Literature DB >> 32519703

Scaffold hopping enables direct access to more potent PROTACs with in vivo activity.

George M Burslem1, Daniel P Bondeson1, Craig M Crews2.   

Abstract

Herein we employ a scaffold hopping approach to enhance the activity of a previously reported BCR-Abl PROTAC. This represents a significant advance in the PROTAC field since it can abrogate the need to optimize the linker to access a more potent degrader. The new PROTAC demonstrates a >10 fold increase in ability to induce degradation and demonstrates in vivo activity.

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Year:  2020        PMID： 32519703      PMCID： PMC7404552          DOI： 10.1039/d0cc02201b

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


  27 in total

1.  Impact of linker length on the activity of PROTACs.

Authors:  Kedra Cyrus; Marie Wehenkel; Eun-Young Choi; Hyeong-Jun Han; Hyosung Lee; Hollie Swanson; Kyung-Bo Kim
Journal:  Mol Biosyst       Date:  2010-10-04

2.  Substrate-assisted inhibition of ubiquitin-like protein-activating enzymes: the NEDD8 E1 inhibitor MLN4924 forms a NEDD8-AMP mimetic in situ.

Authors:  James E Brownell; Michael D Sintchak; James M Gavin; Hua Liao; Frank J Bruzzese; Nancy J Bump; Teresa A Soucy; Michael A Milhollen; Xiaofeng Yang; Anne L Burkhardt; Jingya Ma; Huay-Keng Loke; Trupti Lingaraj; Dongyun Wu; Kristin B Hamman; James J Spelman; Courtney A Cullis; Steven P Langston; Stepan Vyskocil; Todd B Sells; William D Mallender; Irache Visiers; Ping Li; Christopher F Claiborne; Mark Rolfe; Joseph B Bolen; Lawrence R Dick
Journal:  Mol Cell       Date:  2010-01-15       Impact factor: 17.970

3.  The Advantages of Targeted Protein Degradation Over Inhibition: An RTK Case Study.

Authors:  George M Burslem; Blake E Smith; Ashton C Lai; Saul Jaime-Figueroa; Daniel C McQuaid; Daniel P Bondeson; Momar Toure; Hanqing Dong; Yimin Qian; Jing Wang; Andrew P Crew; John Hines; Craig M Crews
Journal:  Cell Chem Biol       Date:  2017-11-09       Impact factor: 8.116

4.  Lessons in PROTAC Design from Selective Degradation with a Promiscuous Warhead.

Authors:  Daniel P Bondeson; Blake E Smith; George M Burslem; Alexandru D Buhimschi; John Hines; Saul Jaime-Figueroa; Jing Wang; Brian D Hamman; Alexey Ishchenko; Craig M Crews
Journal:  Cell Chem Biol       Date:  2017-11-09       Impact factor: 8.116

Review 5.  PROteolysis TArgeting Chimeras (PROTACs) - Past, present and future.

Authors:  Mariell Pettersson; Craig M Crews
Journal:  Drug Discov Today Technol       Date:  2019-02-13

Review 6.  Induced protein degradation: an emerging drug discovery paradigm.

Authors:  Ashton C Lai; Craig M Crews
Journal:  Nat Rev Drug Discov       Date:  2016-11-25       Impact factor: 84.694

7.  Jostling for position: optimizing linker location in the design of estrogen receptor-targeting PROTACs.

Authors:  Kedra Cyrus; Marie Wehenkel; Eun-Young Choi; Hyosung Lee; Hollie Swanson; Kyung-Bo Kim
Journal:  ChemMedChem       Date:  2010-07-05       Impact factor: 3.466

Review 8.  Targeted protein degradation: elements of PROTAC design.

Authors:  Stacey-Lynn Paiva; Craig M Crews
Journal:  Curr Opin Chem Biol       Date:  2019-04-17       Impact factor: 8.822

9.  Differential PROTAC substrate specificity dictated by orientation of recruited E3 ligase.

Authors:  Blake E Smith; Stephen L Wang; Saul Jaime-Figueroa; Alicia Harbin; Jing Wang; Brian D Hamman; Craig M Crews
Journal:  Nat Commun       Date:  2019-01-10       Impact factor: 14.919

10.  Targeting Bcr-Abl by combining allosteric with ATP-binding-site inhibitors.

Authors:  Jianming Zhang; Francisco J Adrián; Wolfgang Jahnke; Sandra W Cowan-Jacob; Allen G Li; Roxana E Iacob; Taebo Sim; John Powers; Christine Dierks; Fangxian Sun; Gui-Rong Guo; Qiang Ding; Barun Okram; Yongmun Choi; Amy Wojciechowski; Xianming Deng; Guoxun Liu; Gabriele Fendrich; André Strauss; Navratna Vajpai; Stephan Grzesiek; Tove Tuntland; Yi Liu; Badry Bursulaya; Mohammad Azam; Paul W Manley; John R Engen; George Q Daley; Markus Warmuth; Nathanael S Gray
Journal:  Nature       Date:  2010-01-13       Impact factor: 49.962
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  3 in total

Review 1.  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 2.  Proteolysis-targeting chimeras (PROTACs) in cancer therapy.

Authors:  Xinyi Li; Wenchen Pu; Qingquan Zheng; Min Ai; Song Chen; Yong Peng
Journal:  Mol Cancer       Date:  2022-04-11       Impact factor: 27.401

Review 3.  Current strategies for the design of PROTAC linkers: a critical review.

Authors:  Robert I Troup; Charlene Fallan; Matthias G J Baud
Journal:  Explor Target Antitumor Ther       Date:  2020-10-30
  3 in total

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