Literature DB >> 22277276

Design and synthesis of estrogen receptor degradation inducer based on a protein knockdown strategy.

Yosuke Demizu1, Keiichiro Okuhira, Hiromi Motoi, Akiko Ohno, Takuji Shoda, Kiyoshi Fukuhara, Haruhiro Okuda, Mikihiko Naito, Masaaki Kurihara.   

Abstract

We designed and synthesized estrogen receptor (ER) degradation inducers 5, 6, and 7, which crosslink the ER and the cellular inhibitor of apoptosis protein 1 (cIAP1). Compounds 5, 6, and 7 induced cIAP1-mediated ubiquitylation of ERα resulting in its proteasomal degradation.
Copyright © 2012. Published by Elsevier Ltd.

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Year:  2011        PMID： 22277276     DOI： 10.1016/j.bmcl.2011.11.086

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  22 in total

1.  In Vivo Knockdown of Pathogenic Proteins via Specific and Nongenetic Inhibitor of Apoptosis Protein (IAP)-dependent Protein Erasers (SNIPERs).

Authors:  Nobumichi Ohoka; Keiichiro Okuhira; Masahiro Ito; Katsunori Nagai; Norihito Shibata; Takayuki Hattori; Osamu Ujikawa; Kenichiro Shimokawa; Osamu Sano; Ryokichi Koyama; Hisashi Fujita; Mika Teratani; Hirokazu Matsumoto; Yasuhiro Imaeda; Hiroshi Nara; Nobuo Cho; Mikihiko Naito
Journal:  J Biol Chem       Date:  2017-02-02       Impact factor: 5.157

Review 2.  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

3.  New Class of Selective Estrogen Receptor Degraders (SERDs): Expanding the Toolbox of PROTAC Degrons.

Authors:  Lucia Wang; Valeria S Guillen; Naina Sharma; Kevin Flessa; Jian Min; Kathryn E Carlson; Weiyi Toy; Sara Braqi; Benita S Katzenellenbogen; John A Katzenellenbogen; Sarat Chandarlapaty; Abhishek Sharma
Journal:  ACS Med Chem Lett       Date:  2018-07-05       Impact factor: 4.345

Review 4.  Targeted protein knockdown using small molecule degraders.

Authors:  Kanak Raina; Craig M Crews
Journal:  Curr Opin Chem Biol       Date:  2017-06-09       Impact factor: 8.822

Review 5.  Targeted Protein Degradation: from Chemical Biology to Drug Discovery.

Authors:  Philipp M Cromm; Craig M Crews
Journal:  Cell Chem Biol       Date:  2017-06-22       Impact factor: 8.116

Review 6.  Proteolysis-targeting chimaeras (PROTACs) as pharmacological tools and therapeutic agents: advances and future challenges.

Authors:  Chao Wang; Yujing Zhang; Tingting Zhang; Lingyu Shi; Zhongmin Geng; Dongming Xing
Journal:  J Enzyme Inhib Med Chem       Date:  2022-12       Impact factor: 5.756

7.  Delineating the role of cooperativity in the design of potent PROTACs for BTK.

Authors:  Adelajda Zorba; Chuong Nguyen; Yingrong Xu; Jeremy Starr; Kris Borzilleri; James Smith; Hongyao Zhu; Kathleen A Farley; WeiDong Ding; James Schiemer; Xidong Feng; Jeanne S Chang; Daniel P Uccello; Jennifer A Young; Carmen N Garcia-Irrizary; Lara Czabaniuk; Brandon Schuff; Robert Oliver; Justin Montgomery; Matthew M Hayward; Jotham Coe; Jinshan Chen; Mark Niosi; Suman Luthra; Jaymin C Shah; Ayman El-Kattan; Xiayang Qiu; Graham M West; Mark C Noe; Veerabahu Shanmugasundaram; Adam M Gilbert; Matthew F Brown; Matthew F Calabrese
Journal:  Proc Natl Acad Sci U S A       Date:  2018-07-16       Impact factor: 11.205

Review 8.  The emerging role for Cullin 4 family of E3 ligases in tumorigenesis.

Authors:  Ji Cheng; Jianping Guo; Brian J North; Kaixiong Tao; Pengbo Zhou; Wenyi Wei
Journal:  Biochim Biophys Acta Rev Cancer       Date:  2018-12-30       Impact factor: 10.680

9.  Snapshots and ensembles of BTK and cIAP1 protein degrader ternary complexes.

Authors:  James Schiemer; Reto Horst; Yilin Meng; Justin I Montgomery; Yingrong Xu; Xidong Feng; Kris Borzilleri; Daniel P Uccello; Carolyn Leverett; Stephen Brown; Ye Che; Matthew F Brown; Matthew M Hayward; Adam M Gilbert; Mark C Noe; Matthew F Calabrese
Journal:  Nat Chem Biol       Date:  2020-11-16       Impact factor: 15.040

Review 10.  E3 Ligase Ligands in Successful PROTACs: An Overview of Syntheses and Linker Attachment Points.

Authors:  Aleša Bricelj; Christian Steinebach; Robert Kuchta; Michael Gütschow; Izidor Sosič
Journal:  Front Chem       Date:  2021-07-05       Impact factor: 5.221
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