Engineered Substrate-Specific Delta PKC Antagonists to Enhance Cardiac Therapeutics.

ABSTRACT: Most protein kinases phosphorylate multiple substrates, each of which induces different and sometimes opposing functions. Determining the role of phosphorylation of each substrate following a specific stimulus is challenging but is essential to elucidate the role of that substrate in the signaling event. Here we describe a rational approach to identify inhibitors of delta protein kinase C (δPKC), each inhibiting the phosphorylation of only one of δPKC's substrates. δPKC regulates many signaling events and we hypothesized that a docking inhibitor of a given substrate to δPKC should selectively abrogate the phosphorylation of only that substrate, without affecting the phosphorylation of the other δPKC substrates. Here we report the development of selective inhibitors of three δPKC substrates

SUBMITTER: Qvit N 

PROVIDER: S-EPMC5308906 | biostudies-literature | 2016 Dec

REPOSITORIES: biostudies-literature