Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, Lexington, Kentucky, USA.
AAPS J. 2015 May;17(3):535-45. doi: 10.1208/s12248-015-9740-x. Epub 2015 Mar 4.
The superfamily of organic anion-transporting polypeptides (OATPs, gene symbol SLCO) includes important transporters handling a variety of endogenous and xenobiotic substrates. Currently, 11 human OATPs are known and their substrates include endogenous hormones and their conjugates, anticancer drugs, and imaging agents. The contribution of OATPs to the in vivo disposition of these substrates has been extensively investigated. An accumulating body of evidence also indicates that the expression of some OATPs may be up- or downregulated in several types of cancers, suggesting potential pathogenic roles during the development and progression of cancer. Given that the role of OATPs in handling cancer therapeutics has been already covered by several excellent reviews, this review will focus on the recent progresses on the topic, in particular the role of OATPs in the disposition of anticancer drugs, the impact of OATP genetic variations on the function of OATPs, and the OATPs differentially expressed in cancer and their potential roles in cancer development, progression, and treatment.
有机阴离子转运多肽超家族(OATPs,基因符号 SLCO)包括重要的转运体,可处理多种内源性和外源性底物。目前已知有 11 种人类 OATPs,其底物包括内源性激素及其缀合物、抗癌药物和成像剂。OATPs 对这些底物在体内处置的贡献已得到广泛研究。越来越多的证据还表明,某些 OATPs 的表达在几种类型的癌症中可能会上调或下调,这表明在癌症的发生和发展过程中可能具有潜在的致病作用。鉴于 OATPs 在处理癌症治疗药物方面的作用已经被多篇优秀综述涵盖,因此本篇综述将重点介绍该主题的最新进展,特别是 OATPs 在抗癌药物处置中的作用、OATP 遗传变异对 OATPs 功能的影响,以及在癌症中差异表达的 OATPs 及其在癌症发生、发展和治疗中的潜在作用。