Tuberculosis drug discovery: challenges and new horizons

GFS Fernandes, AM Thompson… - Journal of Medicinal …, 2022 - ACS Publications
Over the past 2000 years, tuberculosis (TB) has claimed more lives than any other infectious
disease. In 2020 alone, TB was responsible for 1.5 million deaths worldwide, comparable to …

Hit generation in TB drug discovery: from genome to granuloma

T Yuan, NS Sampson - Chemical reviews, 2018 - ACS Publications
Current tuberculosis (TB) drug development efforts are not sufficient to end the global TB
epidemic. Recent efforts have focused on the development of whole-cell screening assays …

High-throughput metabolomic analysis predicts mode of action of uncharacterized antimicrobial compounds

M Zampieri, B Szappanos, MV Buchieri… - Science translational …, 2018 - science.org
Rapidly spreading antibiotic resistance and the low discovery rate of new antimicrobial
compounds demand more effective strategies for early drug discovery. One bottleneck in the …

Pipeline of anti‐Mycobacterium abscessus small molecules: Repurposable drugs and promising novel chemical entities

A Egorova, M Jackson, V Gavrilyuk… - Medicinal research …, 2021 - Wiley Online Library
The Mycobacterium abscessus complex is a group of emerging pathogens that are difficult
to treat. There are no effective drugs for successful M. abscessus pulmonary infection …

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 …

Recent advancements and developments in search of anti-tuberculosis agents: a quinquennial update and future directions

TM Dhameliya, KA Bhakhar, ND Gajjar, KA Patel… - Journal of Molecular …, 2022 - Elsevier
Tuberculosis (TB) has been considered as the highly chronic, contagious and infectious
disorder caused by Mycobacterium tuberculosis (Mtb). Every year more than 10 million …

Screening of TB actives for activity against nontuberculous mycobacteria delivers high hit rates

JL Low, ML Wu, DB Aziz, B Laleu, T Dick - Frontiers in microbiology, 2017 - frontiersin.org
The prevalence of lung disease due to infections with nontuberculous mycobacteria (NTM)
has been increasing and surpassed tuberculosis (TB) in some countries. Treatment …

Unpacking the Pathogen Box—an open source tool for fighting neglected tropical disease

CGL Veale - ChemMedChem, 2019 - Wiley Online Library
Abstract The Pathogen Box is a 400‐strong collection of drug‐like compounds, selected for
their potential against several of the world's most important neglected tropical diseases …

Inhibiting mycobacterial tryptophan synthase by targeting the inter-subunit interface

KA Abrahams, JAG Cox, K Fütterer, J Rullas… - Scientific Reports, 2017 - nature.com
Drug discovery efforts against the pathogen Mycobacterium tuberculosis (Mtb) have been
advanced through phenotypic screens of extensive compound libraries. Such a screen …

Piperidine-4-carboxamides target DNA gyrase in Mycobacterium abscessus

DA Negatu, A Beuchel, A Madani… - Antimicrobial agents …, 2021 - journals.asm.org
New, more-effective drugs for the treatment of lung disease caused by nontuberculous
mycobacteria (NTM) are needed. Among NTM opportunistic pathogens, Mycobacterium …