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35. , Lieu, H. , and Bohmaker, K. (1992) Comparative effects of receptor inactivation, 17 b-estradiol and pertussis toxin on dopaminergic inhibition of prolactin secretion in vitro. J Pharmacol Exp Ther 263, 462–9. 36. , Seeburg, P. , and Journot, L. (1993) Differential signal transduction by five splice variants of the PACAP receptor. Nature 365, 170–5. 37. Berg, K. , and Clarke, W. P. (1998) Effector pathway-dependent relative efficacy at serotonin type 2A and 2 C receptors: evidence for agonist-directed trafficking of receptor stimulus.

Ballesteros, J. , and Palczewski, K. (2006) Crystal structure of a photoactivated deprotonated intermediate of rhodopsin. Proc Natl Acad Sci U S A 103, 16123–8. 14. , Park, J. , Hildebrand, P. , Kim, Y. , Choe, H. , Hofmann, K. , and Ernst, O. P. (2008) Crystal structure of opsin in its G-protein-interacting conformation. Nature 455, 497–502. 15. K. (1995) Fluorescent labeling of purified b2 adrenergic receptor. Evidence for ligand-specific conformational changes. J Biol Chem 270, 28268–75. 16.

But only at values of a or b approaching 0 will agonist responsiveness be abolished. Probe dependence results from the fact that AMs alter the tertiary conformations available to receptor and there is no a priori reason that this “new” receptor will behave like the unmodulated receptor. , and it may be expected that the modulated receptor will exhibit different reactivity toward different probes. For example, the CCR5 AM aplaviroc inhibits the actions of both CCL3 and CCL5 and blocks the binding of CCL3, yet has minimal effect on the binding of CCL5 (119).

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New Scientist 2011-08-20 by Reed Business Info Ltd


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