Diarylquinolines target subunit c of mycobacterial ATP synthase.

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

Research output: Contribution to JournalArticleAcademicpeer-review

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. © 2007 Nature Publishing Group.
Original languageEnglish
Pages (from-to)323-324
JournalNature Chemical Biology
Volume3
DOIs
Publication statusPublished - 2007

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