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Journal of Biomolecular Screening
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Article

Mouse Bsep ATPase Assay: A Nonradioactive Tool for Assessment of the Cholestatic Potential of Drugs

Emese Kis, Zsuzsanna Rajnai, Eniko Ioja, Krisztina Herédi Szabó, Tünde Nagy, Dóra Méhn, and Péter Krajcsi*

* To whom correspondence should be addressed. E-mail: krajcsi{at}solvo.com.


  Abstract
The mouse ortholog of the human bile salt export pump (BSEP) transporter was expressed in a baculovirus-infected insect cell (Sf9) system to study the effect of membrane cholesterol content on the transporter function. The transport activity of cholesterol-loaded mouse Bsep-HAM-Sf9 vesicles was determined in a vesicular transport assay with taurochenodeoxycholate (TCDC), a known BSEP substrate. Mouse Bsep transports TCDC at a high rate that can be sensitively detected in the ATPase assay. Cholesterol upload of the Sf9 membrane potentiates both TCDC transport and TCDC-stimulated ATPase activities. Inhibitory effect of BSEP interactors on probe substrate transport was tested in both vesicular transport and ATPase assays using cholesterol-loaded membrane vesicles. A good rank order correlation was found between IC50 values measured in TCDC-stimulated mBsep ATPase assay and in the human BSEP vesicular transport assay utilizing taurocholate (TC) as probe substrate. This upgraded form of the mouse Bsep-HAM ATPase assay is a user friendly, sensitive, nonradioactive method for early high-throughput screening of drugs with BSEP-related cholestatic potential. It may complement the human BSEP-mediated taurocholate vesicular transport inhibition assay. (Journal of Biomolecular Screening XXXX:xx-xx)

First published on November 21, 2008, doi:10.1177/1087057108326145

Journal of Biomolecular Screening 2009;14:10.

A more recent version of this article appeared on January 1, 2009

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Home page
 Drug Metab. Dispos.Home page
E. Kis, E. Ioja, T. Nagy, L. Szente, K. Heredi-Szabo, and P. Krajcsi
Effect of Membrane Cholesterol on BSEP/Bsep Activity: Species Specificity Studies for Substrates and Inhibitors
Drug Metab. Dispos., September 1, 2009; 37(9): 1878 - 1886.
[Abstract] [Full Text] [PDF]