A Highly Potent and Selective PKCα Inhibitor Generated via Combinatorial Modification of a Peptide Scaffold
- 1 March 2004
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of the American Chemical Society
- Vol. 126 (11) , 3394-3395
- https://doi.org/10.1021/ja037300b
Abstract
A potent and highly selective inhibitor of protein kinase C α has been generated via the combinatorial modification of a consensus sequence peptide. The inhibitor displays a Ki of 800 pM versus variable peptide substrate and good selectivity versus other members of the PKC family, including PKCβ (385-fold), PKCγ (580-fold), PKCδ (2730-fold), PKCε (600-fold), PKCη (1310-fold), PKCθ (1210-fold), PKCι (940-fold), and PKCζ (640-fold). The parallel synthesis strategy employed is easily automated and straightforward to implement.Keywords
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