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多药转运体 P-糖蛋白与抗癫痫药物耐药性。

The multidrug transporter P-glycoprotein in pharmacoresistance to antiepileptic drugs.

机构信息

Clinical Biochemistry and Metabolic Medicine Department, Central Manchester Foundation Trust, Oxford Road, M13 9WL Manchester, UK.

出版信息

Pharmacol Rep. 2012;64(5):1011-9. doi: 10.1016/s1734-1140(12)70900-3.

Abstract

This review provides an overview of the knowledge on P-glycoprotein (P-gp) and its role as a membrane transporter in drug resistance in epilepsy and drug interactions. Overexpression of P-gp, encoded by the ABCB1 gene, is involved in resistance to antiepileptic drugs (AEDs), limits gastrointestinal absorption and brain access of AEDs. Although several association studies on ABCB1 gene with drug disposition and disease susceptibility are completed to date, the data remain unclear and incongruous. Although the literature describes other multidrug resistance transporters, P-gp is the main extensively studied drug efflux transporter in epilepsy.

摘要

这篇综述概述了 P-糖蛋白(P-gp)的知识及其作为膜转运蛋白在癫痫和药物相互作用中的耐药性中的作用。ABCB1 基因编码的 P-gp 过度表达与抗癫痫药物(AEDs)的耐药性有关,限制了 AEDs 的胃肠道吸收和进入大脑。尽管迄今为止已经完成了多项关于 ABCB1 基因与药物处置和疾病易感性的关联研究,但数据仍然不清楚且不一致。尽管文献描述了其他多药耐药转运体,但 P-gp 是癫痫中研究最多的主要药物外排转运体。

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