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. 2021 Oct 21;8(20):2170136. doi: 10.1002/advs.202170136

Destruction of DNA‐Binding Proteins by Programmable Oligonucleotide PROTAC (O'PROTAC): Effective Targeting of LEF1 and ERG (Adv. Sci. 20/2021)

Jingwei Shao, Yuqian Yan, Donglin Ding, Dejie Wang, Yundong He, Yunqian Pan, Wei Yan, Anupreet Kharbanda, Hong‐yu Li, Haojie Huang
PMCID: PMC8529440

Abstract

Proteolysis‐Targeting Chimera Technology

In article number 2102555, Hong‐yu Li, Haojie Huang, and co‐workers demonstrate a new approach, oligonucleotide‐based proteolysis‐targeting chimera (O'PROTAC), to degrade “undruggable” transcriptional factors (TFs) via the ubiquitin‐proteasome system. O'PROTAC is designed by employing the TF‐uniquely‐recognized DNA sequence as natural “ligand”. The programmability of O'PROTAC makes it an attractive arsenal to target TFs for treatment of diseases including cancer.

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