Macrocyclic Histone Deacetylase Inhibitors

Author(s): Sandra C. Mwakwari, Vishal Patil, William Guerrant, Adegboyega K. Oyelere

Journal Name: Current Topics in Medicinal Chemistry

Volume 10 , Issue 14 , 2010

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Histone deacetylase inhibitors (HDACi) are an emerging class of novel anti-cancer drugs that cause growth arrest, differentiation, and apoptosis of tumor cells. In addition, they have shown promise as anti-parasitic, antineurodegenerative, anti-rheumatologic and immunosuppressant agents. To date, several structurally distinct small molecule HDACi have been reported including aryl hydroxamates, benzamides, short-chain fatty acids, electrophilic ketones, and macrocyclic peptides. Macrocyclic HDACi possess the most complex cap-groups which interact with HDAC enzyme's outer rim and have demonstrated excellent HDAC inhibition potency and isoform selectivity. This review focuses on the recent progress and current state of macrocyclic HDACi.

Keywords: Cyclic tetrapeptide, depsipeptide, peptide mimetic, macrolide, ketolide, macrocycles, histone deacetylase inhibitors, HDAC

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Article Details

Year: 2010
Published on: 01 March, 2012
Page: [1423 - 1440]
Pages: 18
DOI: 10.2174/156802610792232079
Price: $65

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