化学
纤溶酶
酰胺
立体化学
胰蛋白酶
尿激酶
选择性
效力
结构-活动关系
结合位点
生物化学
体外
酶
内科学
医学
催化作用
作者
Jörg Stürzebecher,H. Vieweg,Torsten Steinmetzer,Andrea Schweinitz,Milton T. Stubbs,Martin Renatus,P Wikström
标识
DOI:10.1016/s0960-894x(99)00541-7
摘要
Synthesis and anti-uPA activity of a series of Nalpha-triisopropyl-phenylsulfonyl-protected 3-amidinophenylalanine amides are described. We have explored SAR around the C-terminal amide part for inhibition of uPA, plasmin and trypsin. Modification of the amide part has been found to affect potency but not selectivity. With a Ki of 0.41 microM 2r-L is one of the most potent uPA inhibitors described so far. The X-ray crystal structure of 2r-L was solved in complex with trypsin, superimposed with uPA and the results suggest an unique binding mode of this inhibitor type.
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