Diarylquinolines against ATP synthase

Sunday, June 24th, 2012 by hinrich

Structure of TMC207/R207910

A few new articles have appeared over the past months related to TMC207 (Bedaquiline) as well as the class of compounds (diarylquinolines) that TMC207 belongs to.

Segala et al. looked at the interactions of TMC207 with the mycobacterial ATP synthase. Using various in vitro TMC207-resistant mutants from M. tuberculosis and diverse atypical mycobacteria, they gathered experimental data on the molecular interactions between TMC207 and the proton-binding site of C-ring of the ATP synthase.

My colleagues published end of May information on how the class of the diarylquinolines may be used to inhibit the ATP synthase of other Gram-positive bacteria. This is important work given the need of new antibiotics and since we had shown that the ATP synthase is a possible antibacterial target. The recent publications shows that it may be possible to utilize this class of compounds without drifting away from the ATP synthase as the target.

Posted in Tuberculosis


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