Small-molecule procaspase activators identified using fluorescence polarization

Chembiochem. 2013 Aug 19;14(12):1419-22. doi: 10.1002/cbic.201300315. Epub 2013 Jul 8.

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.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Biological Assay
  • Caspase 1 / metabolism*
  • Drug Discovery
  • Enzyme Activation / drug effects
  • Enzyme Activators / chemistry*
  • Enzyme Activators / pharmacology*
  • Fluorescence Polarization
  • Molecular Structure
  • Small Molecule Libraries / chemistry*
  • Small Molecule Libraries / pharmacology*
  • Trans-Activators / chemistry*

Substances

  • Enzyme Activators
  • Small Molecule Libraries
  • Trans-Activators
  • Caspase 1