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Chemistry and Biology of Chromatin Remodeling Agents: State of Art and Future Perspectives of HDAC Inhibitors

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Abstract:

Chromatin remodeling is a fundamental phenomenon in the life of eukaryotic cells, bearing implications to numerous physiological and pathological phenomena. This review outlines the chemistry of natural and synthetic agents endowed with the ability to interfere with such biological function, with a particular emphasis on histone deacetylase (HDAC) inhibitors. Other aspects covered in this article comprise structure activity relationships (SAR) and modes of action at molecular level, including the description of crystal structures of enzyme-inhibitor complexes.

Keywords: Antitumor; Apoptosis; Chromatin remodeling agents; Epigenetic therapy; HDAC inhibitors; Histone acetyltransferase; Histone deacetylase

Document Type: Research Article

DOI: http://dx.doi.org/10.2174/092986706776360905

Affiliations: Dipartimento di Scienze Farmaceutiche, Universita degli Studi di Salerno, Via Don Melillo, 84084, Fisciano, Salerno, Italy.

Publication date: April 1, 2006

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  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.
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