The “Master” tumor suppressor protein p53, which induces cell-cycle arrest and apoptosis through transcriptional regulation of specific target genes, is found mutated in more than 50% of the human tumors, making functional reactivation of the p53 pathway an attractive strategy for cancer therapy. Prodigiosin, a natural product with known potent anti-cancer activity, is able to induce the expression of structurally related to p53 protein p73 and disrupt its interaction with the mutant p53, thereby rescuing p53 pathway deficiency and promoting anti-tumor effects in cancerous cells. Thus, the prodigiosin analogs are envisioned as promising anti-cancer therapeutics with the benefit of small molecules acting in a targeted manner. Currently, no drugs directed into restoration of p53 protein activity are on the market.
Summary of the Invention
Expert researchers in the p53 protein field from Fox Chase Cancer Center have tested successfully prodiogiosin analogs for anti-cancer activity in vast number of mammalian cells. These novel small molecules are projected powerful therapeutics for treating cancers in which p53 mutation is detected, including but not limited to prostate cancer, breast cancer, kidney cancer, ovarian cancer, lymphoma, leukemia, and glioblastoma.
Reference: Prabhu V.V. at al., 2016, Cancer Res. 76 (7): 1989-99.
• Novel therapeutics for treating various cancers.
• Targeted restoration of p53 tumor suppressor protein activity.
• Inexpensive small molecules.
PCT publication WO2017177216 A1
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Inna Khartchenko, MS, MBA
Director, Technology Transfer