By Gary P. Anderson (auth.), Dr. David Raeburn, Dr. Mark A. Giembycz (eds.)
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Additional resources for Airways Smooth Muscle: Neurotransmitters, Amines, Lipid Mediators and Signal Transduction
In panel B the concept of an encounter zone (rather than instantaneous collision) defines a region where G/e interactions can occur, again in a manner not constrained by the occupancy state of the receptor and during which time it is possible for the mean occupancy rate of the receptor-agonist complex to vary allowing activation of G to be related to the frequency with which the receptor is occupied by agonist. Redrawn from Stickle and Barker . Adrenaline and Noradrenaline 31 [164-166] are shown in Figure 9.
126]. subunit allowing the cycle to recommence. Point mutation studies have suggested that Cysteine 341 is important for the coupling of the active conformation of the beta 2-adrenoceptor to adenylyl cyclase via Gsa . Although this scheme is broadly supported by reconstitution experiments for both beta 1- and beta 2-adrenoceptors where putative components of the transduction system have been introduced into a test system, 28 G. P. Anderson the model is disputed and the exact mode of signal transduction via Gs has not been unequivocally demonstrated.
The model predicts: (i) strictly first order kinetics of adenylyl cyclase activation by agonist and or GTP (or its stable analogues), (ii) a linear kinetic relationship between adenylyl cyclase activation and beta-adrenoceptor concentration, (iii) a Michealean (non co-operative) dependence of the rate of adenylyl cyclase activation on agonist concentration. The model assumes instantanous collision activation of the GTP activated G-protein adenylyl cyclase complex (G jC). From Stickle and Barber 1992 .