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 …
disease. In 2020 alone, TB was responsible for 1.5 million deaths worldwide, comparable to …
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 …
Mycobacterium tuberculosis, catalyzing a vital step in the production of lipoarabinomannan …
Identification of hydantoin based Decaprenylphosphoryl-β-d-Ribose Oxidase (DprE1) inhibitors as antimycobacterial agents using computational tools
Tuberculosis (TB) is one of the emerging infectious diseases in the world. DprE1 (
Decaprenylphosphoryl-β-d-ribose 2′-epimerase), an enzyme accountable for …
Decaprenylphosphoryl-β-d-ribose 2′-epimerase), an enzyme accountable for …
[HTML][HTML] The pipeline of new molecules and regimens against drug-resistant tuberculosis
TA Black, UK Buchwald - Journal of Clinical Tuberculosis and Other …, 2021 - Elsevier
The clinical development and regulatory approval of bedaquiline, delamanid and
pretomanid over the last decade brought about significant progress in the management of …
pretomanid over the last decade brought about significant progress in the management of …
Cryo-EM structure and resistance landscape of M. tuberculosis MmpL3: An emergent therapeutic target
Tuberculosis (TB) is the leading cause of death from a single infectious agent and in 2019
an estimated 10 million people worldwide contracted the disease. Although treatments for …
an estimated 10 million people worldwide contracted the disease. Although treatments for …
Synthetic molecules as DprE1 inhibitors: A patent review
Introduction In recent years, the advent of multidrug-resistant tuberculosis (MDR-TB), the
extensively-resistant TB (XDR-TB), and the total drug-resistant-TB (TDR-TB) have led the …
extensively-resistant TB (XDR-TB), and the total drug-resistant-TB (TDR-TB) have led the …
Development of macozinone for TB treatment: an update
V Makarov, K Mikušová - Applied Sciences, 2020 - mdpi.com
Macozinone, a piperazine-benzothiazinone PBTZ169, is currently undergoing Phase 1/2
clinical studies for the treatment of tuberculosis (TB). In this review we summarize the key …
clinical studies for the treatment of tuberculosis (TB). In this review we summarize the key …
DprE1 inhibitors: enduring aspirations for future antituberculosis drug discovery
DprE1 is a crucial enzyme involved in the cell wall synthesis of Mycobacterium tuberculosis
and a promising target for antituberculosis drug development. However, its unique structural …
and a promising target for antituberculosis drug development. However, its unique structural …
Low-cost anti-mycobacterial drug discovery using engineered E. coli
N Bongaerts, Z Edoo, AA Abukar, X Song… - Nature …, 2022 - nature.com
Whole-cell screening for Mycobacterium tuberculosis (Mtb) inhibitors is complicated by the
pathogen's slow growth and biocontainment requirements. Here we present a synthetic …
pathogen's slow growth and biocontainment requirements. Here we present a synthetic …
Medicinal polypharmacology—a scientific glossary of terminology and concepts
Medicinal polypharmacology is one answer to the complex reality of multifactorial human
diseases that are often unresponsive to single-targeted treatment. It is an admittance that …
diseases that are often unresponsive to single-targeted treatment. It is an admittance that …