Publication
Title
Selectivity of TMC207 towards mycobacterial ATP synthase compared with that towards the eukaryotic homologue
Author
Abstract
The diarylquinoline TMC207 kills Mycobacterium tuberculosis by specifically inhibiting ATP synthase. We show here that human mitochondrial ATP synthase (50% inhibitory concentration [IC50] of >200 µM) displayed more than 20,000-fold lower sensitivity for TMC207 compared to that of mycobacterial ATP synthase (IC50 of 10 nM). Also, oxygen consumption in mouse liver and bovine heart mitochondria showed very low sensitivity for TMC207. These results suggest that TMC207 may not elicit ATP synthesis-related toxicity in mammalian cells. ATP synthase, although highly conserved between prokaryotes and eukaryotes, may still qualify as an attractive antibiotic target.
Language
English
Source (journal)
Antimicrobial agents and chemotherapy. - Washington, D.C.
Publication
Washington, D.C. : 2009
ISSN
0066-4804
Volume/pages
53:3(2009), p. 1290-1292
ISI
000263552100070
Full text (Publisher's DOI)
UAntwerpen
Faculty/Department
Research group
Publication type
Subject
Affiliation
Publications with a UAntwerp address
External links
Web of Science
Record
Identification
Creation 13.03.2009
Last edited 29.09.2017
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