Untangling ligand induced activation and desensitization of G-protein-coupled receptors

Biophysical Journal

Volumn 84, Issue 1, 2003, Pages 3-13

  Woolf, Peter J ^a,b   Linderman, Jennifer J ^a  

^a UNIVERSITY OF MICHIGAN   (United States)

^b MASSACHUSETTS INSTITUTE OF TECHNOLOGY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

BUPRENORPHINE; ENKEPHALIN[2 DEXTRO ALANINE 4 METHYLPHENYLALANINE 5 GLYCINE]; ETORPHINE; G PROTEIN COUPLED RECEPTOR; GUANINE NUCLEOTIDE BINDING PROTEIN; MORPHINE;

ARTICLE; DIFFUSION; DISSOCIATION CONSTANT; DRUG EFFICACY; DRUG MECHANISM; MONTE CARLO METHOD; PROTEIN PHOSPHORYLATION; RECEPTOR DOWN REGULATION; RECEPTOR UPREGULATION; SIGNAL TRANSDUCTION;

EID: 0037215808     PISSN: 00063495     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0006-3495(03)74828-0     Document Type: Article

References (43)

1. Balmforth, A. J., P. Warburton, and S. G. Ball. 1990. Homologous desensitization of the D1 dopamine receptor. J. Neurochem. 55:2111-2116.
2. Barak, L. S., S. S. Ferguson, J. Zhang, C. Martenson, T. Meyer, and M. G. Caron. 1997. Internal trafficking and surface mobility of a functionally intact β2-adrenergic receptor-green fluorescent protein conjugate. Mol. Pharmacol. 51:177-184.
3. Barton, A. C., and D. R. Sibley. 1990. Agonist-induced desensitization of D1-dopamine receptors linked to adenyl cyclase activity in cultured NS20Y neuroblastoma cells. Mol. Pharm. 38:531-541.
4. Benovic, J. L., C. Staniszewski, F. Mayor, Jr., M. G. Caron, and R. J. Lefkowitz. 1988. Beta-adrenergic receptor kinase. Activity of partial agonists for stimulation of adenylate cyclase correlates with ability to promote receptor phosphorylation. J. Biol. Chem. 263:3893-3897.
5. Blake, A. D., G. Bot, J. C. Freeman, and T. Reisine. 1997. Differential opioid agonist regulation of the mouse μ-opioid receptor. J. Biol. Chem. 272:782-790.
6. Blane, G. F., A. L. Boura, A. E. Fitzgerald, and R. E. Lister. 1967. Actions of etorphine hydrochloride, (M99): A potent morphine-like agent. Br. J. Pharmacol. 30:11-22.
7. Bunemann, M., K. B. Lee, R. Pals-Rylaarsdam, A. G. Roseberry, and M. M. Hosey. 1999. Desensitization of G-protein-coupled receptors in the cardiovascular system. Annu. Rev. Physiol. 61:169-192.
8. Chuang, H. H., M. Yu, Y. N. Jan, and L. Y. Jan. 1998. Evidence that the nucleotide exchange and hydrolysis cycle of G-proteins causes acute desensitization of G-protein-gated inward rectifier K+ channels. Proc. Natl. Acad. Sci. USA. 95:11727-11732.
9. Chuang, T. T., L. Iacovelli, M. Sallese, and A. De Blasi. 1996. G-protein-coupled receptors: Heterologous regulation of homologous desensitization and its implications. Trends Pharmacol. Sci. 17:416-421.
10. Evanko, D. S., M. M. Thiyagarajan, and P. B. Wedegaertner. 2000. Interaction with G-β γ is required for membrane targeting and palmitoylation of G-α(s) and G-α(q). J. Biol. Chem. 275:1327-1336.
11. Garzon, J., M. Rodriguez-Diaz, A. Lopez-Fando, and P. Sanchez-Blazquez. 2001. RGS9 proteins facilitate acute tolerance to μ-opioid effects. Eur. J. Neurosci. 13:801-811.
12. Gennis, R. B. 1989. Biomembranes: Molecular Structure and Function. Springer-Verlag, New York.
13. Jensen, A. D., F. Guamieri, S. G. Rasmussen, F. Asmar, J. A. Ballesteros, and U. Gether. 2001. Agonist-induced conformational changes at the cytoplasmic side of transmembrane segment 6 in the beta 2 adrenergic receptor mapped by site-selective fluorescent labeling. J. Biol. Chem. 276:9279-9290.
14. Jin, T., N. Zhang, Y. Long, C. A. Parent, and P. N. Devreotes. 2000. Localization of the G-protein β γ-complex in living cells during chemotaxis. Science. 287:1034-1036.
15. Kenakin, T. 2002. Drug efficacy at G-protein-coupled receptors. Annu. Rev. Pharmacol. Toxicol. 42:349-379.
16. Krupnick, J. G., and J. L. Benovic. 1998. The role of receptor kinases and arrestins in G-protein-coupled receptor regulation. Annu. Rev. Pharmacol. Toxicol. 38:289-319.
17. Lauffenburger, D. A., and J. J. Linderman. 1993. Receptors: Models for Binding, Trafficking, and Signaling. Oxford University Press, New York.
18. Lewis, M. M., V. J. Watts, C. P. Lawler, D. E. Nichols, and R. B. Mailman. 1998. Homologous desensitization of the D1A dopamine receptor: Efficacy in causing desensitization dissociates from both receptor occupancy and functional potency. J. Pharmacol. Exp. Ther. 286:345-353.
