Tamai I, Nezu J, Uchino H, Sai Y, Oku A, Shimane M, Tsuji A
Faculty of Pharmaceutical Sciences, Kanazawa University, Kanazawa, 920-0934, Japan.
Biochem Biophys Res Commun. 2000 Jun 24;273(1):251-60. doi: 10.1006/bbrc.2000.2922.
We identified three novel transporters structurally belonging to the organic anion transporting polypeptide (OATP) family in humans. Since previously known rat oatp1 to 3 do not necessarily correspond to the human OATPs in terms of either tissue distribution or function, here we designate the newly identified human OATPs as OATP-B, -D and -E, and we rename the previously known human OATP as OATP-A. OATP-C proved to be identical with the recently reported LST1/OATP-2. Expression profiles of the five OATPs and the prostaglandin transporter PGT (a member of OATP family) in human tissues showed that OATP-C is exclusively localized in liver, OATP-A and PGT are expressed in restricted ranges of tissues, and OATP-B, -D and -E show broad expression profiles. OATP-B, -C, -D and -E exhibited transport activity for [(3)H]estrone-3-sulfate as a common substrate. OATP-C has a high transport activity with broad substrate specificity.
我们在人类中鉴定出三种结构上属于有机阴离子转运多肽（OATP）家族的新型转运蛋白。由于先前已知的大鼠Oatp1至3在组织分布或功能方面不一定与人类OATP相对应，因此我们将新鉴定的人类OATP命名为OATP-B、-D和-E，并将先前已知的人类OATP重新命名为OATP-A。事实证明，OATP-C与最近报道的LST1/OATP-2相同。五种OATP和前列腺素转运蛋白PGT（OATP家族的一员）在人体组织中的表达谱表明，OATP-C仅定位于肝脏，OATP-A和PGT在有限的组织范围内表达，而OATP-B、-D和-E显示出广泛的表达谱。OATP-B、-C、-D和-E对[³H]雌酮-3-硫酸盐作为常见底物表现出转运活性。OATP-C具有高转运活性和广泛的底物特异性。
