Enhanced protein C activation and inhibition of fibrinogen cleavage by a thrombin modulator.
Science
; 273(5280): 1389-91, 1996 Sep 06.
Article
en En
| MEDLINE
| ID: mdl-8703074
A modulator of the enzymatic activity of human thrombin, designated LY254603, was identified that enhances the thrombin-catalyzed generation of the anticoagulant factor activated protein C, yet inhibits thrombin-dependent fibrinogen clotting. By means of mutant substrates, it was shown that LY254603 mediates the change in enzymatic substrate specificity through an alteration in thrombin's S3 substrate recognition site, a mechanism that appeared to be independent of allosteric changes induced by either sodium ions or by thrombomodulin. This compound may represent the prototype of a class of agents that specifically modulates the balance between thrombin's procoagulant and anticoagulant functions.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Éteres Fenílicos
/
Fibrinógeno
/
Proteína C
/
Trombina
/
Naftalenos
Tipo de estudio:
Prognostic_studies
Límite:
Humans
Idioma:
En
Revista:
Science
Año:
1996
Tipo del documento:
Article
País de afiliación:
Estados Unidos
Pais de publicación:
Estados Unidos