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Version: 17.06d (Release date: 2017-06-26)
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PRIMA-1 Analog APR-246 (Code C85465)

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Terms & Properties

Preferred Name: PRIMA-1 Analog APR-246

Definition: A methylated derivative and structural analog of PRIMA-1 (p53 re-activation and induction of massive apoptosis), with potential antineoplastic activity. Upon administration, PRIMA-1 analog APR-246 covalently modifies the core domain of mutated forms of cellular tumor antigen p53 (p53) through the alkylation of thiol groups. These modifications restore both the wild-type conformation and function to mutant p53, which reconstitutes endogenous p53 activity, leading to 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 frequently mutated and overexpressed in cancer cells; it plays a key role in both DNA repair and the induction of apoptosis.

Label: PRIMA-1 Analog APR-246

NCI Thesaurus Code: C85465 (Search for linked caDSR metadata)  (search value sets)

NCI Metathesaurus Link: C2830138  (see NCI Metathesaurus info)

Synonyms & Abbreviations: (see Synonym Details)
PRIMA-1 Analog APR-246

External Source Codes: 
PDQ Closed Trial Search ID 643796
PDQ Open Trial Search ID 643796 (check for NCI PDQ open clinical trial info)
UMLS CUI C2830138

Other Properties:
     Name Value (qualifiers indented underneath)
code C85465
Semantic_Type Pharmacologic Substance

Additional Concept Data: 
Defined Fully by Roles: No  


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