About: p53 Activator APR-246

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Attributes	Values
rdf:type	Class
rdfs:label	p53 Activator APR-246
rdfs:subClassOf	ANTINEOPLASTICS
Semantic_Type	Pharmacologic Substance
Preferred_Name	p53 Activator APR-246
UMLS_CUI	C2830138
PDQ_Open_Trial_Search_ID	643796
PDQ_Closed_Trial_Search_ID	643796
FULL_SYN	APR-246CNNCI p53 Activator APR-246PTNCI PRIMA-1METSYNCI
DEFINITION	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.NCI
code	C85465

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