A coiled-coil enabled split-luciferase three-hybrid system: applied toward profiling inhibitors of protein kinases.

ABSTRACT: The 518 protein kinases encoded in the human genome are exquisitely regulated and their aberrant function(s) are often associated with human disease. Thus, in order to advance therapeutics and to probe signal transduction cascades, there is considerable interest in the development of inhibitors that can selectively target protein kinases. However, identifying specific compounds against such a large array of protein kinases is difficult to routinely achieve utilizing traditional activity assays, where purified protein kinases are necessary. Toward a simple, rapid, and practical method for identifying specific inhibitors, we describe the development and application of a split-protein methodology utilizing a coiled-coil-assisted three-hybrid system. In this approach, a protein kinase of inter

SUBMITTER: Jester BW 

PROVIDER: S-EPMC2966823 | biostudies-literature | 2010 Aug

REPOSITORIES: biostudies-literature