Literature DB >> 31200858

Small-molecule PROTAC degraders of the Bromodomain and Extra Terminal (BET) proteins - A review.

Chao-Yie Yang1, Chong Qin1, Longchuan Bai1, Shaomeng Wang2.   

Abstract

The PROteolysis TArgeting Chimeric (PROTAC) concept has provided an opportunity for the discovery and development of a completely new type of therapy involving induction of protein degradation. The BET proteins, comprised of BRD2, BRD3, BRD4 and the testis-specific BRDT protein, are epigenetic readers and master transcription coactivators. Extremely potent and efficacious small-molecule PROTAC degraders of the BET proteins, based on available, potent and selective BET inhibitors, have been reported. BET degraders differ from BET inhibitors in their cellular potency, phenotypic effects, pharmacokinetic properties and toxicity profiles. Herein, we provide a review of BET degraders and the differential outcome observed in the cellular and animal models for BET degraders in comparison to BET inhibitors.
Copyright © 2019. Published by Elsevier Ltd.

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Year:  2019        PMID： 31200858     DOI： 10.1016/j.ddtec.2019.04.001

Source DB:  PubMed          Journal:  Drug Discov Today Technol        ISSN： 1740-6749


  32 in total

Review 1.  BET Epigenetic Reader Proteins in Cardiovascular Transcriptional Programs.

Authors:  Patricia Cristine Borck; Lian-Wang Guo; Jorge Plutzky
Journal:  Circ Res       Date:  2020-04-23       Impact factor: 17.367

Review 2.  PROTACs: great opportunities for academia and industry.

Authors:  Xiuyun Sun; Hongying Gao; Yiqing Yang; Ming He; Yue Wu; Yugang Song; Yan Tong; Yu Rao
Journal:  Signal Transduct Target Ther       Date:  2019-12-24

3.  Discovery of IAP-recruiting BCL-XL PROTACs as potent degraders across multiple cancer cell lines.

Authors:  Xuan Zhang; Yonghan He; Peiyi Zhang; Vivekananda Budamagunta; Dongwen Lv; Dinesh Thummuri; Yang Yang; Jing Pei; Yaxia Yuan; Daohong Zhou; Guangrong Zheng
Journal:  Eur J Med Chem       Date:  2020-05-04       Impact factor: 6.514

Review 4.  Validation of the epigenetic reader bromodomain-containing protein 4 (BRD4) as a therapeutic target for treatment of airway remodeling.

Authors:  Allan R Brasier; Jia Zhou
Journal:  Drug Discov Today       Date:  2019-11-13       Impact factor: 7.851

5.  The novel BET degrader, QCA570, is highly active against the growth of human NSCLC cells and synergizes with osimertinib in suppressing osimertinib-resistant EGFR-mutant NSCLC cells.

Authors:  Chaoyuan Liu; Luxi Qian; Karin A Vallega; Guangzhi Ma; Dan Zong; Luxiao Chen; Shaomeng Wang; Suresh R Ramalingam; Zhaohui Qin; Shi-Yong Sun
Journal:  Am J Cancer Res       Date:  2022-02-15       Impact factor: 6.166

6.  Targeting Bromodomain and Extraterminal Proteins for Drug Discovery: From Current Progress to Technological Development.

Authors:  Pan Tang; Jifa Zhang; Jie Liu; Cheng-Ming Chiang; Liang Ouyang
Journal:  J Med Chem       Date:  2021-02-22       Impact factor: 7.446

Review 7.  Proteolysis-Targeting Chimeras as Therapeutics and Tools for Biological Discovery.

Authors:  George M Burslem; Craig M Crews
Journal:  Cell       Date:  2020-01-16       Impact factor: 41.582

8.  Getting a handle on chemical probes of chomatin readers.

Authors:  Jarod M Waybright; Lindsey I James
Journal:  Future Med Chem       Date:  2020-01-10       Impact factor: 3.808

Review 9.  BET bromodomains as novel epigenetic targets for brain health and disease.

Authors:  Mandakini B Singh; Gregory C Sartor
Journal:  Neuropharmacology       Date:  2020-09-15       Impact factor: 5.250

10.  Targeting c-Myc to Overcome Acquired Resistance of EGFR Mutant NSCLC Cells to the Third-Generation EGFR Tyrosine Kinase Inhibitor, Osimertinib.

Authors:  Lei Zhu; Zhen Chen; Hongjing Zang; Songqing Fan; Jiajia Gu; Guojing Zhang; Kevin D-Y Sun; Qiming Wang; Yong He; Taofeek K Owonikoko; Suresh S Ramalingam; Shi-Yong Sun
Journal:  Cancer Res       Date:  2021-07-21       Impact factor: 12.701
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