Zhou Yinhui, Yuan Jingjing, Li Zhisong, Wang Zhongyu, Cheng Dan, Du Yingying, Li Wenlu, Kan Quancheng, Zhang Wei
Department of Anesthesiology, Open Key Clinical Medical Experimental Laboratory Institute of Henan Province, The First Affiliated Hospital, Zhengzhou University, Zhengzhou, China.
Pharmacology. 2015;95(3-4):201-8. doi: 10.1159/000381313. Epub 2015 Apr 23.
The solute carrier organic anion-transporting polypeptides (OATPs) are a family of transporter proteins that have been extensively recognized as key determinants of absorption, distribution, metabolism and excretion of various drugs because of their broad substrate specificity and wide tissue distribution as well as the involvement of drug-drug interaction. Human OATP1A2 is a drug uptake transporter known for its broad substrate specificity, including many drugs in clinical use. OATP1A2 expression has been detected in the intestine, liver, brain and kidney. A considerable number of single nucleotide polymorphisms have been found for the OATP1A2 gene. A number of studies have shown that the cellular uptake and pharmacokinetic behavior of some drugs may be impaired in the case of certain OATP1A2 variants. Interestingly, some studies show that the mRNA expression of OATP1A2 is nearly 10-fold higher in breast cancer compared with adjacent healthy breast tissues. This review is, therefore, focused on the genetic polymorphisms, function and clinical relevance of OATP1A2 as well as on the substrates transported by it.
溶质载体有机阴离子转运多肽（OATPs）是一类转运蛋白家族，因其广泛的底物特异性、广泛的组织分布以及药物-药物相互作用的参与，已被广泛认为是各种药物吸收、分布、代谢和排泄的关键决定因素。人OATP1A2是一种药物摄取转运体，以其广泛的底物特异性而闻名，包括许多临床使用的药物。已在肠道、肝脏、大脑和肾脏中检测到OATP1A2的表达。已发现OATP1A2基因存在大量单核苷酸多态性。一些研究表明，在某些OATP1A2变体的情况下，某些药物的细胞摄取和药代动力学行为可能会受损。有趣的是，一些研究表明，与相邻的健康乳腺组织相比，乳腺癌中OATP1A2的mRNA表达几乎高10倍。因此，本综述重点关注OATP1A2的基因多态性、功能和临床相关性以及它所转运的底物。
