reviewMolecular BiomedicineDec 20, 2022DIAMOND OA

An overview of PROTACs: a promising drug discovery paradigm

Sichuan University · State Key Laboratory of Biotherapy · +1 more institution

PubMed
Indexed incrossrefdoajpubmed

Abstract

Proteolysis targeting chimeras (PROTACs) technology has emerged as a novel therapeutic paradigm in recent years. PROTACs are heterobifunctional molecules that degrade target proteins by hijacking the ubiquitin-proteasome system. Currently, about 20-25% of all protein targets are being studied, and most works focus on their enzymatic functions. Unlike small molecules, PROTACs inhibit the whole biological function of the target protein by binding to the target protein and inducing subsequent proteasomal degradation. PROTACs compensate for limitations that transcription factors, nuclear proteins, and other scaffolding proteins are difficult to handle with traditional small-molecule inhibitors. Currently, PROTACs…

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