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Generation of potent coagulation protease inhibitors utilizing zinc-mediated chelation |
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| Authors: | Young Wendy B Sprengeler Paul Shrader William D Li Yong Rai Roopa Verner Erik Jenkins Thomas Fatheree Paul Kolesnikov Aleksandr Janc James W Cregar Lynne Elrod Kyle Katz Brad |
| Affiliation: | Celera, 180 Kimball Way, South San Francisco, CA 94080, USA. Wendy.Young@Celera.com |
| 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. |
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