About: p53 Activator APR-246     Goto   Sponge   NotDistinct   Permalink

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AttributesValues
rdf:type
rdfs:label
  • p53 Activator APR-246
rdfs:subClassOf
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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