Licensing & Royalties >> Licensing Opportunities >> Abstract Details   Mutant Nuclear Orphan Receptor for Drug Metabolism Assays Description of Invention: The constitutively active nuclear orphan receptor (CAR) activates transcription of genes encoding various drug-metabolizing enzymes, such as cytochrome P450, in response to drug exposure. While the direct activation of CAR in response to various drugs has been observed in vivo, CAR is always active in cell-based transfection assays, even in the absence of activating drugs. This constitutive activity of CAR makes it difficult to perform accurate in vitro assays to measure drug metabolism. The NIH has obtained patent protection for modified CAR proteins that can be directly activated by drugs in vitro. This technology may potentially be used in the development of more efficient and cost-effective cell-based drug metabolism assays. Applications: Development of improved in vitro assays to measure drug metabolism. Inventors: Masahiko Negishi et al. (NIEHS) Patent Status: DHHS Reference No. E-034-2002/0 -- U.S. Patent No. 7,365,160 issued 29 Apr 2008 Relevant Publication: T Sueyoshi, T Kawamoto, I Zelko, P Honkakoski, M Negishi. The repressed nuclear receptor CAR responds to phenobarbital in activating the human CYP2B6 gene. J Biol Chem. 1999 Mar 5;274(10):6043-6046. [PubMed abs] T Kawamoto, S Kakizaki, K Yoshinari, M Negishi. Estrogen activation of the nuclear orphan receptor CAR (constitutive active receptor) in induction of the mouse Cyp2b10 gene. Mol Endocrinol. 2000 Nov;14(11):1897-1905. [PubMed abs] Licensing Status: Available for exclusive and non-exclusive licensing. Portfolios: Cancer Cancer -Therapeutics-Conventional Chemotherapy Cancer -Therapeutics For Additional Information Please Contact: Tara L. Kirby Ph.D. NIH Office of Technology Transfer 6011 Executive Blvd, Suite 325 Rockville, MD 20852-3804 Phone: (301)435-4426 Email: tarak@mail.nih.gov Fax: (301)402-0220 Web Ref: 659 Last Updated On: 12/08