KINATEST-ID: a pipeline to develop phosphorylation-dependent terbium sensitizing kinase assays.

ABSTRACT: Nonreceptor protein tyrosine kinases (NRTKs) are essential for cellular homeostasis and thus are a major focus of current drug discovery efforts. Peptide substrates that can enhance lanthanide ion luminescence upon tyrosine phosphorylation enable rapid, sensitive screening of kinase activity, however design of suitable substrates that can distinguish between tyrosine kinase families is a huge challenge. Despite their different substrate preferences, many NRTKs are structurally similar even between families. Furthermore, the development of lanthanide-based kinase assays is hampered by incomplete understanding of how to integrate sequence selectivity with metal ion binding, necessitating laborious iterative substrate optimization. We used curated proteomic data from endogenous kinase substra

SUBMITTER: Lipchik AM 

PROVIDER: S-EPMC4342272 | biostudies-literature | 2015 Feb

REPOSITORIES: biostudies-literature