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J Med Chem. 2013 May 9;56(9):3742-6. doi: 10.1021/jm400236j. Epub 2013 Apr 25.

Development of a selective peptide macrocycle inhibitor of coagulation factor XII toward the generation of a safe antithrombotic therapy.

Author information

1
Institute of Chemical Sciences and Engineering, Ecole Polytechnique Fédérale de Lausanne EPFL, CH-1015 Lausanne, Switzerland.

Abstract

Inhibition of coagulation factor XII (FXII) activity represents an attractive approach for the treatment and prevention of thrombotic diseases. The few existing FXII inhibitors suffer from low selectivity. Using phage display combined to rational design, we developed a potent inhibitor of FXII with more than 100-fold selectivity over related proteases. The highly selective peptide macrocycle is a promising candidate for the control of FXII activity in antithrombotic therapy and a valuable tool in hematology research.

PMID:
23586812
DOI:
10.1021/jm400236j
[Indexed for MEDLINE]

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