Inhibition of ABCG2/BCRP-mediated transport–correlation analysis of various expression systems and probe substrates
BCRP / ABCG2 is a key determinant of pharmacokinetics of substrate drugs. Several BCRP substrates and inhibitors are of low passive permeability, and the vesicular transport assay works well in this permeability space. Membranes were prepared from BCRP-HEK293, MCF-7/MX, and baculovirus-infected Sf9...
Elmentve itt :
| Szerzők: | |
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| Dokumentumtípus: | Cikk |
| Megjelent: |
2021
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| Sorozat: | EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
156 |
| doi: | 10.1016/j.ejps.2020.105593 |
| mtmt: | 31646463 |
| Online Access: | http://publicatio.bibl.u-szeged.hu/21566 |
| LEADER | 02117nab a2200289 i 4500 | ||
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| 024 | 7 | |a 10.1016/j.ejps.2020.105593 |2 doi | |
| 024 | 7 | |a 31646463 |2 mtmt | |
| 040 | |a SZTE Publicatio Repozitórium |b hun | ||
| 041 | |a zxx | ||
| 100 | 1 | |a Sáfár Zsolt | |
| 245 | 1 | 0 | |a Inhibition of ABCG2/BCRP-mediated transport–correlation analysis of various expression systems and probe substrates |h [elektronikus dokumentum] / |c Sáfár Zsolt |
| 260 | |c 2021 | ||
| 300 | |a Terjedelem: 11-Azonosító: 105593 | ||
| 490 | 0 | |a EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES |v 156 | |
| 520 | 3 | |a BCRP / ABCG2 is a key determinant of pharmacokinetics of substrate drugs. Several BCRP substrates and inhibitors are of low passive permeability, and the vesicular transport assay works well in this permeability space. Membranes were prepared from BCRP-HEK293, MCF-7/MX, and baculovirus-infected Sf9 cells with (BCRP-Sf9-HAM), and without (BCRP-Sf9) cholesterol loading. Km values for three substrates - estrone-3-sulfate, sulfasalazine, topotecan - correlated well between the four expression systems. In contrast, a 10-20-fold range in Vmax values was observed, with BCRP-HEK293 membranes possessing the largest dynamic range. IC50 values of the different test systems were similar to each other, with 94.4% of pairwise comparisons being within 3-fold. Substrate dependent inhibition showed somewhat greater variation, as 81.4% of IC50 values in the BCRP-HEK293 membranes were within 3-fold in pairwise comparisons. Overall, BCRP-HEK293 membranes demonstrated the highest activity. The IC50 values showed good concordance but substrate dependent inhibition was observed for some drugs. | |
| 700 | 0 | 1 | |a Kecskeméti Gábor |e aut |
| 700 | 0 | 1 | |a Molnár Judit |e aut |
| 700 | 0 | 1 | |a Kurunczi Anita |e aut |
| 700 | 0 | 1 | |a Szabó Zoltán |e aut |
| 700 | 0 | 1 | |a Janáky Tamás |e aut |
| 700 | 0 | 1 | |a Kis Emese |e aut |
| 700 | 0 | 1 | |a Krajcsi Péter |e aut |
| 856 | 4 | 0 | |u http://publicatio.bibl.u-szeged.hu/21566/1/10.1016j.ejps.2020.105593.pdf |z Dokumentum-elérés |