Author/Authors :
M. L. Quan، نويسنده , , J. Wityak، نويسنده , , R. Rebolo and C. Dominguez Cerdena، نويسنده , , J. V. Duncia، نويسنده , , C. A. Kettner، نويسنده , , C. D. Ellis، نويسنده , , A. Y. Liauw، نويسنده , , J. M. Park، نويسنده , , J. B. Santella، نويسنده , , R. M. Knabb، نويسنده , , M. J. Thoolen، نويسنده , , P. C. Weber، نويسنده , , R. R. Wexler، نويسنده ,
Abstract :
Thrombin is a serine protease that plays an important role in the blood coagulation cascade, and is a target enzyme for new therapeutic agents. Ac-(D)-Phe-Pro-boroArg-OH (DuP 714) was found to be a highly effective thrombin inhibitor. In order to reduce the peptidic nature of DuP 714, we have designed a series of novel biaryl substituted alkylboronate esters as potent thrombin inhibitors. The most potent compounds have subnanomolar affinity for thrombin.
