کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
9002172 | 1118576 | 2005 | 9 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Directional trans-epithelial transport of organic anions in porcine LLC-PK1 cells that co-express human OATP1B1 (OATP-C) and MRP2
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کلمات کلیدی
MDREstrone 3-sulfatePreclinical drug developmentE1SE217βGOATPMDCKDHEASMRPHBSSFBSBSA - BSADehydroepiandrosterone-sulfate - Dehydroepiandrosterone سولفاتHanks balanced salt solution - Hanks محلول نمک را تعویض می کندbovine serum albumin - آلبومین سرم گاوorganic anion transport - حمل آنیون آلیDrug transport - حمل مواد مخدرfetal bovine serum - سرم جنین گاوhemagglutinin - هماگلوتینینmultidrug resistance-associated protein - پروتئین مرتبط با مقاومت چند داروییmultidrug resistance protein - پروتئین مقاوم در برابر چندین رژیمOrganic anion transporting polypeptide - پلیپپتید حمل آنیون ارگانیک
موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
داروشناسی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Directional trans-epithelial transport of organic anions in porcine LLC-PK1 cells that co-express human OATP1B1 (OATP-C) and MRP2 Directional trans-epithelial transport of organic anions in porcine LLC-PK1 cells that co-express human OATP1B1 (OATP-C) and MRP2](/preview/png/9002172.png)
چکیده انگلیسی
The transcellular transport of many compounds, which cannot readily cross the lipid bilayer, is mediated by drug uptake and efflux transporters. Human OATP1B1 and MRP2 have been implicated in the hepato-biliary transport of many endogenous and exogenous compounds. Here, we have established epithelial porcine kidney LLC-PK1 derived cell lines, that express both transporters in a polarized fashion, as a model to predict hepato-biliary transport. Immunological identification of OATP1B1 in the recombinant cell lines was greatly facilitated by its C-terminal tagging with a peptide sequence derived from hemagglutinin (HA) avoiding the generation of OATP1B1 specific antibodies. Importantly, the tag did not interfere with the functionality of the transporter. Compared to LLC-PK1 cells and cells which expressed only OATP1B1, the cell line that co-expressed MRP2 and OATP1B1 displayed high directional basolateral-to-apical transport of 17β-estradiol-17β-glucuronide and estrone-3-sulfate. Dehydroepiandrosterone sulfate already displayed a significant basolateral-to-apical transport in the parental cell line, which was further stimulated upon expression of both transporters. Transcellular flux of all steroid conjugates in the opposite direction (apical-to-basolateral) was much lower. By employing this cellular model we were able to demonstrate for the first time that OATP1B1 together with MRP2 mediates the trans-cellular transport of rifampicin. It is anticipated that the models established herein will greatly facilitate the identification of transporters involved in the disposition of novel drug candidates.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Biochemical Pharmacology - Volume 69, Issue 3, 1 February 2005, Pages 415-423
Journal: Biochemical Pharmacology - Volume 69, Issue 3, 1 February 2005, Pages 415-423
نویسندگان
Kevin J. Spears, Jillian Ross, Alasdair Stenhouse, Clive J. Ward, Lay-Beng Goh, C. Roland Wolf, Paul Morgan, Andy Ayrton, Thomas H. Friedberg,