Taconic and CXR Biosciences Ltd are pleased to announce the publication of two manuscripts describing novel mouse lines humanized for the important drug metabolising enzyme CYP2C9 and the efflux transporter MRP2.
Publication in the prestigious journals Molecular Pharmacology and Drug Metabolism & Disposition provides further confirmation of the enthusiasm in academia and industry for more predictive preclinical models, and demonstrates how these models can be used to better predict drug exposure, distribution, metabolism and safety in humans.
The papers describe for the first time the generation of viable and fertile Cyp2c cluster knockout and humanized CYP2C9 and MRP2 mouse models. It is demonstrated that the human proteins are functionally active in these mice and the use of the models for assessing the role of CYP2C9 and MRP2 in human drug disposition and drug-drug interactions are presented.
The humanized CYP2C9 and MRP2 mice are available as part of a larger program of humanized and knockout models for xenoreceptors, drug metabolising enzymes and drug transporters. As for all of the humanized models, the corresponding murine genes have been replaced with their human counterparts. Humanized and knockout mice are now available for many of the key genes involved in drug metabolism — such as PXR, CAR, AHR, CYP3A4, CYP2D6, MDR1 and OATP1B1 & 1B3.
References:
Generation and Characterization of Novel Cytochrome P450 Cyp2c Gene Cluster Knockout and CYP2C9 Humanized Mouse Lines. Scheer N, Kapelyukh Y, Chatham L, Rode A, Buechel S, Wolf CR. Mol Pharmacol. 2012 Aug 23; doi:10.1124/mol.112.080036.
Generation and Characterization of a Novel MRP2 Humanized Mouse Line. Scheer N, Balimane P, Hayward MD, Buechel S, Kauselmann G, Wolf CR. Drug Metab Dispos. 2012 Aug 23. doi:10.1124/dmd.112.047605.
About CXRCXR Biosciences Ltd. is commercializing innovative approaches to transform the drug development and chemical safety assessment process. As well as introducing new technology platforms, CXR also helps customers to take their candidate compounds through development efficiently, or to resolve problems that have been encountered, through the provision of customized solutions. The company has business relationships with many of the world’s leading pharmaceutical companies, chemical companies, biotechnology companies, universities and research institutions. CXR Biosciences Ltd. is located in Dundee, Scotland. More information can be found at www.cxrbiosciences.com.
About TaconicTaconic is a leading provider of life sciences solutions to researchers worldwide, offering innovative laboratory mice and rats and scientific services that facilitate in vivo studies and advance drug discovery. Taconic’s wide range of advanced solutions include custom genetically engineered model design, generation and production, imaging, off-the-shelf model repositories, contract research, custom breeding, genetic monitoring and health testing. Headquartered in New York’s Hudson River Valley, Taconic operates seven breeding facilities and three service laboratories in the U.S. and Europe and maintains a staff of over 1,000 scientific specialists committed to technological innovation. Additional information about Taconic is available at www.taconic.com.
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