ATP occlusion by P-glycoprotein as a surrogate measure for drug coupling.
Biochemistry
; 47(10): 3294-307, 2008 Mar 11.
Article
en En
| MEDLINE
| ID: mdl-18275155
ABSTRACT
The multidrug efflux pump P-glycoprotein (Pgp) couples drug transport to ATP hydrolysis. Previously, using a synthetic library of tetramethylrosamine ( TMR) analogues, we observed significant variation in ATPase stimulation ( V m (D)). Concentrations required for half-maximal ATPase stimulation ( K m (D)) correlated with ATP hydrolysis transition-state stabilization and ATP occlusion (EC 50 (D)) at a single site. Herein, we characterize several TMR analogues that elicit modest turnover ( k cat
Texto completo:
1
Bases de datos:
MEDLINE
Asunto principal:
Adenosina Trifosfato
/
Miembro 1 de la Subfamilia B de Casetes de Unión a ATP
Idioma:
En
Revista:
Biochemistry
Año:
2008
Tipo del documento:
Article
País de afiliación:
Estados Unidos