Application of bosutinib as enzyme inhibitor of ASPH

作者: Shen Feng , Wang Haibo

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摘要: The invention discloses application of bosutinib as an enzyme inhibitor aspartate beta-hydroxylase (ASPH). can be used for preparing drugs treatment diseases associated with ASPH overexpression. are cancer, liver fibrosis and cirrhosis. cancer includes hepatoma, intrahepatic cholangiocarcinoma, glioblastoma, small cell lung colon pancreatic cancer. A compound capable being bound to the activity structural domain is obtained by virtual screening protein three-dimensional structure, that is, bosutinib. inhibit enzymatic activity, inhibition rate 78.1% at 100 [mu]M. restrain proliferation HepG2, Hep3B Huh7 hepatoma carcinoma cells, IC50values 6.98 [mu]M, 9.52 [mu]M 13.13 respectively.

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