Drug resistance mechanisms and drug susceptibility testing for tuberculosis

P Miotto, Y Zhang, DM Cirillo, WC Yam - Respirology, 2018 - Wiley Online Library
Tuberculosis (TB) caused by Mycobacterium tuberculosis (MTB) is the deadliest infectious
disease and the associated global threat has worsened with the emergence of drug …

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 …

Drug-resistance in Mycobacterium tuberculosis: where we stand

A Mabhula, V Singh - Medchemcomm, 2019 - pubs.rsc.org
Tuberculosis (TB), an infectious disease caused by the bacterium Mycobacterium
tuberculosis (Mtb), has burdened vulnerable populations in modern day societies for …

Pharmacological and molecular mechanisms behind the sterilizing activity of pyrazinamide

P Gopal, G Grüber, V Dartois, T Dick - Trends in pharmacological sciences, 2019 - cell.com
Inclusion of pyrazinamide (PZA) in the tuberculosis (TB) drug regimen during the 1970s
enabled a reduction in treatment duration from 12 to 6 months. PZA has this remarkable …

The molecular basis of pyrazinamide activity on Mycobacterium tuberculosis PanD

Q Sun, X Li, LM Perez, W Shi, Y Zhang… - Nature …, 2020 - nature.com
Pyrazinamide has been a mainstay in the multidrug regimens used to treat tuberculosis. It is
active against the persistent, non-replicating mycobacteria responsible for the protracted …

The bewildering antitubercular action of pyrazinamide

EA Lamont, NA Dillon, AD Baughn - Microbiology and Molecular …, 2020 - Am Soc Microbiol
Pyrazinamide (PZA) is a cornerstone antimicrobial drug used exclusively for the treatment of
tuberculosis (TB). Due to its ability to shorten drug therapy by 3 months and reduce disease …

Pyrazinoic acid inhibits mycobacterial coenzyme A biosynthesis by binding to aspartate decarboxylase PanD

P Gopal, W Nartey, P Ragunathan… - ACS infectious …, 2017 - ACS Publications
Previously, we showed that a major in vitro and in vivo mechanism of resistance to
pyrazinoic acid (POA), the bioactive component of the critical tuberculosis (TB) prodrug …

Novel pyrazine based anti-tubercular agents: Design, synthesis, biological evaluation and in silico studies

NW Hassan, MN Saudi, YS Abdel-Ghany, A Ismail… - Bioorganic …, 2020 - Elsevier
TB continues to be a leading health threat despite the availability of powerful anti-TB drugs.
We report herein the design and synthesis of various hybrid molecules comprising pyrazine …

The Expanding Diversity of Mycobacterium tuberculosis Drug Targets

S Wellington, DT Hung - ACS infectious diseases, 2018 - ACS Publications
After decades of relative inactivity, a large increase in efforts to discover antitubercular
therapeutics has brought insights into the biology of Mycobacterium tuberculosis (Mtb) and …

Transition bias influences the evolution of antibiotic resistance in Mycobacterium tuberculosis

JL Payne, F Menardo, A Trauner, S Borrell… - PLoS …, 2019 - journals.plos.org
Transition bias, an overabundance of transitions relative to transversions, has been widely
reported among studies of the rates and spectra of spontaneous mutations. However …