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Peptide Based Macrocycles: Selective Histone Deacetylase Inhibitors with Antiproliferative Activity

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Histone deacetylase inhibitors (HDACi) have been enthusiastically investigated as a novel generation of chemotherapeutics for cancers usually called as epigenetic therapeutics. Histone deacetylases have been found to influence cellular function by catalyzing the removal of acetyl groups from ε-N-acetylated lysine residues of several protein substrates including histones, transcription factors, α-tubulin, and nuclear importers. Cyclic peptides represent the most structurally complicated and diverse class of histone deacetylase inhibitors. Each subtype of the Histone Deacetylase (HDAC) family perform a distinct role in the gene expression and cyclic peptides with their plentiful set of surface contacts, zinc binding group and macrocyclic cap, can target enzyme precisely through adequate modulation of the amino acid configurational and structural assortment. The present article summarizes current status of different peptide based macrocyclic compounds being developed as HDACi for the treatment of cancer.
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Keywords: Anticancer agents; HDAC; apoptosis; cyclic tetrapeptides; depsipeptides; extrinsic pathway; histone acetylation; histone deacetylase inhibitors; histone deacetylation; intrinsic pathway; macrocycles

Document Type: Research Article

Publication date: 01 May 2013

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