Literature DB >> 31769449

Plasticity in designing PROTACs for selective and potent degradation of HDAC6.

Haiyan Yang1, Wenxing Lv, Ming He, Haiteng Deng, Haitao Li, Wei Wu, Yu Rao.   

Abstract

HDAC6 (histone deacetylase 6) catalyses the deacetylation of non-histone substrates, and plays important roles in cell migration, protein degradation and other cellular processes. Here we report that CRBN-recruiting PROTAC NH2, which introduces pomalidomide at the benzene ring of Nex A, reaches comparable degradation efficiency of HDAC6 compared to aliphatic-chain-introducing PROTAC NP8.

Entities:  

Year:  2019        PMID： 31769449     DOI： 10.1039/c9cc08509b

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


  18 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

2.  Development of Selective Histone Deacetylase 6 (HDAC6) Degraders Recruiting Von Hippel-Lindau (VHL) E3 Ubiquitin Ligase.

Authors:  Ka Yang; Hao Wu; Zhongrui Zhang; Eric D Leisten; Xueqing Nie; Binkai Liu; Zhi Wen; Jing Zhang; Michael D Cunningham; Weiping Tang
Journal:  ACS Med Chem Lett       Date:  2020-03-18       Impact factor: 4.345

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.  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 5.  HDAC6-an Emerging Target Against Chronic Myeloid Leukemia?

Authors:  Hélène Losson; Michael Schnekenburger; Mario Dicato; Marc Diederich
Journal:  Cancers (Basel)       Date:  2020-01-29       Impact factor: 6.639

Review 6.  Anticancer Therapy with HDAC Inhibitors: Mechanism-Based Combination Strategies and Future Perspectives.

Authors:  Robert Jenke; Nina Reßing; Finn K Hansen; Achim Aigner; Thomas Büch
Journal:  Cancers (Basel)       Date:  2021-02-05       Impact factor: 6.639

Review 7.  Opportunities and Challenges of Small Molecule Induced Targeted Protein Degradation.

Authors:  Ming He; Wenxing Lv; Yu Rao
Journal:  Front Cell Dev Biol       Date:  2021-06-22

8.  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

Review 9.  Bifunctional HDAC Therapeutics: One Drug to Rule Them All?

Authors:  Joshua P Smalley; Shaun M Cowley; James T Hodgkinson
Journal:  Molecules       Date:  2020-09-24       Impact factor: 4.411

10.  Discovery of an orally active VHL-recruiting PROTAC that achieves robust HMGCR degradation and potent hypolipidemic activity in vivo.

Authors:  Guoshun Luo; Zhenbang Li; Xin Lin; Xinyu Li; Yu Chen; Kun Xi; Maoxu Xiao; Hanlin Wei; Lizhe Zhu; Hua Xiang
Journal:  Acta Pharm Sin B       Date:  2020-11-06       Impact factor: 11.413
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