Histone deacetylase inhibitors and anticancer therapy.

Article Details

Citation

Kouraklis G, Theocharis S

Histone deacetylase inhibitors and anticancer therapy.

Curr Med Chem Anticancer Agents. 2002 Jul;2(4):477-84. doi: 10.2174/1568011023353921.

PubMed ID
12678732 [ View in PubMed
]
Abstract

Recent reports have shown that pharmacological manipulation of chromatin remodeling by histone deacetylase (HDAC) inhibitors, might develop into a potent and specific strategy for the treatment of cancer. Alterations in histone acetylation may lead to changes in chromatin structure and transcriptional dysregulation of genes that are implicated in controlling either cell cycle progression or pathways regulating cell differentiation and/or apoptosis. Dimethyl sulphoxide was one of the first chemicals to be identified as an inducer of transformed cell differentiation. In the class of HDAC inhibitors, now included a short-chain fatty acids, such as 4-phenylbutyrate and valporic acid, hydroxamic acids, such as suberoylanilide hydroxamic acid (SAHA), pyroxamide, trichostatin A, oxamflatin and CHAPSs, cyclic tetrapeptides, such as trapoxin, apicidin and depsipeptide-also known as FK-228 or FR 901228, and benzamides, such as MS-275. First clinical studies have shown that histone hyperacetylation can be achieved safely in humans and that treatment of cancer with such agents seems to become possible. Thus, HDAC inhibitors remains one of the most promising class of new anticancer agents. Further studies are needed in order to delineate the optimal dosage, the duration of therapy and possibly the efficacy of other agents able to synergize with HDAC inhibitors in the fight against cancer.

DrugBank Data that Cites this Article

Drug Targets
DrugTargetKindOrganismPharmacological ActionActions
EntinostatHistone deacetylase (Protein Group)Protein groupHumans
Yes
Inhibitor
Details
Phenylbutyric acidHistone deacetylase (Protein Group)Protein groupHumans
Unknown
Inhibitor
Details
PyroxamideHistone deacetylase (Protein Group)Protein groupHumans
Unknown
Inhibitor
Details
RomidepsinHistone deacetylase (Protein Group)Protein groupHumans
Unknown
Inhibitor
Details
Valproic acidHistone deacetylase (Protein Group)Protein groupHumans
Unknown
Inhibitor
Details
VorinostatHistone deacetylase (Protein Group)Protein groupHumans
Unknown
Inhibitor
Details