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Drug platforms

Highly potent inhibitors of sirtuin 1 (SIRT1), SIRT2 and SIRT3

Thieno[3,2-d]pyrimidine-6-carboxamide-based sirtuin inhibitors could be used as research compounds to probe the functions of SIRT1, SIRT2 and SIRT3 in human diseases. The therapeutic effects of modulating sirtuin activity have been unclear in part because weak, unselective compounds have been used to investigate sirtuin function. A lead compound from a new series of inhibitors was developed that specifically inhibited SIRT1, SIRT2 and SIRT3 with IC50 values below 5 nM. Next steps include using the compounds to explore the biology of sirtuin regulation and develop new SIRT1 modulators.

SciBX 6(16); doi:10.1038/scibx.2013.400
Published online April 25, 2013

Patent applications filed; unavailable for licensing

Disch, J.S. et al. J. Med. Chem.; published online April 9, 2013;
doi:10.1021/jm400204k
Contact: Ghotas Evindar, GlaxoSmithKline plc, Waltham, Mass.
e-mail:
ghotas.x.evindar@gsk.com

Contact: Jeremy S. Disch, same affiliation as above
e-mail:
jdisch92@gmail.com