论文部分内容阅读
乳腺癌耐药蛋白(BCRP)是体内重要的跨膜外排转运体,属于ATP结合盒转运体超家族,主要负责将内、外源性物质排至细胞外。BCRP体内分布广泛,胎盘、小肠、血脑屏障、肾小管等重要组织中均有表达,是介导药物-药物相互作用及临床用药个体差异的重要因素之一。本文就BCRP转运体的发现、生理功能和转运机制、底物和抑制剂以及对药物代谢动力学特征的影响等方面进行总结,以期为药物转运体BCRP与药物代谢动力学的研究提供借鉴。
Breast cancer drug resistance protein (BCRP) is an important transmembrane efflux transporter in the body and belongs to the ATP-binding cassette transporter superfamily. It is mainly responsible for excreting exogenous and extracellular substances. BCRP is widely distributed in vivo and expressed in important tissues such as the placenta, small intestine, blood-brain barrier, and renal tubules. It is one of the important factors that mediate drug-drug interactions and individual differences in clinical drug use. In this paper, we summarize the discovery of BCRP transporter, physiological functions and transport mechanisms, substrates and inhibitors, and the impact on the pharmacokinetic characteristics of BCRP in order to provide reference for the study of BCRP and pharmacokinetics.