[HTML][HTML] New tuberculosis drug targets, their inhibitors, and potential therapeutic impact

GS Shetye, SG Franzblau, S Cho - Translational Research, 2020 - Elsevier
The current tuberculosis (TB) predicament poses numerous challenges and therefore every
incremental scientific work and all positive socio-political engagements, are steps taken in …

Beyond the approved: target sites and inhibitors of bacterial RNA polymerase from bacteria and fungi

SH Kirsch, FPJ Haeckl, R Müller - Natural Product Reports, 2022 - pubs.rsc.org
Covering: 2016 to 2022 RNA polymerase (RNAP) is the central enzyme in bacterial gene
expression representing an attractive and validated target for antibiotics. Two well-known …

Profiling of rpoB Mutations and MICs for Rifampin and Rifabutin in Mycobacterium tuberculosis

FB Jamieson, JL Guthrie, A Neemuchwala… - Journal of clinical …, 2014 - Am Soc Microbiol
Resistance to rifampin (RIF) and rifabutin (RFB) in Mycobacterium tuberculosis is associated
with mutations within an 81-bp region of the rpoB gene (RIF resistance-determining region …

Structural basis for rifamycin resistance of bacterial RNA polymerase by the three most clinically important RpoB mutations found in Mycobacterium tuberculosis

V Molodtsov, NT Scharf, MA Stefan… - Molecular …, 2017 - Wiley Online Library
Summary Since 1967, Rifampin (RMP, a Rifamycin) has been used as a first line antibiotic
treatment for tuberculosis (TB), and it remains the cornerstone of current short‐term TB …

Structural diversity and biological relevance of benzenoid and atypical ansamycins and their congeners

N Skrzypczak, P Przybylski - Natural Product Reports, 2022 - pubs.rsc.org
Covering: 2011 to 2021 The structural division of ansamycins, including those of atypical
cores and different lengths of the ansa chains, is presented. Recently discovered benzenoid …

Allosteric mechanism of transcription inhibition by NusG-dependent pausing of RNA polymerase

RK Vishwakarma, MZ Qayyum… - Proceedings of the …, 2023 - National Acad Sciences
NusG is a transcription elongation factor that stimulates transcription pausing in Gram+
bacteria including B. subtilis by sequence-specific interaction with a conserved pause …

The enzymes of the rifamycin antibiotic resistome

MD Surette, P Spanogiannopoulos… - Accounts of chemical …, 2021 - ACS Publications
Conspectus Rifamycin antibiotics include the WHO essential medicines rifampin, rifabutin,
and rifapentine. These are semisynthetic derivatives of the natural product rifamycins …

Systematic review of allelic exchange experiments aimed at identifying mutations that confer drug resistance in Mycobacterium tuberculosis

H Nebenzahl-Guimaraes, KR Jacobson… - Journal of …, 2014 - academic.oup.com
Background Improving our understanding of the relationship between the genotype and the
drug resistance phenotype of Mycobacterium tuberculosis will aid the development of more …

Rifabutin: where do we stand in 2016?

Y Crabol, E Catherinot, N Veziris… - Journal of …, 2016 - academic.oup.com
Rifabutin is a spiro-piperidyl-rifamycin structurally closely related to rifampicin that shares
many of its properties. We attempted to address the reasons why this drug, which was …

Mode of action of kanglemycin A, an ansamycin natural product that is active against rifampicin-resistant Mycobacterium tuberculosis

H Mosaei, V Molodtsov, B Kepplinger, J Harbottle… - Molecular cell, 2018 - cell.com
Antibiotic-resistant bacterial pathogens pose an urgent healthcare threat, prompting a
demand for new medicines. We report the mode of action of the natural ansamycin antibiotic …