Receptor-effector coupling

Receptors are proteins that bind specific hormones and generate an intracellular signal (receptor-effector coupling). 

Lawrence, D.M., Joseph, D.B., and Bidlack, J.M., Kappa opioid receptors expressed on three related thymoma cell lines Differences in receptor-effector coupling, Biochem. Pharmacol., 49, 81, 1995... 

Couve, A., Thomas, P, Calver, A. R., et al. (2002) Cyclic AMP-dependent protein kinase phosphorylation facilitates GABAb receptor-effector coupling. Nat. Neurosci. 25,25. 

Birnbaumer L, Abramowitz J, Brown AM. 1990. Receptor-effector coupling by G proteins. Biochim Biophys Acta 1031 163-224. 

In the dorsal raphe nucleus GR agonists cause a reduction in the functional activity of 5-HTia auto receptor mediated inhibition of cell firing (Laaris et ah, 1995), an effect likely to be on receptor-effector coupling since there is no change in the number of 5-HTia receptors (Laaris et al, 1995). In vivo models of somatodendritic 5-HTia function, such as hypothermia in mice, are attenuated by corticosterone administration (McAllister-Williams et al., 2001), in agreement with this electrophysiological data. 

Durand IH, Green RD (2001) Cloning of a chick A3 adenosine receptor characterization of ligand binding and receptor-effector coupling of chick A1 and A adenosine receptors. Naunyn Schmiedebergs Arch Pharmacol 363(1) 81—89... 

Berg KA, Cropper JD, Niswender CM, Sanders-Bush E, Emeson RB, Clarke WP. RNA-editing of the 5-HT(2C) receptor alters agonist-receptor-effector coupling specificity. Br J Pharmacol 2001 134 386-392. 

Liu YF, Jakobs KH, Rasenick MM, Albert PR. G protein specificity in receptor-effector coupling. Analysis of the roles of G0 and Gi2 in GH4C1 pituitary cells. J Biol Chem 1994 269 13,880-13,886. 

Spiegel AM, Shenker A, Weinstein LS. 1992. Receptor-effector coupling by G-proteins implications for normal and abnormal signal transduction. Endocrinol Rev 13 536-565. 

D Angelo DD, Eubank JJ, Davis MG, Dom II GW. Mutagenic analysis of platelet thromboxane receptor cysteines. Roles in ligand binding and receptor-effector coupling. JBiol Chem 1996 271 6233-40... 

Casey PJ, Gilman AG (1988) G protein involvement in receptor-effector coupling. In J. Biol. Chem. 263 2577-2580. 

It is important to point out that a selective response in vivo does not always reflect selectivity at the receptor level but may depend on organ selectivity. This is particularly true for partial agonists of low intrinsic efficacy, which may exhibit receptor-selective activity in a tissue containing a large receptor pool or may operate the receptor-effector coupling system more efficiently. 

Liapakis G, Tallent M, Reisine T (1996c) Molecular and functional properties of somatostatin receptor subtypes. Metabolism 1 12-13 Libert F, Parmentier M, Lefort A, Dinsart C, Wan Sande J, Maenhaut C, Simons M-J, DuMont JE, Vassart G (1989) Selective amplification and cloning of four new members of the G protein-coupled receptor family. Science 244 569-572 Liu YF, Jakobs KH, Rasenick MM, Albert PR (1994) G protein specificity in receptor-effector coupling. Analysis of the roles of Go and Giz in GH4C1 pituitary cells. J Biol Chem 269 13880-13886... 

Measurements of the mobility of membrane-associated components, particularly those associating with the cytoplasmic side of the lipid bilayer and positioned to interact with the intracellular domain of the receptor, are few (Bruckert et al., 1992 Kwon and Neubig, 1992 Kwon, 1992). Measurements of the diffusivity of membrane-associated effectors (see Fig. 2), for example, will be important in determining the role of diffusion in receptor/effector coupling and signal transduction. 

Escin and a-toxin have attracted a lot of interest since permeabilization with either one of them appears not to interfere with the receptor effector coupling. This allows the study of the intracellular signaling cascades involved in pharmacomechanical coupling. (3-Escin is a saponin ester and a-toxin is a bacterial toxin from Staphylococcus aureus. They differ by the size of fhe holes they produce in the plasma membrane. 

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