reviewSignal Transduction and Targeted TherapyApr 4, 2022GOLD OA

Targeted protein degradation: mechanisms, strategies and application

Sichuan University · State Key Laboratory of Biotherapy

PubMed
Indexed incrossrefdoajpubmed

Abstract

Traditional drug discovery mainly focuses on direct regulation of protein activity. The development and application of protein activity modulators, particularly inhibitors, has been the mainstream in drug development. In recent years, PROteolysis TArgeting Chimeras (PROTAC) technology has emerged as one of the most promising approaches to remove specific disease-associated proteins by exploiting cells' own destruction machinery. In addition to PROTAC, many different targeted protein degradation (TPD) strategies including, but not limited to, molecular glue, Lysosome-Targeting Chimaera (LYTAC), and Antibody-based PROTAC (AbTAC), are emerging. These technologies have not only greatly expanded the scope of TPD,…

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