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Current Topics in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

Macrocyclic Histone Deacetylase Inhibitors

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

Volume 10, Issue 14, 2010

Page: [1423 - 1440] Pages: 18

DOI: 10.2174/156802610792232079

Price: $65

Abstract

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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