天然物由来のがん治療薬シーズの探索と標的分子の機能解析

概要

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As a part of our study of biologically active substances from marine organisms, we have been searching for new candidates for cancer chemotheraphy. We isolated a C_<36> linear acetylene alcohol named lembehyne A as a neuronal differentiation inducer against neuroblastoma cells. Furthermore, we synthesized a radioactive photoaffinity probe of lembehyne A and succeeded in the specific photolabeling ofa protein of Mr 30 kDa as the target protein for lembehyne A. On the other hand, multidrug resistance (MDR) in tumor cells have been recognized as one of major obstacles to successful cancer chemotherapy. Overexpression of membrane glycoprotein (e.g. P-glycoprotein, MRP1) that is believed to function as an energy-dependent efflux pump, is observed in MDR tumor cells. We started the search for substances that would reduce MDR in tumor cells and found agosterol A from a marine sponge of Spongia sp. as a reversing substance to both P-gp and MRP1-mediated MDR. Furthermore, we synthesized a radioactive photoaffinity probe of agosterol A, to try to investigate the function of MRP1.
日本生薬学会の論文
2004-12-20