Gong Zhang; Juan Zhang; Yuting Gao; Yangfeng Li; Yizhou Li
Expert Opin. Drug Discov., 2022, 17(1), 55-69
https://doi.org/10.1080/17460441.2021.1969359

Abstract

Undruggable targets refer to clinically meaningful therapeutic targets that are ‘difficult to drug’ or ‘yet to be drugged’ via traditional approaches. Featuring characteristics of lacking defined ligand-binding pockets, non-catalytic protein–protein interaction functional modes and less-investigated 3D structures, these undruggable targets have been targeted with novel therapeutic entities developed with the progress of unconventional drug discovery approaches, such as targeted degradation molecules and display technologies.