The use of the LanthaScreen TR-FRET CAR coactivator assay in the characterization of constitutive androstane receptor (CAR) inverse agonists

Sensors (Switzerland)

Volumn 15, Issue 4, 2015, Pages 9265-9276

  Carazo, Alejandro ^a   Pávek, Petr ^a  

^a CHARLES UNIVERSITY   (Czech Republic)

Author keywords

Constitutive androstane receptor; Pharmacodynamics interactions; Terbium; TR FRET

Indexed keywords

CELL SIGNALING; MOBILE SECURITY; PHARMACODYNAMICS; TERBIUM;

CELLULAR MODEL; COACTIVATORS; CONSTITUTIVE ANDROSTANE RECEPTORS; INVERSE AGONISTS; LIGAND BINDING DOMAIN; NUCLEAR RECEPTORS; RELIABLE METHODS; TR-FRET;

LIGANDS;

EID: 84928152183     PISSN: 14248220     EISSN: None     Source Type: Journal    
DOI: 10.3390/s150409265     Document Type: Article

References (18)

1. Carazo Fernandez, A.; Smutny, T.; Hyrsova, L.; Berka, K.; Pavek, P. Chrysin, baicalein and galangin are indirect activators of the human constitutive androstane receptor (CAR). Toxicol. Lett. 2015, 233, 68-77.
2. Chai, X.; Zeng, S.; Xie, W. Nuclear receptors PXR and CAR: Implications for drug metabolism regulation, pharmacogenomics and beyond. Expert Opin. Drug Metab. Toxicol. 2013, 9, 253-266.
3. Jiang, M.; Xie, W. Role of the constitutive androstane receptor in obesity and type 2 diabetes: A case study of the endobiotic function of a xenobiotic receptor. Drug Metab. Rev. 2013, 45, 156-163.
4. Wada, T.; Gao, J.; Xie, W. PXR and CAR in energy metabolism. Trends Endocr. Metab. 2009, 20, 273-279.
5. Ingraham, H.A.; Redinbo, M.R. Orphan nuclear receptors adopted by crystallography. Curr. Opin. Struct. Biol. 2005, 15, 708-715.
6. Osabe, M.; Negishi, M. Active ERK1/2 protein interacts with the phosphorylated nuclear constitutive active/androstane receptor (CAR; NR1I3), repressing dephosphorylation and sequestering CAR in the cytoplasm. J. Biol. Chem. 2011, 286, 35763-35769.
7. Mutoh, S.; Sobhany, M.; Moore, R.; Perera, L.; Pedersen, L.; Sueyoshi, T.; Negishi, M. Phenobarbital indirectly activates the constitutive active androstane receptor (CAR) by inhibition of epidermal growth factor receptor signaling. Sci. Signal. 2013, 6, ra31.
8. Yang, H.; Wang, H. Signaling control of the constitutive androstane receptor (CAR). Protein Cell 2014, 5, 113-123.
9. Maglich, J.M.; Parks, D.J.; Moore, L.B.; Collins, J.L.; Goodwin, B.; Billin, A.N.; Stoltz, C.A.; Kliewer, S.A.; Lambert, M.H.; Willson, T.M.; Moore, J.T. Identification of a novel human constitutive androstane receptor (CAR) agonist and its use in the identification of CAR target genes. J. Biol. Chem. 2003, 278, 17277-17283.
10. Moore, L.B.; Parks, D.J.; Jones, S.A.; Bledsoe, R.K.; Consler, T.G.; Stimmel, J.B.; Goodwin, B.; Liddle, C.; Blanchard, S.G.; Willson, T.M.; Collins, J.L.; Kliewer, S.A. Orphan nuclear receptors constitutive androstane receptor and pregnane X receptor share xenobiotic and steroid ligands. J. Biol. Chem. 2000, 275, 15122-15127.
11. Li, L.; Chen, T.; Stanton, J.D.; Sueyoshi, T.; Negishi, M.; Wang, H. The peripheral benzodiazepine receptor ligand 1-(2-chlorophenyl-methylpropyl)-3-isoquinoline-carboxamide is a novel antagonist of human constitutive androstane receptor. Mol. Pharmacol. 2008, 74, 443-453.
12. Forman, B.M.; Tzameli, I.; Choi, H.S.; Chen, J.; Simha, D.; Seol, W.; Evans, R.M.; Moore, D.D. Androstane metabolites bind to and deactivate the nuclear receptor CAR-beta. Nature 1998, 395, 612-615.
13. Manufacturer's Manual, Invitrogen, Assay Pharmacology. Lantha Screen™ TR-FRET Constitutive Androstane Receptor Coactivator Assay Manual; Invitrogen Corporation: Carlsbad, CA, USA, 2007.
14. Kupcho, K.R.; Stafslien, D.K.; De Rosier, T.; Hallis, T.M.; Ozers, M.S.; Vogel, K.W. Simultaneous monitoring of discrete binding events using dual-acceptor terbium-based LRET. J. Am. Chem. Soc. 2007, 129, 13372-13373.
15. Zhang, J.H.; Chung, T.D.; Oldenburg, K.R. A Simple Statistical Parameter for Use in Evaluation and Validation of High Throughput Screening Assays. J. Biomol. Screen. 1999, 4, 67-73.
16. Kenakin, T.; Williams, M. Defining and characterizing drug/compound function. Biochem. Pharmacol. 2014, 87, 40-63.
17. Parks, D.J.; Blanchard, S.G.; Bledsoe, R.K.; Chandra, G.; Consler, T.G.; Kliewer, S.A.; Stimmel, J.B.; Willson, T.M.; Zavacki, A.M.; Moore, D.D.; et al. Bile acids: Natural ligands for an orphan nuclear receptor. Science 1999, 284, 1365-1368.
18. Collins, J.L.; Parks, D.J. Constitutive Androstane Receptor. Patent WO 2001071361 A2, 2001.