Human p2 adrenergic receptor

Fig. 8.5 A comparison of A3AR models based on bovine rhodopsin, the human P2-adrenergic receptor, and the A AR as templates. On the left Extracellular side view of hAjAR models based on different templates and estimated volume of the binding pockets. On the right Representation of EL2 of each hAjAR model (in yellow hA3AR built from rhodopsin, in magenta hA.AR built from 32-AR and in cyan hA3AR built from hA AR)...

Green SA, Cole G, Jacinto M, Innis M, Liggett SB. APolymorphism of the Human P2-Adrenergic Receptor within the fourth Transmembrane Domain Alters Ligand-Binding and Functional-Properties of the Receptor. J Biol Chem 1993 268 23,116— 23,121. 

Freddolino PL, Kalani MY, Vaidehi N, et al. Predicted 3D structure for the human P2 adrenergic receptor and its binding site for agonists and antagonists. Proc Natl Acad Sci USA 2004 101 2736-2741. 

Edelberg JM, Aird WC, Rosenberg RD. Enhancement of murine cardiac chronotropy by the molecular transfer of the human P2 adrenergic receptor cDNA. J Clin Invest 1998 101 337-343. 

Turki J, Lorenz JN, Green SA, Donnelly ET, Jacinto M, Liggett SB. Myocardial signalling defects and impaired cardiac function of a human p2-adrenergic receptor polymorphism expressed in transgenic mice. Proc Natl Acad Sci USA 1996 93 10,483-10,488. 

Green S, Turki J, Innis M, Liggett SB. Amino-terminal polymorphisms of the human p2-adrenergic receptor impart distinct agonist-promoted regulatory properties. Biochemistry 1994 33 9414-9419. 

Figure 6.10 The amino add sequence of the human P2 adrenergic receptor (ExC, extracellular InC, intracellular). Membrane-spanning helices in bold, adrenaline binding sites in red, and serine phosphorylation sites in blue.

TABLE 12-6 Properties of human [5-adrenergic receptor subtypes Pi P2 P3... 

P2-adrenergic receptors may function similar to HR2 in humans [196,197]. The role of histamine and other redundant G-protein-coupled receptors in the regulation of inunune/inflammatory pathways in allergic inflammation remain to be intensely focused in future studies. 

Bristow MR, Hershberger RE, Port JD, Minobe W, Rasmussen R. pr Adrenergic and p2-adrenergic receptor-mediated adenylate-cyclase stimulation in nonfailing and failing human ventricular myocardium. MolPharmacol 1989 35 295-303. 

Chanrachakul B, Matharoo-Ball B, Turner A, et al. Reduced expression of immu-noreactive p2-adrenergic receptor protein in human myometrium with labor. J Clin Endocrinol Metab 2003 88 4997-5001. 

Bristow M, Ginsburg R, Umans V, et al. pr and p2-adrenergic-receptor subpopulations in nonfailing and failing human ventricular myocardium coupling of both receptor subtypes to muscle contraction and selective Pj -receptor down-regulation in heart failure. Circ Res 1986 59 297-309. 

Friedman J, Babu B, Clark RB. p2-Adrenergic receptor lacking the cyclic AMP-dependent protein kinase consensus sites fully activates extracellular signal-regulated kinase 1/2 in human embryonic kidney 293 cells lack of evidence for G./G switching. Mol Pharmacol 2002 62 1094-1102. 

Green SA, Turki J, Bejarano P, Hall IP, Liggett SB. Influence of p2-adrenergic receptor genotypes on signal transduction in human airway smooth muscle cells. Am J Resp Cell Mol Biol 1995 13 25-33. 

Moore PE, Laporte JD, Abraham JH, et al. Polymorphism of the p2-adrenergic receptor gene and desensitization in human airway smooth muscle. Am J Respir Crit Care Med 2000 162 2117-2124. 

Bray MS, Krushkal J, Li L, et al. Positional genomic analysis identifies the P2-adrenergic receptor gene as a susceptibility locus for human hypertension. Circulation 2000 101 2877-2882. 

Eickelberg 0, Roth M, Lorx R, et al. Ligand-independent activation of the glucocorticoid receptor by P2-adrenergic receptor agonists in primary human lung fibroblasts and vascular smooth muscle cells. J Biol Chem 1999 274 1005-1010. 

Epinephrine and norepinephrine have equal affinity for Pj-receptors, the predominant adrenergic receptors on the heart. However, the human heart also contains a small percentage of P2-receptors that, like Pj-receptors, are excitatory. Therefore, epinephrine is capable of stimulating a greater number of receptors and causing a greater stimulatory effect on the myocardium. 

Kilts JD, Gerhardt MA, Richardson MD, et al. P2-Adrenergic and several other G protein-coupled receptors in human atrial membranes activate both Gs and Gj. Circ Res 2000 87 705-709. 

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