Title
Diarylquinolines target subunit c of mycobacterial ATP synthase Diarylquinolines target subunit c of mycobacterial ATP synthase
Author
Faculty/Department
Faculty of Pharmaceutical, Biomedical and Veterinary Sciences. Pharmacy
Publication type
article
Publication
New York :Nature Publishing Group ,
Subject
Biology
Human medicine
Source (journal)
Nature chemical biology. - New York
Volume/pages
3(2007) :6 , p. 323-324
ISSN
1552-4450
Carrier
E
Target language
English (eng)
Full text (Publishers DOI)
Affiliation
University of Antwerp
Abstract
The diarylquinoline R207910 (TMC207) is a promising candidate in clinical development for the treatment of tuberculosis. Though R207910-resistant mycobacteria bear mutations in ATP synthase, the compound's precise target is not known. Here we establish by genetic, biochemical and binding assays that the oligomeric subunit c (AtpE) of ATP synthase is the target of R207910. Thus targeting energy metabolism is a new, promising approach for antibacterial drug discovery.
Handle