title: 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.
authors.affiliation: Department of Molecular and Experimental Medicine and Chemical Physiology, The Scripps Research Institute, La Jolla, California 92037, USA.
authors.forename: Chris J
authors.initials: CJ
authors.lastname: Vickers
authors.forename: Gonzalo E
authors.initials: GE
authors.lastname: González-Páez
authors.forename: Jeffrey C
authors.initials: JC
authors.lastname: Umotoy
authors.forename: Charmagne
authors.initials: C
authors.lastname: Cayanan-Garrett
authors.forename: Steven J
authors.initials: SJ
authors.lastname: Brown
authors.forename: Dennis W
authors.initials: DW
authors.lastname: Wolan
mesh_terms: D001681:Biological Assay; D020170:Caspase 1 / Q000378:metabolism*; D055808:Drug Discovery; D004789:Enzyme Activation / Q000187:drug effects; D020536:Enzyme Activators / Q000737:chemistry* / Q000494:pharmacology*; D005454:Fluorescence Polarization; D015394:Molecular Structure; D054852:Small Molecule Libraries / Q000737:chemistry* / Q000494:pharmacology*; D015534:Trans-Activators / Q000737:chemistry*
chemical_list: D020536:Enzyme Activators; D054852:Small Molecule Libraries; D015534:Trans-Activators; D020170:Caspase 1
keywords: activators; apoptosis; caspases; high-throughput screening; zymogens