Advances in the development of new tuberculosis drugs and treatment regimens

A Zumla, P Nahid, ST Cole - Nature reviews Drug discovery, 2013 - nature.com
Despite the introduction 40 years ago of the inexpensive and effective four-drug (isoniazid,
rifampicin, pyrazinamide and ethambutol) treatment regimen, tuberculosis (TB) continues to …

The mycobacterial cell envelope—lipids

M Jackson - Cold Spring Harbor perspectives in …, 2014 - perspectivesinmedicine.cshlp.org
Mycobacterium tuberculosis (Mtb) lipids are indelibly imprinted in just about every key
aspect of tuberculosis (TB) basic and translational research. Although the interest in these …

Recent Advances of DprE1 Inhibitors against Mycobacterium tuberculosis: Computational Analysis of Physicochemical and ADMET Properties

PSM Amado, C Woodley, MLS Cristiano, PM O'Neill - ACS omega, 2022 - ACS Publications
Decaprenylphosphoryl-β-d-ribose 2′-epimerase (DprE1) is a critical flavoenzyme in
Mycobacterium tuberculosis, catalyzing a vital step in the production of lipoarabinomannan …

Mycobacterial cell wall: a source of successful targets for old and new drugs

C Vilchèze - Applied Sciences, 2020 - mdpi.com
Eighty years after the introduction of the first antituberculosis (TB) drug, the treatment of drug-
susceptible TB remains very cumbersome, requiring the use of four drugs (isoniazid …

Overview of the development of DprE1 inhibitors for combating the menace of tuberculosis

RV Chikhale, MA Barmade, PR Murumkar… - Journal of medicinal …, 2018 - ACS Publications
Decaprenylphosphoryl-β-d-ribose 2′-epimerase (DprE1), a vital enzyme for cell wall
synthesis, plays a crucial role in the formation of lipoarabinomannan and arabinogalactan. It …

Targeting bacterial central metabolism for drug development

P Murima, JD McKinney, K Pethe - Chemistry & biology, 2014 - cell.com
Current antibiotics, derived mainly from natural sources, inhibit a narrow spectrum of cellular
processes, namely DNA replication, protein synthesis, and cell wall biosynthesis. With the …

Structural Basis for Benzothiazinone-Mediated Killing of Mycobacterium tuberculosis

J Neres, F Pojer, E Molteni, LR Chiarelli… - Science translational …, 2012 - science.org
The benzothiazinone BTZ043 is a tuberculosis drug candidate with nanomolar whole-cell
activity. BTZ043 targets the DprE1 catalytic component of the essential enzyme …

The cell envelope glycoconjugates of Mycobacterium tuberculosis

SK Angala, JM Belardinelli, E Huc-Claustre… - Critical reviews in …, 2014 - Taylor & Francis
Tuberculosis (TB) remains the second most common cause of death due to a single
infectious agent. The cell envelope of Mycobacterium tuberculosis (Mtb), the causative agent …

Recent advances in the development of DprE1 inhibitors using AI/CADD approaches

K Chen, R Xu, X Hu, D Li, T Hou, Y Kang - Drug Discovery Today, 2024 - Elsevier
Tuberculosis (TB) is a global lethal disease caused by Mycobacterium tuberculosis (Mtb).
The flavoenzyme decaprenylphosphoryl-β-d-ribose 2′-oxidase (DprE1) plays a crucial part …

Tuberculosis drug discovery in the post‐post‐genomic era

B Lechartier, J Rybniker, A Zumla… - EMBO molecular …, 2014 - embopress.org
The expectation that genomics would result in new therapeutic interventions for infectious
diseases remains unfulfilled. In the post‐genomic era, the decade immediately following the …