The Effect of Albumin on MRP2 and BCRP in the Vesicular Transport Assay

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http://hdl.handle.net/10138/169142

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Deng , F , Sjöstedt , N & Kidron , H 2016 , ' The Effect of Albumin on MRP2 and BCRP in the Vesicular Transport Assay ' , PLoS One , vol. 11 , no. 10 , 0163886 . https://doi.org/10.1371/journal.pone.0163886

Title: The Effect of Albumin on MRP2 and BCRP in the Vesicular Transport Assay
Author: Deng, Feng; Sjöstedt, Noora; Kidron, Heidi
Contributor: University of Helsinki, Faculty of Pharmacy
University of Helsinki, Faculty of Pharmacy
University of Helsinki, Faculty of Pharmacy
Date: 2016-10-05
Language: eng
Number of pages: 15
Belongs to series: PLoS One
ISSN: 1932-6203
URI: http://hdl.handle.net/10138/169142
Abstract: The ABC transporters multidrug resistance associated protein 2 (MRP2) and breast cancer resistance protein (BCRP) are of interest in drug development, since they affect the pharmacokinetics of several drugs. Membrane vesicle transport assays are widely used to study interactions with these proteins. Since albumin has been found to affect the kinetics of metabolic enzymes in similar membrane preparations, we investigated whether albumin affects the kinetic parameters of efflux transport. We found that albumin increased the V-max of 5(6)-carboxy-2',7'-dichlorofluorescein (CDCF) and estradiol-17-beta-D-glucuronide uptake into MRP2 vesicles in the presence of 0.1% bovine serum albumin (BSA) by 2 and 1.5-fold, respectively, while BSA increased Lucifer yellow uptake by 30% in BCRP vesicles. K-m values increased slightly, but the change was not statistically significant. The effect of BSA on substrate uptake was dependent on the vesicle amount, while increasing BSA concentration did not significantly improve substrate uptake. These results indicate a minor effect of albumin on MRP2 and BCRP, but it should be considered if albumin is added to transporter assays for example as a solubilizer, since the effect may be substrate or transporter specific.
Subject: CANCER RESISTANCE PROTEIN
IN VIVO EXTRAPOLATION
DUBIN-JOHNSON-SYNDROME
BOVINE SERUM-ALBUMIN
K-M VALUES
DRUG CLEARANCE
FATTY-ACIDS
ABC TRANSPORTER
VITRO DATA
V-MAX
317 Pharmacy
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