دورية أكاديمية
Novel method of measurement of in vitro drug uptake in OATP1B3 overexpressing cells in the presence of dextran.
| العنوان: | Novel method of measurement of in vitro drug uptake in OATP1B3 overexpressing cells in the presence of dextran. |
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| المؤلفون: | Kowal-Chwast A; Ryvu Therapeutics S.A., Leona Henryka Sternbacha 2, 30-394, Kraków, Poland. anna.kowal-chwast@ryvu.com.; Department of Analytical Chemistry and Biochemistry, Faculty of Materials Science and Ceramics, AGH University of Krakow, Al. Mickiewicza 30, 30-059, Kraków, Poland. anna.kowal-chwast@ryvu.com., Gabor-Worwa E; Ryvu Therapeutics S.A., Leona Henryka Sternbacha 2, 30-394, Kraków, Poland.; Department of Analytical Chemistry and Biochemistry, Faculty of Materials Science and Ceramics, AGH University of Krakow, Al. Mickiewicza 30, 30-059, Kraków, Poland., Gaud N; Ryvu Therapeutics S.A., Leona Henryka Sternbacha 2, 30-394, Kraków, Poland., Gogola D; Ryvu Therapeutics S.A., Leona Henryka Sternbacha 2, 30-394, Kraków, Poland., Piątek A; Ryvu Therapeutics S.A., Leona Henryka Sternbacha 2, 30-394, Kraków, Poland., Zarębski A; Ryvu Therapeutics S.A., Leona Henryka Sternbacha 2, 30-394, Kraków, Poland., Littlewood P; Ryvu Therapeutics S.A., Leona Henryka Sternbacha 2, 30-394, Kraków, Poland., Smoluch M; Department of Analytical Chemistry and Biochemistry, Faculty of Materials Science and Ceramics, AGH University of Krakow, Al. Mickiewicza 30, 30-059, Kraków, Poland., Brzózka K; Ryvu Therapeutics S.A., Leona Henryka Sternbacha 2, 30-394, Kraków, Poland., Kuś K; Ryvu Therapeutics S.A., Leona Henryka Sternbacha 2, 30-394, Kraków, Poland. |
| المصدر: | Pharmacological reports : PR [Pharmacol Rep] 2024 Apr; Vol. 76 (2), pp. 400-415. Date of Electronic Publication: 2024 Mar 26. |
| نوع المنشور: | Journal Article |
| اللغة: | English |
| بيانات الدورية: | Publisher: Springer International Publishing Country of Publication: Switzerland NLM ID: 101234999 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 2299-5684 (Electronic) Linking ISSN: 17341140 NLM ISO Abbreviation: Pharmacol Rep Subsets: MEDLINE |
| أسماء مطبوعة: | Publication: 2020- : Cham, Switzerland : Springer International Publishing Original Publication: Kraków, Poland : Institute of Pharmacology, Polish Academy of Sciences, c2005- |
| مواضيع طبية MeSH: | Dextrans* , Organic Anion Transporters*/genetics , Organic Anion Transporters*/metabolism, Humans ; Solute Carrier Organic Anion Transporter Family Member 1B3/genetics ; Solute Carrier Organic Anion Transporter Family Member 1B3/metabolism ; Solute Carrier Organic Anion Transporter Family Member 1B3/pharmacology ; Liver-Specific Organic Anion Transporter 1/genetics ; Liver-Specific Organic Anion Transporter 1/metabolism ; Liver-Specific Organic Anion Transporter 1/pharmacology ; HEK293 Cells ; Hepatocytes/metabolism ; Liver ; Membrane Transport Proteins/metabolism ; Albumins ; Organic Anion Transporters, Sodium-Independent/genetics ; Organic Anion Transporters, Sodium-Independent/metabolism |
| مستخلص: | Background: In predictions about hepatic clearance (CL Methods: The uptake of eight known substrates of the organic anion-transporting polypeptide 1B3 (OATP1B3) was assessed using a human embryonic kidney cell line (HEK293), which stably overexpresses this transporter. An inert polymer, dextran, was used to simulate cellular conditions, and the results were compared with experiments involving human plasma and human serum albumin (HSA). Results: This study is the first to demonstrate that dextran increases compound uptake in cells with overexpression of the OATP1B3 transporter. Contrary to the common theory that highly protein-bound ligands interact with hepatocytes to increase drug uptake, the results indicate that dextran's interaction with test compounds does not significantly increase concentrations near the cell membrane surface. Conclusions: We evaluated the effect of dextran on the uptake of known substrates using OATP1B3 overexpressed in the HEK293 cell line, and we suggest that its impact on drug concentrations in liver cells may differ from the traditional role of plasma proteins and albumin. (© 2024. The Author(s) under exclusive licence to Maj Institute of Pharmacology Polish Academy of Sciences.) |
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| فهرسة مساهمة: | Keywords: Dextran; In vitro uptake; OATP1B3 |
| المشرفين على المادة: | 0 (Dextrans) 0 (Solute Carrier Organic Anion Transporter Family Member 1B3) 0 (Liver-Specific Organic Anion Transporter 1) 0 (Organic Anion Transporters) 0 (Membrane Transport Proteins) 0 (Albumins) 0 (Organic Anion Transporters, Sodium-Independent) |
| تواريخ الأحداث: | Date Created: 20240326 Date Completed: 20240416 Latest Revision: 20240416 |
| رمز التحديث: | 20240416 |
| DOI: | 10.1007/s43440-024-00583-8 |
| PMID: | 38530582 |
| قاعدة البيانات: | MEDLINE |
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Full Text Finder | تدمد: | 2299-5684 |
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| DOI: | 10.1007/s43440-024-00583-8 |