loading...| Preferred Name |
vorinostat |
|
| Synonyms |
N-hydroxy-N'-phenyloctanediamide |
|
| Definitions |
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. Check for "https://www.cancer.gov/about-cancer/treatment/clinical-trials/intervention/C1796" active clinical trials using this agent. ("http://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI%20Thesaurus&code=C1796" NCI Thesaurus) |
|
| ID |
http://purl.bioontology.org/ontology/PDQ/CDR0000037944 |
|
| altLabel |
N-hydroxy-N'-phenyloctanediamide SAHA L-001079038 Zolinza MSK390 suberoylanilide hydroxamic acid |
|
| Component of |
http://purl.bioontology.org/ontology/PDQ/CDR0000437143 http://purl.bioontology.org/ontology/PDQ/CDR0000445585 |
|
| cui |
C0672708 C1738860 C4087052 C1832065 |
|
| Date last modified |
2015-11-05 |
|
| definition |
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. Check for "https://www.cancer.gov/about-cancer/treatment/clinical-trials/intervention/C1796" active clinical trials using this agent. ("http://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI%20Thesaurus&code=C1796" NCI Thesaurus) |
|
| Legacy PDQ ID |
10363 |
|
| LT |
TRD |
|
| NCI ID |
C1796 |
|
| notation |
CDR0000037944 |
|
| ORIG STY |
Drug/agent |
|
| prefLabel |
vorinostat |
|
| tui |
T109 T121 |