Literature DB >> 32201871

PROTAC-mediated degradation of class I histone deacetylase enzymes in corepressor complexes.

Joshua P Smalley1, Grace E Adams2, Christopher J Millard3, Yun Song3, James K S Norris1, John W R Schwabe3, Shaun Michael Cowley2, James T Hodgkinson1.   

Abstract

We have identified a proteolysis targeting chimera (PROTAC) of class I HDACs 1, 2 and 3. The most active degrader consists of a benzamide HDAC inhibitor, an alkyl linker, and the von Hippel-Lindau E3 ligand. Our PROTAC increased histone acetylation levels and compromised colon cancer HCT116 cell viability, establishing a degradation strategy as an alternative to class I HDAC inhibition.

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Year:  2020        PMID： 32201871      PMCID： PMC7610821          DOI： 10.1039/d0cc01485k

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


  31 in total

1.  Histone deacetylase (HDAC) inhibitor kinetic rate constants correlate with cellular histone acetylation but not transcription and cell viability.

Authors:  Benjamin E L Lauffer; Robert Mintzer; Rina Fong; Susmith Mukund; Christine Tam; Inna Zilberleyb; Birgit Flicke; Allegra Ritscher; Grazyna Fedorowicz; Roxanne Vallero; Daniel F Ortwine; Janet Gunzner; Zora Modrusan; Lars Neumann; Christopher M Koth; Patrick J Lupardus; Joshua S Kaminker; Christopher E Heise; Pascal Steiner
Journal:  J Biol Chem       Date:  2013-07-29       Impact factor: 5.157

Review 2.  Histone deacetylases and their inhibitors in cancer, neurological diseases and immune disorders.

Authors:  Katrina J Falkenberg; Ricky W Johnstone
Journal:  Nat Rev Drug Discov       Date:  2014-08-18       Impact factor: 84.694

Review 3.  PROteolysis TArgeting Chimeras (PROTACs) - Past, present and future.

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

4.  Histone deacetylase 1 (HDAC1), but not HDAC2, controls embryonic stem cell differentiation.

Authors:  Oliver M Dovey; Charles T Foster; Shaun M Cowley
Journal:  Proc Natl Acad Sci U S A       Date:  2010-04-19       Impact factor: 11.205

Review 5.  HDAC expression and clinical prognosis in human malignancies.

Authors:  Wilko Weichert
Journal:  Cancer Lett       Date:  2008-12-21       Impact factor: 8.679

Review 6.  Physiological roles of class I HDAC complex and histone demethylase.

Authors:  Tomohiro Hayakawa; Jun-Ichi Nakayama
Journal:  J Biomed Biotechnol       Date:  2010-10-26

7.  Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4.

Authors:  Michael Zengerle; Kwok-Ho Chan; Alessio Ciulli
Journal:  ACS Chem Biol       Date:  2015-06-16       Impact factor: 5.100

8.  H3K9ac and HDAC2 Activity Are Involved in the Expression of Monocarboxylate Transporter 1 in Oligodendrocyte.

Authors:  Qingwei Lai; Wantong Du; Jian Wu; Xiao Wang; Xinyu Li; Xuebin Qu; Xiuxiang Wu; Fuxing Dong; Ruiqin Yao; Hongbin Fan
Journal:  Front Mol Neurosci       Date:  2017-11-14       Impact factor: 5.639

9.  Class I histone deacetylase (HDAC) inhibitor CI-994 promotes functional recovery following spinal cord injury.

Authors:  Suxiang Zhang; Yuki Fujita; Rieko Matsuzaki; Toshihide Yamashita
Journal:  Cell Death Dis       Date:  2018-05-01       Impact factor: 8.469

10.  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
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  20 in total

1.  Developing HDAC4-Selective Protein Degraders To Investigate the Role of HDAC4 in Huntington's Disease Pathology.

Authors:  Natsuko Macabuag; William Esmieu; Perla Breccia; Rebecca Jarvis; Wesley Blackaby; Ovadia Lazari; Liudvikas Urbonas; Maria Eznarriaga; Rachel Williams; Annelieke Strijbosch; Rhea Van de Bospoort; Kim Matthews; Cole Clissold; Tammy Ladduwahetty; Huw Vater; Patrick Heaphy; Douglas G Stafford; Hong-Jun Wang; John E Mangette; George McAllister; Vahri Beaumont; Thomas F Vogt; Hilary A Wilkinson; Elizabeth M Doherty; Celia Dominguez
Journal:  J Med Chem       Date:  2022-09-13       Impact factor: 8.039

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

3.  Discovery of histone deacetylase 3 (HDAC3)-specific PROTACs.

Authors:  Yufeng Xiao; Jia Wang; Lisa Y Zhao; Xinyi Chen; Guangrong Zheng; Xuan Zhang; Daiqing Liao
Journal:  Chem Commun (Camb)       Date:  2020-08-25       Impact factor: 6.222

Review 4.  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 5.  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

Review 6.  Proteolysis targeting chimeras (PROTACs) are emerging therapeutics for hematologic malignancies.

Authors:  Yonghan He; Sajid Khan; Zhiguang Huo; Dongwen Lv; Xuan Zhang; Xingui Liu; Yaxia Yuan; Robert Hromas; Mingjiang Xu; Guangrong Zheng; Daohong Zhou
Journal:  J Hematol Oncol       Date:  2020-07-27       Impact factor: 17.388

Review 7.  Proteasomal and lysosomal degradation for specific and durable suppression of immunotherapeutic targets.

Authors:  Yungang Wang; Shouyan Deng; Jie Xu
Journal:  Cancer Biol Med       Date:  2020-08-15       Impact factor: 4.248

8.  Chemo-proteomics exploration of HDAC degradability by small molecule degraders.

Authors:  Yuan Xiong; Katherine A Donovan; Nicholas A Eleuteri; Nadia Kirmani; Hong Yue; Anthony Razov; Noah M Krupnick; Radosław P Nowak; Eric S Fischer
Journal:  Cell Chem Biol       Date:  2021-07-26       Impact factor: 9.039

9.  Development of a Bestatin-SAHA Hybrid with Dual Inhibitory Activity against APN and HDAC.

Authors:  Jiangying Cao; Wei Zhao; Chunlong Zhao; Qian Liu; Shunda Li; Guozhen Zhang; C James Chou; Yingjie Zhang
Journal:  Molecules       Date:  2020-10-28       Impact factor: 4.411

10.  Hydroxamic Acids Immobilized on Resins (HAIRs): Synthesis of Dual-Targeting HDAC Inhibitors and HDAC Degraders (PROTACs).

Authors:  Laura Sinatra; Jan J Bandolik; Martin Roatsch; Melf Sönnichsen; Clara T Schoeder; Alexandra Hamacher; Andrea Schöler; Arndt Borkhardt; Jens Meiler; Sanil Bhatia; Matthias U Kassack; Finn K Hansen
Journal:  Angew Chem Int Ed Engl       Date:  2020-10-09       Impact factor: 15.336
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