Targeted Degradation of Proteins by PROTACs.
Curr Protoc Chem Biol
; 2(2): 71-87, 2010 Jun 01.
Article
en En
| MEDLINE
| ID: mdl-23836551
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. 271-87. © 2010 by John Wiley & Sons, Inc.
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01-internacional
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MEDLINE
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En
Revista:
Curr Protoc Chem Biol
Año:
2010
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Article