Histone deacetylase inhibitor

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.

[1] 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.

[2] 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.

[3] 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.

[4] 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.

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