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.
Keywords: Anticancer agents, apoptosis, cyclic tetrapeptides, depsipeptides, extrinsic pathway, histone deacetylase inhibitors,
HDAC, histone acetylation, histone deacetylation, intrinsic pathway, macrocycles.
Rights & PermissionsPrintExport
Published on: 27 March, 2013
Page: [1887 - 1903]