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Staurosporine analogs (staralogs) with improved selectivity toward analog-sensitive kinases

Staralogs could expand approaches to study kinase function using analog-sensitive kinase variants. Kinase variants with genetically engineered sensitivity to ATP analogs have been used in functional studies, but in some cases the ATP analogs also inhibit wild-type and unrelated kinases. In cultured cells, staralogs inhibited analog-sensitive variants of EPH receptor A4 (EPHA4), pyruvate dehydrogenase kinase 1
(PDK1) and ret proto-oncogene (RET) kinases but not their wild-type counterparts. Next steps include developing staurosporine analogs and analog-sensitive kinases for use in animal studies.

SciBX 6(48); doi:10.1038/scibx.2013.1410
Published online Dec. 19, 2013

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Lopez, M.S. et al. J. Am. Chem. Soc.; published online Oct. 30, 2013;
Contact: Kevan M. Shokat, University of California, San Francisco, Calif.