Unit

Targeted Degradation of Proteins by PROTACs

  1. Eun Ryoung Jang,
  2. Wooin Lee,
  3. Kyung Bo Kim

Published Online: 1 APR 2010

DOI: 10.1002/9780470559277.ch090242

Current Protocols in Chemical Biology

Current Protocols in Chemical Biology

How to Cite

Jang, E. R., Lee, W. and Kim, K. B. 2010. Targeted Degradation of Proteins by PROTACs. Current Protocols in Chemical Biology. 2:71–87.

Author Information

  1. University of Kentucky, Lexington, Kentucky

Publication History

  1. Published Online: 1 APR 2010
  2. Published Print: APR 2010

Abstract

In recent years, small interference RNAs (siRNAs) have greatly enhanced our understanding of protein functions by allowing knockdown of targeted proteins at the mRNA level. Similarly, in an effort to achieve degradation of targeted proteins at the post-translational level, chimeric small molecules called “PROTACs” (PROteolysis TArgeting Chimeric molecules) have been developed. The PROTAC approach utilizes chimeric small molecules which recruit targeted proteins to the ubiquitin-proteasome pathway, a major intracellular protein degradation system. Unlike conventional small molecules that bind to protein and inhibit its function, the PROTAC approach induces destruction of target protein via the ubiquitin-proteasome system. This article presents a typical strategy for PROTAC design and preparation and biological characterization. Curr. Protoc. Chem Biol. 2:71-87. © 2010 by John Wiley & Sons, Inc.

Keywords:

  • PROTAC;
  • ubiquitin;
  • proteasome;
  • small molecule