Modulation of nuclear receptors on drug-metabolizing enzymes and transporters / 药学学报
Acta Pharmaceutica Sinica
;
(12): 1575-1581, 2012.
Artigo
em Chinês
| WPRIM
| ID: wpr-274620
ABSTRACT
PXR, CAR and PPAR, widely distributed in the body, are important members of the nuclear receptors (NRs) family. The activities and gene expressions of drug-metabolizing enzymes (DMEs) and transporters can be regulated by the activation of NRs, which effect the drug disposition. Multidrug resistance (MDR) is the leading cause of failure in cancer therapy. NRs, including PXR, CAR and PPAR, were shown to regulate the expressions of DMEs and transporters involved in the drug metabolism and clearance, suggesting that the modulation of NRs can be considered as a new target to overcome MDR. This review described the research progress of NR family members PXR, CAR, PPAR and their transcriptional activation mechanism, the regulation of DMEs and transporters by NRs, which may provide a valuable reference for clinical medication and overcome of MDR.
Texto completo:
DisponíveL
Índice:
WPRIM (Pacífico Ocidental)
Assunto principal:
Proteínas de Membrana Transportadoras
/
Receptores de Esteroides
/
Receptores Citoplasmáticos e Nucleares
/
Resistência a Múltiplos Medicamentos
/
Resistencia a Medicamentos Antineoplásicos
/
Sistema Enzimático do Citocromo P-450
/
Receptores Ativados por Proliferador de Peroxissomo
/
Metabolismo
/
Neoplasias
Limite:
Animais
/
Humanos
Idioma:
Chinês
Revista:
Acta Pharmaceutica Sinica
Ano de publicação:
2012
Tipo de documento:
Artigo
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