血脑屏障上有机阴离子转运多肽的表达、分子调控及其介导的药物转运

Expression,molecular regulation and medidated drug transport of organic anion transport polypeptides at blood brain barrier

血脑屏障(BBB)在很大程度上限制了药物进入中枢神经系统(CNS),使得各种脑部疾病的治疗效果不佳甚至无效,因此开发有效的跨脑屏障药物传递技术成为了CNS疾病治疗的研究热点。已知有机阴离子转运多肽(人类:OATPs;啮齿类动物:Oatps)在BBB中高表达,并且可参与各种内源性物质和外源性药物的细胞摄取过程,因此OATPs/Oatps家族成员有很大的潜力可用于改善治疗药物进入大脑的过程。本文主要总结了OATPs/Oatps在BBB中的定位、功能表达、分子调控及其介导的药物转运过程,以期为改善CNS疾病的药物治疗效果提供理论依据。

The blood brain barrier(BBB)largely limits the entry of drugs into the central nervous system(CNS),which weakens the treatment of various brain diseases or even makes it ineffective.Therefore,the development of effective drug delivery technology across the BBB has become a research hotspot in the treatment of CNS diseases.It is known that organic anion transport polypeptides(Human:Oatps;Rodent:Oatps)are highly expressed in the BBB and participate in the cellular uptake of various endogenous substances and exogenous drugs.So OATPs/Oatps family members have great potential to improve the way therapeutic drugs enter the BBB.This paper mainly summarized the localization,functional expression and molecular regulation of OATPs/Oatps at the BBB,and drug transport mediated by it to provide a theoretical basis to improve the therapeutic effect of CNS diseases.