Article

Charting functional E3 ligase hotspots and resistance mechanisms to small-molecule degraders

2022-04-14

Abstract excerpt

Targeted protein degradation is a new pharmacologic paradigm established by drugs that recruit target proteins to E3 ubiquitin ligases via a ternary ligase-degrader-target complex. Based on the structure of the degrader and the neosubstrate, different E3 ligase interfaces are critically involved in this process, thus forming defined “functional hotspots”. Understanding disruptive mutations in functional hotspots i...

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Literature Corpus work: 113f4202-7fc7-5cf7-96f1-8d64606571cc
DOI: 10.1101/2022.04.14.488316

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