Issue 98, 2019
From the journal:

Chemical Communications

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

Haiyan Yang, ORCID logo ‡a   Wenxing Lv,‡b   Ming He,b   Haiteng Deng,c   Haitao Li,d   Wei Wu*a  and  Yu Rao ORCID logo *b  

* Corresponding authors

a MOE Key Laboratory of Protein Sciences, School of Life Sciences, Tsinghua University, Beijing 100084, P. R. China
E-mail: wwu@mail.tsinghua.edu.cn

b MOE Key Laboratory of Protein Sciences, School of Pharmaceutical Sciences, MOE Key Laboratory of Bioorganic Phosphorus Chemistry & Chemical Biology, Tsinghua University, Beijing 100084, P. R. China
E-mail: yrao@mail.tsinghua.edu.cn

c Tsinghua-Peking Center for Life Sciences, Center for Structural Biology, School of Life Sciences and School of Medicine, Tsinghua University, Beijing, 100084, China

d MOE Key Laboratory of Protein Sciences, Beijing Advanced Innovation Center for Structural Biology, Beijing Frontier Research Center for Biological Structure, Tsinghua-Peking Joint Center for Life Sciences, Department of Basic Medical Sciences, School of Medicine, Tsinghua University, 100084 Beijing, China

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.

Graphical abstract: Plasticity in designing PROTACs for selective and potent degradation of HDAC6

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Article information

DOI
https://doi.org/10.1039/C9CC08509B
Article type
Communication
Submitted
31 Oct 2019
Accepted
08 Nov 2019
First published
19 Nov 2019

Chem. Commun., 2019,55, 14848-14851

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Plasticity in designing PROTACs for selective and potent degradation of HDAC6

H. Yang, W. Lv, M. He, H. Deng, H. Li, W. Wu and Y. Rao, Chem. Commun., 2019, 55, 14848 DOI: 10.1039/C9CC08509B

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