p53 mutant reactivator APR-548

{
  "id": "MLC-T-ONC-015748",
  "term": "p53 mutant reactivator APR-548",
  "field": "Oncology and biomedicine",
  "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.",
  "references": [
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/p53-mutant-reactivator-apr-548/"
}