Androstane receptor ligands

B., Goodwin, B., Liddle, C. Blanchard, S. G., Willson, T.M., Collins, J.L. and Kliewer, S.A (2000) Orphan nuclear receptors constitutive androstane receptor and pregnane X receptor share xenobiotic and steroid ligands. The Journal of Biological Chemistry, 275, 15122-15127. 

Jyrkkarinne, J., Windshugel, B., Makinen, J., Ylisimio, M., Perakyla, M., Poso, A., Sippl, W. and Honkakoski, P. (2005) Amino adds important for ligand specificity of the human constitutive androstane receptor. The Journal of Biological Chemistry, 280, 5960-5971. 

Table 2 Nuclear receptors (NR) for enzyme inducers. Enzyme inducers are now known to act as ligands to nuclear receptors, leading to gene activation and increased synthesis of the enzyme. Affinity of inducers to die receptors is now known to be responsible for the differential induction potential and can explain die observed species-differences in induction. The receptors tabulated are aryl hydrocarbon receptors (AhR), constituitively androstane receptor (CAR), pregnane X receptor (PXR), and glucocorticoid receptor (GR). The isoforms in bold type are the major isoform regulated by the corresponding receptors.

Huang W, Zhang J, Wei P, Schrader WT, Moore DD. Meclizine is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for human CAR. Mol Endocrinol 2004 18 2402-8. 

PXR), the Ah receptor (AhR) and the constitutive androstane receptor (CAR) ligand binding domains from the human oestrogen receptor alpha (hERalpha) crystal structure, and the human peroxisome proliferator activated receptor alpha (PPARalpha) ligand binding domain from the human PPARgamma crystal structure. / Steroid Biochem Mol Biol 2003 84 117-32. 

Min, G., Kemper, J.K. and Kemper, B. (2002) Glucocorticoid receptorinteracting protein 1 mediates ligand-independent nuclear translocation and activation of constitutive androstane receptor in vivo. The Journal of Biological Chemistry, 277, 26356-26363. 

N., Isomoto, H., Bronk, S.F., Braley, K., Craig, R.W., Moore, D.D. and Gores, G.J. (2006) Constitutive androstane receptor (CAR) ligand, TCPOBOP, attenuates Fas-induced murine liver injury by altering Bcl-2 proteins. Hepatology, 44, 252-262. 

O., Miyazaki, N., Petrov, E.A., Batoev, V.B. and Tanabe, S. (2006) Constitutive androstane receptor (CAR) as a potential sensing biomarker of persistent organic pollutants (POPs) in aquatic mammal molecular characterization, expression level, and ligand profiling in Baikal seal (Pusa sibirica). Toxicological Sciences, 94, 57-70. 

Dussault, I., Lin, M., Hollister, K., Fan, M., Termini, J., Sherman, M. A., and Forman, B. M. (2002) A structural model of the constitutive androstane receptor defines novel interactions that mediate ligand-independent activity. Mol. Cell. Biol. 22 (15), 5270-5280. 

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