Affiliation:
1. State Key Laboratory of Functions and Applications of Medicinal Plants, Engineering Research Center for the Development and Application of Ethnic Medicine and TCM (Ministry of Education), Guizhou Medical University, Guiyang 550004, China
Abstract
The state of histone acetylation plays a very crucial role in carcinogenesis and its development
by chromatin remodeling and thus altering transcription of oncogenes and tumor suppressor genes. Such
epigenetic regulation was controlled by zinc-dependent histone deacetylases (HDACs), one of the major
regulators. Due to the therapeutic potential of HDACs as one of the promising drug targets in cancer,
HDAC inhibitors have been intensively investigated over the last few decades. Notably, there are five
HDAC inhibitors already approved to the market. Vorinostat (SAHA), Belinostat (PXD-101) and Romidepsin
(FK228) have been approved by Food and Drug Administration (FDA) in USA for treating cutaneous
T-cell lymphoma (CTCL) or peripheral T cell lymphoma (PTCL) while Panbinostat (LBH-589) has
also been approved by the FDA for the treatment of multiple myeloma. Recently, Chidamide was approved
by China Food and Drug Administration (CFDA) for the treatment of PTCL. The structural feature of almost
all HDAC inhibitors consists of Cap group, linker, and zinc-binding group (ZBG). The binding of
ZBG groups to zinc ion plays a decisive role in the inhibition of HDAC. Therefore, we will summarize the
developed HDAC inhibitors according to different ZBG groups and discuss their binding mode with zinc
ion.
Funder
Department of Science and Technology of Guizhou Province
Guiyang Municipal Science and Technology Project
Natural Science Foundation of Guizhou Province
National Natural Science Foundation of China
Publisher
Bentham Science Publishers Ltd.
Subject
Drug Discovery,General Medicine
Cited by
50 articles.
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