Preferred Label : p53 Mutant Reactivator APR-548;
NCIt definition : An analog of eprenetapopt and an orally bioavailable, small molecule prodrug and reactivator
of p53 mutants, with potential antineoplastic activity. Upon oral administration of
p53 mutant reactivator APR-548, as a prodrug APR-548 is converted to its active form,
2-methylene-quinuclidin-3-one (MQ), which binds to mutant p53 proteins at their DNA-binding
domain and restores wild-type p53 protein structure and activity. This reconstitutes
endogenous p53 activity, blocks tumor cell cycle progression and induces apoptosis
in tumor cells expressing the TP53 mutations. 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.;
Molecule name : APR 548; APR-548;
NCI Metathesaurus CUI : CL1661907;
Origin ID : C179264;
UMLS CUI : C5555564;
Semantic type(s)
- concept_is_in_subset
- has_target
