Top > Research results > Joint research > World's first Golgi apparatus inhibitor, confirmation of its effect on intractable gastric cancer, Tokyo University of Science, etc.

2016/5/17

World's first Golgi apparatus inhibitor, confirmation of its effect on intractable gastric cancer, Tokyo University of Science, etc.

University Journal Online Editorial Department

　The joint research team of Eisai Co., Ltd. is Professor Isamu Shiina of the Department of Applied Chemistry, Faculty of Science, Tokyo University of Science , Succeeded in the treatment experiment of MET-positive gastric cancer known as a poor prognosis factor for advanced gastric cancer using the Gorgi body inhibitor M-COPA, and the possibility that the Gorji body inhibitor can be applied as a new anticancer agent for intractable gastric cancer. Announced that it was revealed for the first time in the world.

　Researchers have previously shown that natural mold-derived M-COPA (2-methylcoprofyrine amide) has Golgi inhibitory activity and strong anticancer activity, and succeeded in artificially synthesizing M-COPA. It was unclear what kind of cancer would be effective.

　Receptor tyrosine kinases (RTKs) such as MET are processed by the Golgi apparatus and expressed on the surface of cancer cells.The research team has now investigated the sensitivity of M-COPA to cell proliferation as it can be applied to the treatment of gastric cancer in which M-COPA overexpresses MET.As a result, it showed good sensitivity in MET-amplified gastric cancer cells, inhibited the processing of MET protein, and markedly suppressed the expression on the cell surface.Furthermore, when a MET-positive gastric cancer cell line (MKN-45) was transplanted subcutaneously into nude mice and a treatment experiment with M-COPA was performed, tumor growth was significantly suppressed.The selective anticancer effect of M-COPA was also confirmed in the refractory scirrhous gastric cancer cell line expressing FGFR2 (fibroblast growth factor receptor 2).These results show for the first time in the world that the Golgi apparatus is promising as a therapeutic target for gastric cancer that gene-amplifies RTKs such as MET and FGFR2.

　The results of this research are expected to accelerate the development of Golgi apparatus inhibitors as a new therapeutic approach for RTK-dependent cancers, which is different from tyrosine kinase inhibitors and monoclonal antibody drugs.

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