Inhibitor of the E3 ligase human double minute-2 (HDM2); cholesterol transport inhibitor
JNJ-26854165 (serdemetan) is an inhibitor of the E3 ligase human double minute-2 (HDM2) that inhibits cell proliferation and induces apoptosis in models of acute myeloid and lymphoid leukemias, and solid tumors. Also JNJ-26854165 inhibits cholesterol transport. JNJ-26854165 appears to stimulate cholesterol regulatory genes, but simultaneously inhibits cholesterol transport.
International journal of molecular sciences, 22(16) (2021-08-28)
As the most common gene mutation found in cancers, p53 mutations are detected in up to 96% of high-grade serous ovarian carcinoma (HGSOC). Meanwhile, mutant p53 overexpression is known to drive oncogenic phenotypes in cancer patients and to sustain the
Chronic myeloid leukemia (CML) is a clonal malignant disease caused by the expression of BCR/ABL. MDM2 (human homolog of the murine double minute-2) inhibitors such as Nutlin-3 have been shown to induce apoptosis in a p53-dependent manner in CML cells
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