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It was confirmed that CD147 (Emmprin) was expressed on the cell surface of carcinoma cells. For the purpose of studying the efficacy of a CD147-targeting agent on CD147-expressing carcinoma cells, we investigated the effect of a conjugate of glutathione-doxorubicin (GSH-DXR) encapsulated in an anti-CD147 antibody-labeled liposome (aCD147ab-liposome) in terms of specific accumulation and cytotoxicity in CD147-expressing human carcinoma cells. Expression of CD147 was not observed in many normal human tissues. However, slight expression of CD147 in kidney, prostate and breast tissues was observed. By contrast, high-level expression of CD147 in all carcinoma cells such as A431, PC3 and Ishikawa cell lines was confirmed by fluorescent microscopy and Western blot analysis. Specific accumulation of the aCD147ab-liposome in the above-described CD147-expressing cells was observed. GSH-DXR encapsulated in an aCD147ab-liposome expressed specific cytotoxicity against these carcinoma cells. These results suggested that target chemotherapy of GSH-DXR encapsulated in an aCD147ab-liposome on CD147-expressing carcinoma cells was effective.

Target chemotherapy of anti-CD147 antibody-labeled liposome encapsulated GSH-DXR conjugate on CD147 highly expressed carcinoma cells