Xenoreceptor Panel Portfolio
A collection of transporter humanized and knockout mouse models
Humanized and Knockout Mouse Models for In Vivo Applications
The ligand specificity of xenoreceptors as well as the biological consequences of their activation differs significantly between species, limiting the predictability of current animal models in studying drug-mediated activation of such receptors. In order to address this problem we have generated a variety of xenoreceptor humanized and knockout mouse models which can be used for different in vivo applications.
- In vivo induction studies
Literature examples: Nature. 2000 Jul 27; 406(6794):435-9 and J Clin Invest. 2008 Sep; 118(9):3228-39.
- Prediction of clinical drug-drug interactions
Literature examples: Drug Metab Dispos. 2007 Feb; 35(2):194-200 and Mol Pharmacol. 2011 Sep; 80(3):518-28.
- Non-genotoxic carcinogenicity testing
Literature examples: Toxicol Sci. 2008 Jan; 101(1):132-9 and Toxicol Sci. 2010 Aug; 116(2):452-66.
- Effect of receptor activation on drug toxicity
Literature examples: Drug Metab Dispos. 2009 Aug; 37(8):1611-21 and Proc Natl Acad Sci USA. 2003 May 13; 100(10):5652-7.
- Evaluation of receptors as drug targets
Literature example: J Pharmacol Exp Ther. 2010 Oct; 335(1):32-41.
- See also: Scheer N, Roland Wolf C. (2013) Xenobiotic receptor humanized mice and their utility. Drug Metab Rev. 2013 Feb; 45(1):110-21.
- Use of pure inbred C57BL/6 genetic background. This will minimize variance between mice and increase reproducibility of results.
- Use of mouse promoters and insertion of human genes into the corresponding mouse locus. Expression is therefore at endogenous levels and not restricted to the liver, but occurs in other organs where xenoreceptors are normally expressed.
- Use of large genomic inserts ensures the expression of important alternative human splice variants.
- Corresponding mouse genes are deleted in the humanized models.
- Multiple humanized models available.
- Pre-validation data available.