Targeted Degradation of Proteins by PROTACs
Published Online: 1 APR 2010
Copyright © 2010 by John Wiley and Sons, Inc.
Lab Protocol Title
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.
- Published Online: 1 APR 2010
- Published Print: APR 2010
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.
- small molecule