Thursday, December 19, 2013
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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),
dehydrogenase kinase 1
kinases but not their wild-type counterparts. Next steps include developing
staurosporine analogs and analog-sensitive kinases for use in animal studies.
Published online Dec. 19, 2013
Patented; licensing status
Lopez, M.S. et al. J.
Am. Chem. Soc.; published online Oct. 30, 2013;
Contact: Kevan M. Shokat, University of California, San
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