Constitutively active receptor

The thrombin receptor is unusual in that the receptor is activated by the enzymatic action of thrombin which cleaves the N-terminus of the receptor leaving the receptor constitutively active. 

Jensen, A. A., Spalding, T. A., Burstein, E. S., et al. (2000) Functional importance of the Ala116-Pro136 region in the calcium-sensing receptor constitutive activity and inverse ago-nism in a family C G protein coupled receptor../. Biol. Chem. 275,29547-29555. 

Huang, P., Li, J., Visiers, I., Weinstein, H., and Liu-Chen, L.-Y. (2001) Functional role of a conserved motif in TM6 of the rat m opioid receptor constitutively active and inactive receptors result from substitutions of Thr6.34(279) with Lys and Asp. Biochemistry 40, 13501-13509. 

Rasmussen, S. G., Jensen, A. D., Liapakis, G., Ghanouni, P., Javitch, J. A., and Gether, U. (1999). Mutation of a highly conserved aspartic acid in the beta2 adrenergic receptor Constitutive activation, structural instability, and conformational rearrangement of transmembrane segment 6. Mol. Pharmacol. 56, 175-184. 

Yamamoto, Y, Moore, R., Goldsworthy, T. L., Negishi, M., and Maronpot, R. R. (2004). The orphan nuclear receptor constitutive active/androstane receptor is essential for liver tumor promotion by phenobarbital in mice. Cancer Res 64, 7197-7200. 

Phillips, J.M., Yamamoto, Y., Negishi, M., Maronpot, R.R. and Goodman, J.I. (2007) Orphan nuclear receptor constitutive active/androstane receptor-mediated alterations in DNA methylation during phenobarbital promotion of liver tumorigenesis. Toxicological Sciences, 96, 72-82. 

Tien, E.S., Matsui, K., Moore, R. and Negishi, M. (2007) The nuclear receptor constitutively active/androstane receptor regulates type 1 deiodinase and thyroid hormone activity in the regenerating mouse liver. The Journal of Pharmacology and Experimental Therapeutics, 320, 307-313. 

Keywords Adrenergic receptors G protein-coupled receptors Constitutive activity Inverse agonism Molecular dynamics... 

Schwarz, M. and Murphy, P.M. (2001) Kaposi s sarcoma-associated herpesvirus G protein-coupled receptor constitutively activates NF-kappa B and induces proinflammatory cytokine and chemokine production via a C-terminal signaling determinant. Journal of Immunology (Baltimore, Md 1950), 167, 505—513. 

Ponimaskin EG, Heine M, Joubert L, et al. The 5-hydroxytryptamine(4a) receptor is paknitoylated at two different sites, and acylation is critically involved in regulation of receptor constitutive activity. J Biol Chem. 2002 277(4) 2534r-2546. 

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