Innovation in neglected tropical disease drug discovery and development

HB Weng, HX Chen, MW Wang - Infectious diseases of poverty, 2018 - mednexus.org
Background: Neglected tropical diseases (NTDs) are closely related to poverty and affect
over a billion people in developing countries. The unmet treatment needs cause high …

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 …

Dihydrofolate reductase inhibitors for use as antimicrobial agents

J He, W Qiao, Q An, T Yang, Y Luo - European journal of medicinal …, 2020 - Elsevier
Drug-resistant bacteria pose an increasingly serious threat to mankind all over the world.
However, the currently available clinical treatments do not meet the urgent demand …

Therapeutic potential of the Mycobacterium tuberculosis mycolic acid transporter, MmpL3

W Li, A Obregón-Henao, JB Wallach… - Antimicrobial agents …, 2016 - Am Soc Microbiol
In recent years, whole-cell-based screens for novel small molecule inhibitors active against
Mycobacterium tuberculosis in culture followed by the whole-genome sequencing of …

A genetic strategy to identify targets for the development of drugs that prevent bacterial persistence

JH Kim, KM O'Brien, R Sharma… - Proceedings of the …, 2013 - National Acad Sciences
Antibacterial drug development suffers from a paucity of targets whose inhibition kills
replicating and nonreplicating bacteria. The latter include phenotypically dormant cells …

Mycobacterium tuberculosis Folate Metabolism and the Mechanistic Basis for para-Aminosalicylic Acid Susceptibility and Resistance

Y Minato, JM Thiede, SL Kordus… - Antimicrobial agents …, 2015 - Am Soc Microbiol
ABSTRACT para-Aminosalicylic acid (PAS) entered clinical use in 1946 as the second
exclusive drug for the treatment of tuberculosis (TB). While PAS was initially a first-line TB …

Enabling Photo‐Crosslinking and Photo‐Sensitizing Properties for Synthetic Fluorescent Protein Chromophores

H Feng, Q Zhao, B Zhang, H Hu, M Liu… - Angewandte …, 2023 - Wiley Online Library
Synthetic fluorescent protein chromophores have been reported for their singlet state
fluorescence properties and applications in bioimaging, but rarely for the triplet state …

The complex mechanism of antimycobacterial action of 5-fluorouracil

V Singh, M Brecik, R Mukherjee, JC Evans… - Chemistry & biology, 2015 - cell.com
A combination of chemical genetic and biochemical assays was applied to investigate the
mechanism of action of the anticancer drug 5-fluorouracil (5-FU), against Mycobacterium …

Why are membrane targets discovered by phenotypic screens and genome sequencing in Mycobacterium tuberculosis?

RC Goldman - Tuberculosis, 2013 - Elsevier
High through put screening (HTS) was extensively used in attempts to discover new TB
drugs from libraries of pure small molecule compounds many of which complied with the …

Discovery of Selective Toxoplasma gondii Dihydrofolate Reductase Inhibitors for the Treatment of Toxoplasmosis

AT Hopper, A Brockman, A Wise, J Gould… - Journal of medicinal …, 2019 - ACS Publications
A safer treatment for toxoplasmosis would be achieved by improving the selectivity and
potency of dihydrofolate reductase (DHFR) inhibitors, such as pyrimethamine (1), for …