Development of an Efficient Screening System for HDAC Inhibitor Based on TCF Response Element

Author(s): Chen Pang, Limeng Dai, Gang He, You Lu, Bo Zhang*

Journal Name: Anti-Cancer Agents in Medicinal Chemistry
(Formerly Current Medicinal Chemistry - Anti-Cancer Agents)

Volume 18 , Issue 15 , 2018

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Graphical Abstract:


Background: Acetylation of core histones is governed by opposing actions of a variety of histone acetyltransferases (HATs) and Histone Deacetylases (HDACs). Deregulation of histone acetylation has been causally linked to cancer development and progression, and can be potentially reversed by drug treatments. HDAC inhibitors (HDACis) have the anti-cancer effects such as induction of cell cycle arrest, promotion of cell apoptosis, and inhibition of metastasis. Many of these HDACis are currently in clinical development.

Methods: To screen for novel compound with HDACis activity, cell-based strategy has been developed in current work. The interaction of HDACs and TCFs was determined by reporter assay, and Natural products library (A10) was screened by our system in colon cancer cells.

Results: Based on the interaction of HDACs and TCFs, compounds with HDACis activity could be easily picked out from Natural products library (A10) by using this screening system. Finally, a compound Wsu-18 was preliminarily identified as a potential HDACis.

Conclusion: These data suggest our screening system for HDACis was efficient and promising, and it is suitable for screening other small molecular chemical libraries.

Keywords: Histone deacetylase, histone acetyltransferase, TCFs, screening system, HDAC inhibitor, Wsu-18, potential HDACis.

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Article Details

Year: 2018
Page: [2131 - 2136]
Pages: 6
DOI: 10.2174/1871520618666181031090614
Price: $65

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