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Vorinostat
Pronunciation
Definition 1
A drug that is used to treat cutaneous T-cell lymphoma that does not get better, gets worse, or comes back during or after treatment with other drugs. It is also being studied in the treatment of other types of cancer. Vorinostat is a type of histone deacetylase inhibitor. Also called SAHA, suberoylanilide hydroxamic acid, and Zolinza. (NCI Dictionary)
Definition 2
A synthetic hydroxamic acid derivative with antineoplastic activity. Vorinostat, a second generation polar-planar compound, binds to the catalytic domain of the histone deacetylases (HDACs). This allows the hydroxamic moiety to chelate zinc ion located in the catalytic pockets of HDAC, thereby inhibiting deacetylation and leading to an accumulation of both hyperacetylated histones and transcription factors. Hyperacetylation of histone proteins results in the upregulation of the cyclin-dependant kinase p21, followed by G1 arrest. Hyperacetylation of non-histone proteins such as tumor suppressor p53, alpha tubulin, and heat-shock protein 90 produces additional anti-proliferative effects. This agent also induces apoptosis and sensitizes tumor cells to cell death processes. Vorinostat crosses the blood-brain barrier. (NCI Thesaurus)
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