Search Results - "Mikusova, Katarina"
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DprE1--from the discovery to the promising tuberculosis drug target
Published in Current pharmaceutical design (01-01-2014)“…Several groups working in the field of the development of new antituberculosis drugs have recently reported active compounds targeting mycobacterial enzyme…”
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Galactosyl Transferases in Mycobacterial Cell Wall Synthesis
Published in Journal of Bacteriology (01-02-2008)“…Article Usage Stats Services JB Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley…”
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Fragment-Based Design of Mycobacterium tuberculosis InhA Inhibitors
Published in Journal of medicinal chemistry (14-05-2020)“…Tuberculosis (TB) remains a leading cause of mortality among infectious diseases worldwide. InhA has been the focus of numerous drug discovery efforts as this…”
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Benzothiazinones Are Suicide Inhibitors of Mycobacterial Decaprenylphosphoryl-β-d-ribofuranose 2′-Oxidase DprE1
Published in Journal of the American Chemical Society (18-01-2012)“…Benzothiazinones (BTZs) are antituberculosis drug candidates with nanomolar bactericidal activity against tubercle bacilli. Here we demonstrate that BTZs are…”
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Development of 3,5-Dinitrobenzylsulfanyl-1,3,4-oxadiazoles and Thiadiazoles as Selective Antitubercular Agents Active Against Replicating and Nonreplicating Mycobacterium tuberculosis
Published in Journal of medicinal chemistry (24-03-2016)“…Herein, we report the discovery and structure–activity relationships of 5-substituted-2-[(3,5-dinitrobenzyl)sulfanyl]-1,3,4-oxadiazoles and 1,3,4-thiadiazoles…”
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DprE1 Is a Vulnerable Tuberculosis Drug Target Due to Its Cell Wall Localization
Published in ACS chemical biology (17-07-2015)“…The flavo-enzyme DprE1 catalyzes a key epimerization step in the decaprenyl-phosphoryl d-arabinose (DPA) pathway, which is essential for mycobacterial cell…”
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Drugging the Folate Pathway in Mycobacterium tuberculosis: The Role of Multi-targeting Agents
Published in Cell chemical biology (20-06-2019)“…The folate biosynthetic pathway offers many druggable targets that have yet to be exploited in tuberculosis therapy. Herein, we have identified a series of…”
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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
Published in Journal of medicinal chemistry (12-09-2019)“…We report herein the discovery of 3,5-dinitrophenyl 1,2,4-triazoles with excellent and selective antimycobacterial activities against Mycobacterium…”
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Structural and Activity Relationships of 6-Sulfonyl-8-Nitrobenzothiazinones as Antitubercular Agents
Published in Journal of medicinal chemistry (14-10-2021)“…The benzothiazinone (BTZ) scaffold compound PBTZ169 kills by inhibiting the essential flavoenzyme DprE1, consequently blocking the synthesis of the cell wall…”
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Both Nitro Groups Are Essential for High Antitubercular Activity of 3,5-Dinitrobenzylsulfanyl Tetrazoles and 1,3,4-Oxadiazoles through the Deazaflavin-Dependent Nitroreductase Activation Pathway
Published in Journal of medicinal chemistry (11-01-2024)“…3,5-Dinitrobenzylsulfanyl tetrazoles and 1,3,4-oxadiazoles, previously identified as having high in vitro activities against both replicating and…”
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Decaprenylphosphoryl Arabinofuranose, the Donor of the d-Arabinofuranosyl Residues of Mycobacterial Arabinan, Is Formed via a Two-Step Epimerization of Decaprenylphosphoryl Ribose
Published in Journal of Bacteriology (01-12-2005)“…Article Usage Stats Services JB Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley…”
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Compartmentalization of galactan biosynthesis in mycobacteria
Published in The Journal of biological chemistry (01-03-2024)“…Galactan polymer is a prominent component of the mycobacterial cell wall core. Its biogenesis starts at the cytoplasmic side of the plasma membrane by a…”
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Design, synthesis and evaluation of covalent inhibitors of DprE1 as antitubercular agents
Published in European journal of medicinal chemistry (15-12-2020)“…Decaprenylphosphoryl-β-d-ribose 2′-oxidoreductase (DprE1) is a promising drug target for the development of novel anti-tubercular agents, and inhibitors of…”
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Structural basis for selective recognition of acyl chains by the membrane-associated acyltransferase PatA
Published in Nature communications (11-03-2016)“…The biosynthesis of phospholipids and glycolipids are critical pathways for virtually all cell membranes. PatA is an essential membrane associated…”
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Identification of a small molecule with activity against drug-resistant and persistent tuberculosis
Published in Proceedings of the National Academy of Sciences - PNAS (02-07-2013)“…A cell-based phenotypic screen for inhibitors of biofilm formation in mycobacteria identified the small molecule TCA1, which has bactericidal activity against…”
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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
Published in Beilstein journal of organic chemistry (27-07-2020)“…A series of ten novel ᴅ-fructofuranosyl and ᴅ-tagatofuranosyl sulfones bearing a 1- -phosphono moiety and three different substituents at C-2 has been…”
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Copper-related toxicity in replicating and dormant Mycobacterium tuberculosis caused by 1-hydroxy-5-R-pyridine-2(1H)-thiones
Published in Metallomics (18-07-2018)“…With the emerging primary resistance of Mycobacterium tuberculosis to current drugs and wide distribution of latent tuberculosis infection, the need for new…”
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Design, Syntheses, and Anti-TB Activity of 1,3-Benzothiazinone Azide and Click Chemistry Products Inspired by BTZ043
Published in ACS medicinal chemistry letters (10-03-2016)“…Electron deficient nitroaromatic compounds such as BTZ043 and its closest congener, PBTZ169, and related agents are a promising new class of anti-TB compounds…”
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The 8-Pyrrole-Benzothiazinones Are Noncovalent Inhibitors of DprE1 from Mycobacterium tuberculosis
Published in Antimicrobial agents and chemotherapy (01-08-2015)“…8-Nitro-benzothiazinones (BTZs), such as BTZ043 and PBTZ169, inhibit decaprenylphosphoryl-β-d-ribose 2'-oxidase (DprE1) and display nanomolar bactericidal…”
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GtrA Protein Rv3789 Is Required for Arabinosylation of Arabinogalactan in Mycobacterium tuberculosis
Published in Journal of bacteriology (01-12-2015)“…Mycobacterium tuberculosis possesses a thick and highly hydrophobic cell wall principally composed of a mycolyl-arabinogalactan-peptidoglycan complex, which is…”
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