Diarylquinolines target subunit c of mycobacterial ATP synthase.

Article Details

Citation

Koul A, Dendouga N, Vergauwen K, Molenberghs B, Vranckx L, Willebrords R, Ristic Z, Lill H, Dorange I, Guillemont J, Bald D, Andries K

Diarylquinolines target subunit c of mycobacterial ATP synthase.

Nat Chem Biol. 2007 Jun;3(6):323-4. Epub 2007 May 13.

PubMed ID
17496888 [ View in PubMed
]
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.

DrugBank Data that Cites this Article

Drug Targets
DrugTargetKindOrganismPharmacological ActionActions
BedaquilineATP synthase subunit cProteinMycobacterium tuberculosis
Yes
Inhibitor
Details