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- Bfa446c6acf15cb7bef574e013c3d417d NCIT_P378 "NCI" @default.
- Bfa446c6acf15cb7bef574e013c3d417d type Axiom @default.
- Bfa446c6acf15cb7bef574e013c3d417d annotatedProperty IAO_0000115 @default.
- Bfa446c6acf15cb7bef574e013c3d417d annotatedSource NCIT_C1796 @default.
- Bfa446c6acf15cb7bef574e013c3d417d annotatedTarget "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." @default.