Organic anion-transporting polypeptide (OATP) transporter family and drug disposition

Organic anion-transporting polypeptide (OATP) transporter family and drug disposition
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DOI:
10.1046/j.1365-2362.33.s2.5.x
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发表时间:
2003-11-01
影响因子:
5.5
通讯作者:
Kim, RB
Kim, RB
中科院分区:
医学3区
文献类型:
--
作者:
Kim, RB

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药物转运蛋白越来越被认为是药物处置的关键决定因素。最近的研究表明,药物摄取和外排转运蛋白向特定细胞膜域的靶向表达使得许多药物在临床使用中能够有效定向移动。虽然某些外排转运蛋白(例如 MDR1(P-糖蛋白))在药物处置中的作用已得到广泛研究,但新出现的证据表明,摄取转运蛋白对于药物的肠道吸收以及肾脏或肝脏消除也可能很重要。药物摄取转运蛋白有机阴离子转运多肽 (OATP) 家族的成员已被发现能够转运大量结构不同的药物。此外,OATP 同工型在胃肠道、肝脏和肾脏以及血脑屏障水平的表达对于我们了解控制药物吸收、消除和组织渗透的因素具有重要意义。
Drug transporters are increasingly recognized as a key determinant of drug disposition. Recent studies have revealed that targeted expression of drug uptake and efflux transporters to specific cell membrane domains allows for the efficient directional movement of many drugs in clinical use. While the role of certain efflux transporters such as MDR1 (P-glycoprotein) in drug disposition has been extensively studied, emerging evidence suggests that uptake transporters may also be important to the intestinal absorption and renal or hepatic elimination of drugs. Members of the organic anion-transporting polypeptide (OATP) family of drug uptake transporters have been found capable of transporting a large array of structurally divergent drugs. Moreover, expression of OATP isoforms in the gastrointestinal tract, liver and kidney, as well as at the level of the blood-brain barrier, has important implications for our understanding of the factors governing drug absorption, elimination and tissue penetration.