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

共 50 条

[31] Chimera induced protein degradation: PROTACs and beyond
Yin, Lina
Hu, Qingzhong
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2020, 206
[32] Precise Modulation of Protein Degradation by Smart PROTACs
Cheng, Junfei
Dong, Guoqiang
Wang, Wei
Sheng, Chunquan
CHEMBIOCHEM, 2025, 26 (01)
[33] PROTACS: Induced protein degradation as a therapeutic strategy
Crews, Craig
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2017, 253
[34] Targeted selective degradation of Bruton's tyrosine kinase by PROTACs
Liu, Shaodong
Da, Yang
Wang, Feng
Yan, Renjie
Shu, Yongzhi
Lin, Pei
Lin, Jun
MEDICINAL CHEMISTRY RESEARCH, 2020, 29 (04) : 802 - 808
[35] Targeted selective degradation of Bruton’s tyrosine kinase by PROTACs
Shaodong Liu
Yang Da
Feng Wang
Renjie Yan
Yongzhi Shu
Pei Lin
Jun Lin
Medicinal Chemistry Research, 2020, 29 : 802 - 808
[36] Reversible Covalent PROTACs: Novel and Efficient Targeted Degradation Strategy
Yuan, Minghua
Chu, Yanan
Duan, Yongtao
FRONTIERS IN CHEMISTRY, 2021, 9
[37] Efficient Targeted Degradation via Reversible and Irreversible Covalent PROTACs
Gabizon, Ronen
Shraga, Amit
Gehrtz, Paul
Livnah, Ella
Shorer, Yamit
Gurwicz, Neta
Avram, Liat
Unger, Tamar
Aharoni, Hila
Albeck, Shira
Brandis, Alexander
Shulman, Ziv
Katz, Ben-Zion
Herishanu, Yair
London, Nir
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 2020, 142 (27) : 11734 - 11742
[38] TF-PROTACs Enable Targeted Degradation of Transcription Factors
Liu, Jing
Chen, He
Kaniskan, H. Umit
Xie, Ling
Chen, Xian
Jin, Jian
Wei, Wenyi
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 2021, 143 (23) : 8902 - 8910
[39] Targeted and selective degradation of estrogen receptor (ER) alpha by PROTACs
Flanagan, J. J.
Rossi, A. K.
Anderoli, M.
Willard, R. R.
Gordon, D.
Harling, J.
Churcher, I.
Smith, I.
Zinn, N.
Bantscheff, M.
Crews, C. M.
Crew, A.
Coleman, K. G.
Winkler, J. D.
Qian, Y.
CANCER RESEARCH, 2017, 77
[40] Targeted Protein Destruction Advances in PROTACs and Other Degraders
Niewijk G.
Genetic Engineering and Biotechnology News, 2020, 40 (12): : 42 - 44+46

← 1 2 3 4 5 →