Development of a Selective Peptide Macrocycle Inhibitor of Coagulation Factor XII toward the Generation of a Safe Antithrombotic Therapy.


Autoria(s): Baeriswyl V.; Calzavarini S.; Gerschheimer C.; Diderich P.; Angelillo-Scherrer A.; Heinis C.
Data(s)

2013

Resumo

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.

Identificador

http://serval.unil.ch/?id=serval:BIB_73BC92D2A3DA

isbn:1520-4804 (Electronic)

pmid:23586812

doi:10.1021/jm400236j

isiid:000318892500028

Idioma(s)

en

Fonte

Journal of Medicinal Chemistry, vol. 56, no. 9, pp. 3742-3746

Tipo

info:eu-repo/semantics/article

article