Author/Authors :
Wendy B. Young، نويسنده , , Paul Sprengeler، نويسنده , , William D. Shrader، نويسنده , , Yong Li، نويسنده , , Roopa Rai، نويسنده , , Erik Verner، نويسنده , , Thomas Jenkins، نويسنده , , Paul Fatheree، نويسنده , , Aleksandr Kolesnikov، نويسنده , , James W. Janc، نويسنده , , Lynne Cregar، نويسنده , , Kyle Elrod، نويسنده , , Brad Katz، نويسنده ,
Abstract :
Inhibition of coagulation proteases such as thrombin, fXa, and fVIIa has been a focus of ongoing research to produce safe and effective antithrombotic agents. Herein, we describe a unique zinc-mediated chelation strategy to streamline the discovery of potent inhibitors of fIIa, fXa, and fVIIa. SAR studies that led to the development of selective inhibitors of fXa will also be detailed.
Keywords :
Zinc chelation , Factor Xa , factor VIIa , protease inhibitor , coagulation , thrombin
