Development of a selective peptide macrocycle inhibitor of coagulation factor XII toward the generation of a safe antithrombotic therapy
Baeriswyl, Vanessa; Calzavarini, Sara; Gerschheimer, Christiane; Diderich, Philippe; Angelillo-Scherrer, Anne; Heinis, Christian
2013

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.

Details

Title Development of a selective peptide macrocycle inhibitor of coagulation factor XII toward the generation of a safe antithrombotic therapy
Author(s) Baeriswyl, Vanessa ; Calzavarini, Sara ; Gerschheimer, Christiane ; Diderich, Philippe ; Angelillo-Scherrer, Anne ; Heinis, Christian
Published in Journal of medicinal chemistry
Volume 56
Issue 9
Pages 3742-3746
Date 2013
ISSN 1520-4804
Keywords
DOI https://doi.org/10.1021/jm400236j
Other identifier(s) View record in Web of Science
Laboratories LPPT
Record Appears in Scientific production and competences > SB - School of Basic Sciences > ISIC - Institute of Chemical Sciences and Engineering > LPPT - Laboratory of Therapeutic Proteins and Peptides
Work produced at EPFL
Journal Articles
Published
Record creation date 2013-10-15

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