Targeted Protein Degradation by Chimeric Small Molecules, PROTACs and SNIPERs

被引：35

作者：

Naito, Mikihiko ^{[1
]}

Ohoka, Nobumichi ^{[1
]}

Shibata, Norihito ^{[1
]}

Tsukumo, Yoshinori ^{[1
]}

机构：

[1] Natl Inst Hlth Sci, Lab Mol Target & Gene Therapy Prod, Kawasaki, Kanagawa, Japan

来源：

FRONTIERS IN CHEMISTRY | 2019年 / 7卷

基金：

日本学术振兴会;

关键词：

PROTAC; SNIPER; E3; modulator; ubiquitin; proteasome; protein degradation; SELECTIVE DEGRADATION; INDUCE DEGRADATION; KNOCKDOWN; UBIQUITINATION; INHIBITORS; DESIGN; LIGAND; TIR1;

D O I：

10.3389/fchem.2019.00849

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Technologies that induce targeted protein degradation by small molecules have been developed recently. Chimeric small molecules such as Proteolysis Targeting Chimeras (PROTACs) and Specific and Non-genetic IAP-dependent Protein Erasers (SNIPERs), and E3 modulators such as thalidomides, hijack the cellular machinery for ubiquitylation, and the ubiquitylated proteins are subjected to proteasomal degradation. This has motivated drug development in industry and academia because "undruggable targets" can now be degraded by targeted protein degradation.

引用

页数：5

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