Receptor agonist binding

Hwa, J. and Perez, D.M. (1996) The unique nature of the serine interactions for alpha 1-adrenergic receptor agonist binding and activation. The Journal of Biological Chemistry, 271, 6322-6327. 

Reeves DC, Sayed MF, Chau PL, Price KL, Lummis SC. Prediction of 5-HT(3) receptor agonist-binding residues using homology modeling. Biophys J 2003 84(4) 2338-2344. 

Madden, D. R., Abele, R., Andersson, A., and Keinanen, K. (2000). Large-scale expression and thermodynamic characterization of a glutamate receptor agonist-binding domain. Eur. J. Biochem. 267, 4281-4289. 

Page 80, figure 9.5 Biochemistry, 42 271 -283 (2003), Chiara D.C. et al. Identification of amino acids in the nicotinic acetylcholine receptor agonist binding site and ion channel photolabeled by 4-[(3-trifluo-romethyl)-3H-diazirin-3-yl]benzoylcholine, a novel pho-toaffinity antagonist. Reproduced with permission from publisher and authors. 

Studies of TP receptor agonist binding performed in other cells and tissues have revealed similar variability in regard to the presence of one or two binding affinities. Nonlinear analysis of [ I]-BOP binding to placental tissue indicated a superior fit to two affinity... 

Dopamine, and most of the known dopamine receptor agonists, binds with higher affinity to the dopamine D3 than to the dopamine D2 receptor. Due to the close homology between the dopamine D2 and D3 receptors, especially in the transmembrane domains (-80%), it is difficult to predict dopamine D2 versus dopamine D3 receptor selectivity based on receptor models. Malmberg et al.115 suggested that the observed dopamine D3 receptor selectivity may not be due to a single specific interaction but rather to a small difference in conformation between the dopamine D3 and D2 receptors. 

Several cannabinoid receptor agonists bind more or less equally well to CBi and CB2 receptors (Table 2), although they do exhibit different relative intrinsic activities at these receptors. Among these are HU-210, CP55940, lt-(-i-)-WlN55212, (-)-A -THC, anandamide and 2-arachidonoyl glycerol (reviewed in Howlett et al. 2002 Pertwee 1999a). 

Witt MR. WesthHansen SE. Rasmussen PB, Hastrup S, Nielsen M. Unsaturated free fatty acids increase benzodiazepine receptor agonist binding depending on the subunit composition of the GAB A( A) receptor complex. J Neurochem 1996 67 2141-2145. 

Molecular mechanism by which toxin-substrate G-proteins act as transducer in signaling. Fig. 1 illustrates the maimer in which the toxin-substrate G-proteins play their roles as transducer between receptors and effectors such as adenylate cyclase, phospholipase C and cation charmels. It is well known that a receptor agonist binds to its own membrane receptor with a higher affinity in the absence of GTP than in its presence. The higher affinity of binding results from association of a GDP-bound trimeric G-protein (GDP- aPy) to the receptor as shown in die upper-left part of Fig. 1. This is an inactive state of the G-protein in the sense that the protein never... 

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