Therapeutic developments for tuberculosis and nontuberculous mycobacterial lung disease

V Dartois, T Dick - Nature Reviews Drug Discovery, 2024 - nature.com
Tuberculosis (TB) drug discovery and development has undergone nothing short of a
revolution over the past 20 years. Successful public–private partnerships and sustained …

Cryptosporidium lysyl-tRNA synthetase inhibitors define the interplay between solubility and permeability required to achieve efficacy

N Caldwell, C Peet, P Miller, BL Colon… - Science Translational …, 2024 - science.org
Cryptosporidiosis is a diarrheal disease caused by infection with Cryptosporidium spp.
parasites and is a leading cause of death in malnourished children worldwide. The only …

Cladosporin, A Highly Potent Antimalaria Drug?

A Hou, B Li, Z Deng, M Xu, JS Dickschat - ChemBioChem, 2023 - Wiley Online Library
Cladosporin, a unique natural product from the fungus Cladosporium cladosporioides,
exhibits nanomolar inhibitory activity against Plasmodium falciparum by targeting its …

Side-by-side profiling of oxazolidinones to estimate the therapeutic window against mycobacterial infections

DA Negatu, WW Aragaw, J Cangialosi… - Antimicrobial Agents …, 2023 - Am Soc Microbiol
New oxazolidinones are in clinical development for the treatment of tuberculosis and
nontuberculous mycobacterial (NTM) infections, as a replacement for linezolid and tedizolid …

Identification and Optimization of Novel Inhibitors of the Polyketide Synthase 13 Thioesterase Domain with Antitubercular Activity

SR Green, C Wilson, TC Eadsforth… - Journal of Medicinal …, 2023 - ACS Publications
There is an urgent need for new tuberculosis (TB) treatments, with novel modes of action, to
reduce the incidence/mortality of TB and to combat resistance to current treatments. Through …

Mycobacterial biotin synthases require an auxiliary protein to convert dethiobiotin into biotin

D Qu, P Ge, L Botella, SW Park, HN Lee… - Nature …, 2024 - nature.com
Lipid biosynthesis in the pathogen Mycobacterium tuberculosis depends on biotin for
posttranslational modification of key enzymes. However, the mycobacterial biotin synthetic …

Peptidyl tRNA hydrolase is required for robust prolyl-tRNA turnover in Mycobacterium tuberculosis

FG Tomasi, JTP Schweber, S Kimura, J Zhu… - Mbio, 2023 - Am Soc Microbiol
Enzymes involved in rescuing stalled ribosomes and recycling translation machinery are
ubiquitous in bacteria and required for growth. Peptidyl tRNA drop-off is a type of abortive …

Structure-guided conversion from an anaplastic lymphoma kinase inhibitor into Plasmodium lysyl-tRNA synthetase selective inhibitors

J Zhou, M Xia, Z Huang, H Qiao, G Yang… - Communications …, 2024 - nature.com
Aminoacyl-tRNA synthetases (aaRSs) play a central role in the translation of genetic code,
serving as attractive drug targets. Within this family, the lysyl-tRNA synthetase (LysRS) …

Design and synthesis of Thieno [3, 2-b] pyridinone derivatives exhibiting potent activities against Mycobacterium tuberculosis in vivo by targeting Enoyl-ACP reductase

L Liang, Z Liu, J Chen, Q Zha, Y Zhou, J Li, Y Hu… - European Journal of …, 2024 - Elsevier
In this study, a series of novel thieno [3, 2-b] pyridinone derivatives were designed and
synthesized using a scaffold hopping strategy. Six compounds showed potent anti …

Indole Propionic Acid Disturbs the Normal Function of Tryptophanyl-tRNA Synthetase in Mycobacterium tuberculosis

X Han, Y Gao, B Zhou, HMA Hameed… - ACS Infectious …, 2024 - ACS Publications
Tuberculosis (TB) is the leading infectious disease caused by Mycobacterium tuberculosis
and the second-most contagious killer after COVID-19. The emergence of drug-resistant TB …