The state of the art of PROTAC technologies for drug discovery

被引：73

作者：

Wang, Chao ^{[1
]}

Zheng, Cangxin ^{[2
]}

Wang, Han ^{[2
]}

Zhang, Liangren ^{[2
,3
]}

Liu, Zhenming ^{[2
,3
]}

Xu, Ping ^{[2
,3
]}

机构：

[1] Peking Univ, Natl Pharmaceut Teaching Lab Ctr, Sch Pharmaceut Sci, Beijing, Peoples R China

[2] Peking Univ, Sch Pharmaceut Sci, Dept Med Chem, Beijing, Peoples R China

[3] Peking Univ, State Key Lab Nat & Biomimet Drugs, Beijing, Peoples R China

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2022年 / 235卷

基金：

中国国家自然科学基金;

关键词：

PROTAC; Degradation; CLIPTAC; PHOTAC; SPNpro; floate-PROTAC; antibody-PROTAC conjugate; AbTAC; RIBOTAC; TF-PROTAC; CHAMP; bioPROTAC; Molecular glue; PROTEIN-DEGRADATION; DEGRADERS; MOLECULES; COMPLEX;

D O I：

10.1016/j.ejmech.2022.114290

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Protein degradation technology has progressed dramatically since 2001 when proteolysis targeting chimera (PROTAC) was first reported. Various of distinctive degradation technologies based on PROTAC have been developed for the degradation of kinases, nuclear receptors, epigenetic proteins, misfolded proteins, and also RNAs, etc. These technologies greatly broaden the spectrum of targets and the scope of clinical applications for the treatment of cancer, neurodegenerative diseases and virus diseases, etc. More than 15 targeted degraders have been in the clinic to date. Here in this review, we summarized the constituents and examples of different degradation strategies, as well as their advantages and limitations.(c) 2022 Elsevier Masson SAS. All rights reserved.

引用

页数：8

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