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[摘要]：Diazepinomicin is a structurally novel farnesylated dibenzodiazepinone discovered using a drug discovery platform (DECIPHER) designed for the screening of anticancer compounds from actinomycete cultures. Preclinical data suggest that diozepinomicin is a targeted anticancer drug with dual activity: selective binding to the peripheral benzodiazepine receptor (PBR), resulting in tumor apoptosis, and inhibition of the Ras/MAP kinase signaling pathway, which is involved in cellular proliferation and migration. The compound has demonstrated broad-spectrum antitumor activity in cancer cells in vitro and in tumor xenografts in vivo, including leukemia and solid tumors such as melanoma and glioma. It has been shown to be safe and well tolerated when administered as a continuous infusion in primates and in clinical studies in cancer patients. Efficacy has been observed in advanced cancer patients and the compound is under early clinical investigation for the treatment of glioblastoma multiforme. |
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