Clavatadine A, a natural product with selective recognition and irreversible inhibition of factor XIa.
J Med Chem
; 51(12): 3583-7, 2008 Jun 26.
Article
en En
| MEDLINE
| ID: mdl-18510371
ABSTRACT
Bioassay-guided fractionation of a CH2Cl2/MeOH extract of the sponge Suberea clavata using the serine protease factor XIa to detect antithrombotic activity led to the isolation of the new marine natural products, clavatadines A and B. Clavatadines A and B inhibited factor XIa with IC50's of 1.3 and 27 microM, respectively. A crystal structure of protein-inhibitor (clavatadine A) complex was obtained and revealed interesting selective binding and irreversible inhibition of factor XIa. The cocrystal structure provides guidance for the design and synthesis of future factor XIa inhibitors as antithrombotic agents.
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Fenilacetatos
/
Poríferos
/
Productos Biológicos
/
Fibrinolíticos
/
Inhibidores del Factor Xa
/
Guanidinas
Tipo de estudio:
Prognostic_studies
Límite:
Animals
Idioma:
En
Revista:
J Med Chem
Asunto de la revista:
QUIMICA
Año:
2008
Tipo del documento:
Article
País de afiliación:
Australia