Recent advance in the mechanism study of polymeric inhibitors of P-glycoprotein / 药学学报
Acta Pharmaceutica Sinica
; (12): 1224-1231, 2010.
Article
en Zh
| WPRIM
| ID: wpr-354523
Biblioteca responsable:
WPRO
ABSTRACT
P-glycoprotein (P-gp) is an ATP-dependent multidrug efflux pump that acts as a major obstacle for oral drug delivery and cancer therapy. Recent reports have provided evidence that excipients often used in pharmaceutical formulations, such as Pluronic and TPGS, also have inhibitory effects on P-glycoprotein. Because inhibition of efflux transporters by polymeric inhibitors may dramatically increase the bioavailability of P-gp substrates with negligible side effects, identification of the mechanism and their structure activity relationship is therefore of significant importance for pharmaceutical development. Other than competitive inhibition for traditional inhibitors, polymeric inhibitors may modify P-gp function through alterations on membrane fluidity, inhibition of P-gp ATPase, depletion of intracellular ATP and down-regulating of P-gp expression. In the present review, the inhibition mechanism of potential polymeric inhibitors and their structure activity relationship will be discussed along with a brief introduction to the established methodologies.
Texto completo:
1
Base de datos:
WPRIM
Asunto principal:
Farmacología
/
Polímeros
/
Relación Estructura-Actividad
/
Disponibilidad Biológica
/
Expresión Génica
/
Adenosina Trifosfato
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Química
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Adenosina Trifosfatasas
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Miembro 1 de la Subfamilia B de Casetes de Unión a ATP
/
Excipientes
Límite:
Animals
/
Humans
Idioma:
Zh
Revista:
Acta Pharmaceutica Sinica
Año:
2010
Tipo del documento:
Article