Diarylquinolines target subunit c of mycobacterial ATP synthaseDiarylquinolines target subunit c of mycobacterial ATP synthase
Faculty of Pharmaceutical, Biomedical and Veterinary Sciences. Pharmacy
Laboratory for Microbiology, Parasitology and Hygiene (LMPH)
2007New York :Nature Publishing Group, 2007
Nature chemical biology. - New York
3(2007):6, p. 323-324
University of Antwerp
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.