Frontiers in Medicinal Chemistry

Volume: 2

Indexed in: Scopus, EMBASE, Chemical Abstracts, EBSCO, Ulrich's Periodicals Directory.

Frontiers in Medicinal Chemistry is a book series devoted to the review of areas of important topical interest to medicinal chemists and others in allied disciplines. Frontiers in Medicinal Chemistry ...
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Histone Deacetylase Inhibitors: From Chromatin Remodelling to Experimental Cancer Therapeutics

Pp. 299-315 (17)

Janine Arts, Stefanie de Schepper and Kristof Van Emelen

Abstract

Histone deacetylases (HDACs) are key enzymes in the regulation of gene expression. By maintaining the dynamic equilibrium of the acetylation status of highly conserved lysine residues on histones, they regulate chromatin remodelling and gene expression. A link between aberrant HDAC activity and cancer has been widely reported and HDAC inhibitors have been shown to inhibit the proliferation of human tumor cell lines in vitro. Furthermore, several HDAC inhibitors have exhibited potent anti-tumor activity in human xenograft models, suggesting this class of compounds to be promising novel cancer therapeutic agents. This review provides an update on the current knowledge on HDAC inhibition with a focus on the most recent progress of HDAC inhibitors in clinical development.

Keywords:

Chromatin, histone acetylation, anti-cancer

Affiliation:

Department of Medicinal Chemistry, Johnson&Johnson Pharmaceutical Research and Development, Turnhoutseweg 30, 2340 Beerse, Belgium.