Compounds that inhibit histone deacetylases
Histone deacetylase inhibitors (HDAC inhibitors , HDACi , HDIs ) are chemical compounds that inhibit histone deacetylases . Since deacetylation of histones produces transcriptionally silenced heterochromatin , HDIs can render chromatin more transcriptionally active and induce epigenomic changes.
HDIs have a long history of use in psychiatry and neurology as mood stabilizers and anti-epileptics , such as valproic acid . Since at least 2003 they have been investigated as possible treatments for cancers,[ 1] [ 2] parasitic[ 3] and inflammatory diseases.[ 4]
^ Miller TA, Witter DJ, Belvedere S (November 2003). "Histone deacetylase inhibitors" . Journal of Medicinal Chemistry . 46 (24): 5097–116. doi :10.1021/jm0303094 . PMID 14613312 .
^ Mwakwari SC, Patil V, Guerrant W, Oyelere AK (2010). "Macrocyclic histone deacetylase inhibitors" . Current Topics in Medicinal Chemistry . 10 (14): 1423–40. doi :10.2174/156802610792232079 . PMC 3144151 . PMID 20536416 .
^ Patil V, Guerrant W, Chen PC, Gryder B, Benicewicz DB, Khan SI, et al. (January 2010). "Antimalarial and antileishmanial activities of histone deacetylase inhibitors with triazole-linked cap group" . Bioorganic & Medicinal Chemistry . 18 (1): 415–25. doi :10.1016/j.bmc.2009.10.042 . PMC 2818366 . PMID 19914074 .
^ Blanchard F, Chipoy C (February 2005). "Histone deacetylase inhibitors: new drugs for the treatment of inflammatory diseases?" . Drug Discovery Today . 10 (3): 197–204. doi :10.1016/S1359-6446(04)03309-4 . PMID 15708534 .