Bifunctional HDAC Therapeutics: One Drug to Rule Them All?
Bifunctional HDAC Therapeutics: One Drug to Rule Them All?
复制标题
DOI：
10.3390/molecules25194394
复制
发表时间：
2020-09-24
期刊：
影响因子：
--
通讯作者：
Hodgkinson JT
中科院分区：
文献类型：
--
作者：
Smalley JP;Cowley SM;Hodgkinson JT
Histone deacetylase (HDAC) enzymes play crucial roles in epigenetic gene expression and are an attractive therapeutic target. Five HDAC inhibitors have been approved for cancer treatment to date, however, clinical applications have been limited due to poor single-agent drug efficacy and side effects associated with a lack of HDAC isoform or complex selectivity. An emerging strategy aiming to address these limitations is the development of bifunctional HDAC therapeutics—single molecules comprising a HDAC inhibitor conjugated to another specificity targeting moiety. This review summarises the recent advancements in novel types of dual-targeting HDAC modulators, including proteolysis-targeting chimeras (PROTACs), with a focus on HDAC isoform and complex selectivity, and the future potential of such bifunctional molecules in achieving enhanced drug efficacy and therapeutic benefits in treating disease.
登录
查看更多内容
影响因子：
--
作者：
Aldana-Masangkay GI;Sakamoto KM
通讯作者：
Sakamoto KM
影响因子：
56.9
作者：
Choudhary, Chunaram;Kumar, Chanchal;Mann, Matthias
通讯作者：
Mann, Matthias
影响因子：
46.9
作者：
Bantscheff, Marcus;Hopf, Carsten;Drewes, Gerard
通讯作者：
Drewes, Gerard
影响因子：
4.8
作者：
Chou, C. James;Herman, David;Gottesfeld, Joel M.
通讯作者：
Gottesfeld, Joel M.
影响因子：
--
作者：
Booth L;Roberts JL;Sander C;Lee J;Kirkwood JM;Poklepovic A;Dent P
通讯作者：
Dent P