Small-molecule procaspase activators identified using fluorescence polarization

Abstract

Wake up, protein! Small molecules that directly activate proteins are rare and their discovery opens new avenues for the development of drugs and chemical tools to probe the functions and mechanisms of protein targets. To address the one-sided dichotomy between enzyme inhibition and activation, we describe a series of procaspase activators as chemical tools in the study of caspase biology.

Keywords: activators; apoptosis; caspases; high-throughput screening; zymogens.