【作者】 张连茹； 郑忠辉； 宋思扬； 黄耀坚； 沈月毛；

【机构】 厦门大学生命科学学院；

【摘要】 <正>Hsp90在肿瘤细胞与正常细胞中表现出不同的特性,目前已成为研发抗肿瘤药物的最有潜力的靶点之一。筛选Hsp90抑制剂已成为抗肿瘤等药物研发的重要方向[1-2]。通过体外检测结合虚拟筛选等方法,发现来源于海洋真菌的抗肿瘤活性化合物(MycoE)对Hsp90的ATPase活性具有较强更多还原

【Abstract】 Hsp90 has been one of the most potent targets for screening anti tumor drug, due to its different property expressed in normal and cancer cell[1-2]. Applied Hsp90-dependent refolding of firefly luciferase testing system, fluorescence titration method, and virtual screening technology, the compound MycoE which of isolated from marine fungus HLY-2, show good inhibition for Hsp90 with IC50 value is 0.48μg/ml, compare with the known inhibitor of geldanamycin, which IC50 with 0.11μg/ml, the association constant is 7.6×106 (Fig. 1) , and the docking model show the same pattern mycoE and GA with Hsp90(Fig. 2).Above results provide the basic information about of MycoE is a potent antitumor drug by binding and inhibiting the activity of Hsp90-dependent ATPase.更多还原