Tuberculosis drug discovery: A decade of hit assessment for defined targets

S Oh, L Trifonov, VD Yadav, CE Barry III… - Frontiers in Cellular …, 2021 - frontiersin.org
More than two decades have elapsed since the publication of the first genome sequence of
Mycobacterium tuberculosis (Mtb) which, shortly thereafter, enabled methods to determine …

[HTML][HTML] An insight into the discovery, clinical studies, compositions, and patents of macozinone: A drug targeting the DprE1 enzyme of Mycobacterium tuberculosis

M Imran, SA Khan, SMB Asdaq, M Almehmadi… - Journal of Infection and …, 2022 - Elsevier
Abstract Decaprenyl-phosphoryl-ribose 2′-epimerase (DprE1) inhibitors are an innovative
and futuristic orally active group of antituberculosis agents. A few DprE1 inhibitors are in the …

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

KA Abrahams, C Chung, S Ghidelli-Disse… - Nature …, 2016 - nature.com
Phenotypic screens for bactericidal compounds are starting to yield promising hits against
tuberculosis. In this regard, whole-genome sequencing of spontaneous resistant mutants …

In silico study to identify new antituberculosis molecules from natural sources by hierarchical virtual screening and molecular dynamics simulations

VS Pinto, JSC Araújo, RC Silva, GV da Costa, JN Cruz… - Pharmaceuticals, 2019 - mdpi.com
Tuberculosis (TB) is an infection caused by Mycobacterium tuberculosis, responsible for 1.5
million documented deaths in 2016. The increase in reported cases of M. tuberculosis …

Fragment-based drug discovery against mycobacteria: the success and challenges

NS Togre, AM Vargas, G Bhargavi… - International Journal of …, 2022 - mdpi.com
The emergence of drug-resistant mycobacteria, including Mycobacterium tuberculosis (Mtb)
and non-tuberculous mycobacteria (NTM), poses an increasing global threat that urgently …

New quinoline-thiolactone conjugates as potential antitubercular and antibacterial agents

S Faazil, MS Malik, SA Ahmed, QMS Jamal… - Journal of Molecular …, 2023 - Elsevier
Tuberculosis and bacterial infections are major challenges because of elevated infection
rates and drug resistance. New chemical agents need to be developed to address them …

Lineage-Specific Proteomic Signatures in the Mycobacterium tuberculosis Complex Reveal Differential Abundance of Proteins Involved in Virulence, DNA Repair …

SA Yimer, S Kalayou, H Homberset… - Frontiers in …, 2020 - frontiersin.org
Despite the discovery of the tubercle bacillus more than 130 years ago, its physiology and
the mechanisms of virulence are still not fully understood. A comprehensive analysis of the …

Mycobacterium tuberculosis KasA as a drug target: Structure-based inhibitor design

RS Rudraraju, SS Daher, R Gallardo-Macias… - Frontiers in Cellular …, 2022 - frontiersin.org
Recent studies have reported the β-ketoacyl-acyl carrier protein KasA as a druggable target
for Mycobacterium tuberculosis. This review summarizes the current status of major classes …

Identification of potent indolizine derivatives against Mycobacterial tuberculosis: In vitro anti-TB properties, in silico target validation, molecular docking and dynamics …

KN Venugopala, S Chandrashekharappa… - International journal of …, 2024 - Elsevier
In the current study, two sets of compounds:(E)-1-(2-(4-substitutedphenyl)-2-oxoethyl)-4-
((hydroxyimino) methyl) pyridinium derivatives (3a-3e); and (E)-3-(substitutedbenzoyl)-7 …

Synergistic lethality of a binary inhibitor of Mycobacterium tuberculosis KasA

P Kumar, GC Capodagli, D Awasthi, R Shrestha… - MBio, 2018 - Am Soc Microbiol
ABSTRACT We report GSK3011724A (DG167) as a binary inhibitor of β-ketoacyl-ACP
synthase (KasA) in Mycobacterium tuberculosis. Genetic and biochemical studies …