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p53 activator APR-246
A quinuclidinone derivative that targets the Wrap53 gene with potential antineoplastic activity. p53 activator APR-246 binds to and activates transcription of the Wrap53 gene, which results in an increase in WRAP53 p53 antisense transcript levels and, potentially, an increase in native p53 activity; in turn, increased p53 activity may lead to an induction of cell cycle arrest and apoptosis in tumor cells. This agent may work synergistically with other antineoplastic agents. p53, a tumor suppressor and transcription factor normally activated upon DNA damage, is mutated or absent in various cancer cell types and plays a key role in DNA repair and the induction of apoptosis. The Wrap53 transcript, a natural p53 antisense transcript, regulates endogenous p53 mRNA levels and additional induction of p53 protein by targeting the 5' untranslated region of p53 mRNA. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus)
| Synonym: | | PRIMA-1MET | |
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| Code name: | | APR-246 | |
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