Literature DB >> 31922153

Protein degradation through covalent inhibitor-based PROTACs.

Gang Xue1, Jiahui Chen, Lihong Liu, Danli Zhou, Yingying Zuo, Tiancheng Fu, Zhengying Pan.   

Abstract

Tremendous advancements in proteolysis targeting chimera (PROTAC) technology have been made in recent years. However, whether a covalent inhibitor-based PROTAC can be developed remains controversial. Here, we successfully developed chimeric degraders based on covalent inhibitors to degrade BTK and BLK kinases, demonstrating that covalent inhibitor-based PROTACs are viable and useful tools.

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Year:  2020        PMID: 31922153     DOI: 10.1039/c9cc08238g

Source DB:  PubMed          Journal:  Chem Commun (Camb)        ISSN: 1359-7345            Impact factor:   6.222


  19 in total

Review 1.  Recent Developments in PROTAC-Mediated Protein Degradation: From Bench to Clinic.

Authors:  Zhenyi Hu; Craig M Crews
Journal:  Chembiochem       Date:  2021-09-23       Impact factor: 3.461

Review 2.  PROTACs: great opportunities for academia and industry (an update from 2020 to 2021).

Authors:  Ming He; Chaoguo Cao; Zhihao Ni; Yongbo Liu; Peilu Song; Shuang Hao; Yuna He; Xiuyun Sun; Yu Rao
Journal:  Signal Transduct Target Ther       Date:  2022-06-09

Review 3.  Major Advances in Emerging Degrader Technologies.

Authors:  Hang Luo; Li Wu; Yujian He; Chong Qin; Xinjing Tang
Journal:  Front Cell Dev Biol       Date:  2022-06-22

4.  Covalent PROTACs: the best of both worlds?

Authors:  Neil P Grimster
Journal:  RSC Med Chem       Date:  2021-07-15

Review 5.  Targeted protein degradation: A promise for undruggable proteins.

Authors:  Kusal T G Samarasinghe; Craig M Crews
Journal:  Cell Chem Biol       Date:  2021-05-17       Impact factor: 9.039

Review 6.  PROTACs: An Emerging Therapeutic Modality in Precision Medicine.

Authors:  Dhanusha A Nalawansha; Craig M Crews
Journal:  Cell Chem Biol       Date:  2020-08-13       Impact factor: 9.039

7.  Efficient Targeted Degradation via Reversible and Irreversible Covalent PROTACs.

Authors:  Ronen Gabizon; Amit Shraga; Paul Gehrtz; Ella Livnah; Yamit Shorer; Neta Gurwicz; Liat Avram; Tamar Unger; Hila Aharoni; Shira Albeck; Alexander Brandis; Ziv Shulman; Ben-Zion Katz; Yair Herishanu; Nir London
Journal:  J Am Chem Soc       Date:  2020-05-19       Impact factor: 15.419

Review 8.  Targeting Protein Kinases Degradation by PROTACs.

Authors:  Fei Yu; Ming Cai; Liang Shao; Jihong Zhang
Journal:  Front Chem       Date:  2021-06-30       Impact factor: 5.221

9.  Reversible Covalent PROTACs: Novel and Efficient Targeted Degradation Strategy.

Authors:  Minghua Yuan; Yanan Chu; Yongtao Duan
Journal:  Front Chem       Date:  2021-07-05       Impact factor: 5.221

10.  Development of PROTACs to address clinical limitations associated with BTK-targeted kinase inhibitors.

Authors:  Rachael Arthur; Beatriz Valle-Argos; Andrew J Steele; Graham Packham
Journal:  Explor Target Antitumor Ther       Date:  2020-06-29
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