BCRP-HAM membranes and vesicles
March 14, 2007
SOLVO Biotechnology is introducing the revolutionary BCRP HAM membranes and vesicles! SOLVO Biotechnology is introducing the revolutionary BCRP HAM membranes and vesicles! HAM = High Activity Membrane A REVOLUTIONARY PROPRIETARY TECHNOLOGY PATENTED BY SOLVO BIOTECHNOLOGY o Greater dynamic range: The BCRP-HAM assays are more robust than BCRP-M or BCRP-Sf9 assays o More suitable for screening drug-drug interactions o Excellent model for mammalian BCRP: EC50 and IC50 values obtained in mammalian system (BCRP-M) correlate well with those from BCRP-HAM There is good correlation between the ATP dependence of the BCRP (ABCG2)-mediated methotrexate transport and substrate specificity of transport inhibition studies in BCRP-Sf9 and BCRP-M vesicles (Glavinas et al. submitted). However, there was no correlation in drug-stimulated ATPase profiles of the BCRP-Sf9 system and the human BCRP-M system (Glavinas et al. submitted). The effect of cholesterol on the ABCG2 ATPase activation was studied, as insect cells harbour much less cholesterol in their membrane than human cells (Gimpl et al., 1995). Cholesterol loading led to a specific and marked improvement of the rate of drug stimulated ATPase and maximal velocity of transport for the substrates studied. Cholesterol loading of MXR-Sf9 membranes ensures that their ATPase and transport properties become similar to the MXR-M membranes that contain high levels of endogenous cholesterol. Therefore, cholesterol loaded ABCG2 overexpressing insect cell membranes are suitable models to study ABCG2 function. (Pal et al. JPET 2007 in press) Cholesterol loading mainly affected enzyme activity with relatively little effect on potencies of drugs for transporters. The cholesterol loaded BCRP-Sf9 membranes with a much improved dynamic range are the test systems of choice to study drug - ABCG2 interactions at high throughput. BCRP-HAM membranes and vesicles are available either as a product (SB-BCRP-HAM-PREDEASY ATPase Kit; SB-BCRP-HAM-Sf9-ATPase, SB-BCRP-HAM-Sf9-VT) for in house screening or as part of the PrediScreenTM solution packages conducted at the SOLVO Screening Laboratory. How to order: For North American Customers (US & Canada): XenoTech LLC http://www.xenotechllc.com/ For Customers in Japan: Nosan www.nosan.co.jp For Customers in Europe and other countries: SOLVO Biotechnology www.solvo.com Fax: +36 23 503941 Email: .(JavaScript must be enabled to view this email address)Next entry: Professor Yuichi Sugiyama joins SOLVO Scientific Advisory Board
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