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Drugs that stop MDM2 destroying p53, reawakening the cell's guardian protein in tumours where p53 is intact but suppressed, such as some sarcomas and leukaemias.
MDM2 tags the tumour suppressor p53 for degradation, and MDM2 amplification is the hallmark of liposarcoma and other tumours that keep wild-type p53. Small molecules that block the MDM2-p53 interaction (idasanutlin, milademetan, navtemadlin, brigimadlin) restore p53 and cause cell-cycle arrest and death. Trials in acute myeloid leukaemia and liposarcoma have shown activity but also thrombocytopenia and gastrointestinal toxicity, and no agent is approved; combinations and intermittent dosing are being tested.
Inhibitors occupy the p53-binding pocket of MDM2, stabilising p53 so it can trigger apoptosis or senescence in cells with wild-type TP53.
Query for this technology: (TITLE:"MDM2 inhibitors" OR ABSTRACT:"MDM2 inhibitors") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about MDM2 inhibitors, not a curated reading list.
Shares Retroperitoneal sarcoma, Liposarcoma, Sarcomas (soft tissue, bone, GIST).
Shares Retroperitoneal sarcoma, Liposarcoma.
Shares MDM2, Liposarcoma.