ATP synthase selectivity of TMC207/R207910

Thursday, April 02th, 2009 by hinrich

Article by Haagsma et al.

I have written previously about the >20.000 fold lower sensitivity of TMC207/R207910 on the human mitochondrial ATP synthase in comparison to the ATP synthase of Mycobacterium smegmatis.

The article has now been published in the March 2009 edition of Antimicrobial Agents and Chemotherapy. It nicely shows the clear difference in activity of TMC207/R207910 on the ATP synthase from human mitochondrial ATP synthase (derived from the human ovarian cancer cell line OVCAR3) in contrast to the ATP synthase of the Mycobacterium strain Mycobacterium smegmatis mc2155.

I like the last sentence of the paper that highlights how the disqualification of a bacterial protein as a potential drug target should not be done: "More generally, our results illustrate that in drug discovery, a protein should not be disregarded a priori as a potential drug target because of the existence of a human homologue".

You can read the abstract of the paper here.

Posted in Tuberculosis


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