Peptide-based ligand screening and functional analysis of protein kinase C

Abstract

Protein kinase C (PKC) plays an important role in cell signaling pathways and is implicated in disorders ranging from cancer to Alzheimer's disease. Highly potent PKC ligands as therapeutic drugs have not been developed to date and useful methodologies for controlling PKC activation in defined areas are necessary to analyze precise PKC functions in cells. Studies focused on the development of PKC ligand screening systems and methods for regulation of PKC activation have been performed in our laboratory. In this review, our ligand screening methods involving synthetic peptides and solvatochromic fluorescent dye-labeled small compounds are summarized and the technique of spatio-temporal manipulation of PKC activation by caging strategies is introduced.

Keywords: PKC; caged compound; ligand screening; solvatochromic fluorescent dye.