthetic fluorescent sensor protein for glutamate. 10.1021/ja3002277
A caged, localizable rhodamine derivative for superresolution microscopy. 10.1021/cb2002889
Directed evolution of the suicide protein O⁶-alkylguanine-DNA alkyltransferase for increased reactivity results in an alkylated protein with exceptional stability. 10.1021/bi2016537
Triplet imaging of oxygen consumption during the contraction of a single smooth muscle cell (A7r5). 10.1007/978-1-4614-1566-4_39
Benzothiazinones are suicide inhibitors of mycobacterial decaprenylphosphoryl-β-D-ribofuranose 2'-oxidase DprE1. 10.1021/ja211042r
Exploiting ligand-protein conjugates to monitor ligand-receptor interactions. 10.1371/journal.pone.0037598
Switchable fluorophores for protein labeling in living cells. 10.1016/j.cbpa.2011.10.015
Semisynthesis of fluorescent metabolite sensors on cell surfaces. 10.1021/ja206915m
Development of SNAP-tag fluorogenic probes for wash-free fluorescence imaging. 10.1002/cbic.201100173
A yeast-based screen reveals that sulfasalazine inhibits tetrahydrobiopterin biosynthesis. 10.1038/nchembio.557
Measuring in vivo protein half-life. 10.1016/j.chembiol.2011.03.014
Real-time measurements of protein dynamics using fluorescence activation-coupled protein labeling method. 10.1021/ja200225m
Labelling cell structures and tracking cell lineage in zebrafish using SNAP-tag. 10.1002/dvdy.22574
Reflections on chemical biology. 10.1021/cb100405m
NCCR Chemical Biology: Interdisciplinary Research Excellence, Outreach, Education, and New Tools for Switzerland. 10.2533/chimia.2011.832
Visualizing biochemical activities in living cells through chemistry. 10.2533/chimia.2011.868
Chemical biology approaches to membrane homeostasis and function. 10.2533/chimia.2011.849
How to obtain labeled proteins and what to do with them. 10.1016/j.copbio.2010.09.011
Benzothiazinones: prodrugs that covalently modify the decaprenylphosphoryl-β-D-ribose 2'-epimerase DprE1 of Mycobacterium tuberculosis. 10.1021/ja106357w
Fura-2FF-based calcium indicator for protein labeling. 10.1039/c000158a
Localizable and highly sensitive calcium indicator based on a BODIPY fluorophore. 10.1021/ac100741t
Targeted photoswitchable probe for nanoscopy of biological structures. 10.1002/cbic.201000189
Phosphopantetheinyl transferase-catalyzed formation of bioactive hydrogels for tissue engineering. 10.1021/ja9098164
Photoactivatable and photoconvertible fluorescent probes for protein labeling. 10.1021/cb1000229
Triplet imaging of oxygen consumption during the contraction of a single smooth muscle cell (A7r5). 10.1016/j.bpj.2009.10.006
Using peptide loop insertion mutagenesis for the evolution of proteins. 10.1007/978-1-60761-652-8_16
Selective cross-linking of interacting proteins using self-labeling tags. 10.1021/ja907818q
Semisynthetic fluorescent sensor proteins based on self-labeling protein tags. 10.1021/ja900149e
Indo-1 derivatives for local calcium sensing. 10.1021/cb800258g
Visualizing biochemical activities in living cells. 10.1038/nchembio0209-63
Regulation of glutamate metabolism by protein kinases in mycobacteria. 10.1111/j.1365-2958.2008.06489.x
Subunit-specific surface mobility of differentially labeled AMPA receptor subunits. 10.1016/j.ejcb.2008.02.014
A designed protein for the specific and covalent heteroconjugation of biomolecules. 10.1021/bc800268j
Investigative reporters. 10.1021/cb800134q
A split-protein sensor for studying protein-protein interaction in mycobacteria. 10.1016/j.mimet.2008.02.008
An engineered protein tag for multiprotein labeling in living cells. 10.1016/j.chembiol.2008.01.007
Caged substrates for protein labeling and immobilization. 10.1002/cbic.200700472
A covalent chemical genotype-phenotype linkage for in vitro protein evolution. 10.1002/cbic.200700459
Chemical probes shed light on protein function. 10.1016/j.sbi.2007.07.005
Inducing and sensing protein--protein interactions in living cells by selective cross-linking. 10.1002/anie.200700408
Directed evolution of O6-alkylguanine-DNA alkyltransferase for applications in protein labeling. 10.1093/protein/gzl014
Post-translational covalent labeling reveals heterogeneous mobility of individual G protein-coupled receptors in living cells. 10.1002/cbic.200500477
Chimeric streptavidins with reduced valencies. 10.1038/nmeth0406-247
Covalent labeling of cell-surface proteins for in-vivo FRET studies. 10.1016/j.febslet.2006.02.007
FRET imaging reveals that functional neurokinin-1 receptors are monomeric and reside in membrane microdomains of live cells. 10.1073/pnas.0507686103
Protein function microarrays based on self-immobilizing and self-labeling fusion proteins. 10.1002/cbic.200500278
The laboratory in a droplet. 10.1016/j.chembiol.2005.11.006
Multicolor imaging of cell surface proteins. 10.1021/ja0533850
Adding value to fusion proteins through covalent labelling. 10.1016/j.copbio.2005.06.001
Engineering substrate specificity of O6-alkylguanine-DNA alkyltransferase for specific protein labeling in living cells. 10.1002/cbic.200400431
Fast directed evolution of non-immunoglobulin proteins by somatic hypermutation in immune cells. 10.1002/cbic.200500011
Protein chemistry on the surface of living cells. 10.1002/cbic.200400290
Protein-functionalized polymer brushes. 10.1021/bm050016n
Specific labeling of cell surface proteins with chemically diverse compounds. 10.1021/ja048396s
Labeling of fusion proteins with synthetic fluorophores in live cells. 10.1073/pnas.0401923101
Synthesis and characterization of bifunctional probes for the specific labeling of fusion proteins. 10.1016/j.bmcl.2004.03.078
Labeling of fusion proteins of O6-alkylguanine-DNA alkyltransferase with small molecules in vivo and in vitro. 10.1016/j.ymeth.2003.10.007
Induced protein dimerization in vivo through covalent labeling. 10.1021/ja037883p
DNA repair protein O6-methylguanine-DNA methyltransferase in testis and testicular tumors as determined by a novel nonradioactive assay. 10.1016/S0003-2697(03)00432-9
A fusion of disciplines: chemical approaches to exploit fusion proteins for functional genomics. 10.1002/cbic.200200603
Covalent and selective immobilization of fusion proteins. 10.1021/ja034145s
Directed evolution of O6-alkylguanine-DNA alkyltransferase for efficient labeling of fusion proteins with small molecules in vivo. 10.1016/S1074-5521(03)00068-1
A general method for the covalent labeling of fusion proteins with small molecules in vivo. 10.1038/nbt765
Examining reactivity and specificity of cytochrome c peroxidase by using combinatorial mutagenesis. 10.1002/1439-7633(20021104)3:11<1097::AID-CBIC1097>3.0.CO;2-4
Towards the generation of artificial O6-alkylguanine-DNA alkyltransferases: in vitro selection of antibodies with reactive cysteine residues. 10.1002/1439-7633(20020603)3:6<573::AID-CBIC573>3.0.CO;2-F
Inter- and intramolecular domain interactions of the catalase-peroxidase KatG from M. tuberculosis. 10.1016/S0014-5793(01)03179-9
Changing the substrate specificity of cytochrome c peroxidase using directed evolution. 10.1006/bbrc.2001.5366
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