19. Ljungquist-Hoddelius, P., M. Lirvall, A. Wasteson, and K. E. Magnusson. 1991. Lateral diffusion of PDGF beta-receptors in human fibroblasts. Biosci. Rep. 11:43-52.
20. Mahama, P. A., and J. J. Linderman. 1994. A Monte Carlo study of the dynamics of G-protein activation. Biophys. J. 67:1345-1357.
21. Mahama, P. A., and J. J. Linderman. 1995. Monte Carlo simulations of membrane signal transduction events: Effect of receptor blockers on G-protein activation. Ann. Biomed. Eng. 23:299-307.
22. Neubig, R. R., and D. P. Siderovski. 2002. Regulators of G-protein signalling as new central nervous system drug targets. Nat. Rev. Drug Discov. 1:187-197.
23. Niswender, G. D., D. A. Roess, H. R. Sawyer, W. J. Silvia, and B. G. Barisas. 1985. Differences in the lateral mobility of receptors for luteinizing hormone (LH) in the luteal cell plasma membrane when occupied by ovine LH versus human chorionic gonadotropin. Endocrinology. 116:164-169.
24. Patten, M., J. Bunemann, B. Thoma, E. Kramer, M. Thoenes, S. Stube, C. Mittmann, and T. Wieland. 2002. Endotoxin induces desensitization of cardiac endothelin-1 receptor signaling by increased expression of RGS4 and RGS16. Cardiovasc. Res. 53:156-164.
25. Riccobene, T. 1999. Analysis of G-Protein-Coupled Receptor Signaling: The Relationship Between Signaling Parameters and Cellular Responses. University of Michigan, Ann Arbor.
26. Riccobene, T. A., G. M. Omann, and J. J. Linderman. 1999. Modeling activation and desensitization of G-protein-coupled receptors provides insight into ligand efficacy. J. Theor. Biol. 200:207-222.
27. Rothman, R. G., Q. Ni, and H. Xu. 1995. Buprenorphine: A review of the binding literature. In Buprenorphine: Combatting Drug Abuse With a Unique Opioid. A. Cowan, J. W. Lewis, editors. Wiley-Liss, Inc., New York. 19-23.
28. Rousseau, G., N. Guilbault, A. Da Silva, B. Mouillac, P. Chidiac, and M. Bouvier. 1997. Influence of receptor density on the patterns of β2-adrenocepter desensitization. Eur. J. Pharmacol. 326:75-84.
29. Saitoh, O., I. Masuho, I. Terakawa, S. Nomoto, T. Asano, and Y. Kubo. 2001. Regulator of G-protein signaling 8 (RGS8) requires its NH2 terminus for subcellular localization and acute desensitization of G-protein-gated K+ channels. J. Biol. Chem. 276:5052-5058.
30. Scheibe, S. D., D. B. Bennett, J. W. Spain, B. L. Roth, and C. J. Coscia. 1984. Kinetic evidence for differential agonist binding to bovine hippocampal synaptic membrane opioid receptors. J. Biol. Chem. 259:13298-13303.
31. Shea, L., and J. J. Linderman. 1997. Mechanistic model of G-protein signal transduction. Determinants of efficacy and effect of precoupled receptors. Biochem. Pharmacol. 53:519-530.
32. Shea, L. D., R. R. Neubig, and J. J. Linderman. 2000. Timing is everything - The role of kinetics in G-protein activation. Life Sci. 68:647-658.
33. Shen, K. F., and S. M. Crain. 1997. Ultra-low doses of naltrexone or etorphine increase morphine's antinociceptive potency and attenuate tolerance/dependence in mice. Brain Res. 757:176-190.
34. Silvestri, S., M. V. Seeman, J. C. Negrete, S. Houle, C. M. Shammi, G. J. Remington, S. Kapur, R. B. Zipursky, A. A. Wilson, and B. K. Christensen. 2000. Increased dopamine D2 receptor binding after long-term treatment with antipsychotics in humans: A clinical PET study. Psychopharmacology (Berl.). 152:174-180.
35. Smith, P. R., I. E. Morrison, K. M. Wilson, N. Fernandez, and R. J. Cherry. 1999. Anomalous diffusion of major histocompatibility complex class I molecules on HeLa cells determined by single particle tracking. Biophys. J. 76:3331-3344.
36. Stickle, D., and R. Barber. 1989. Evidence for the role of epinephrine binding frequency in activation of adenylate cyclase. Mol. Pharm. 36:437-445.
37. Stickle, D., and R. Barber. 1992. The encounter coupling model for β-adrenergic receptor/GTP-binding protein interaction in the S49 cell. Calculation of the encounter frequency. Biochem. Pharmacol. 43:2015-2028.
38. Strauer, B. E. 1990. Beta-blocking agents in heart failure: Modern concepts and overview. J. Cardiovasc. Pharmacol. 16(Suppl. 5):S129-S132.
39. Thomsen, W. J., and R. R. Neubig. 1989. Rapid kinetics of α 2-adrenergic inhibition of adenylate cyclase. Evidence for a distal rate-limiting step. Biochemistry. 28:8778-8786.
40. Tolkovsky, A. M. 1982. Etorphine binds to multiple opiate receptors of the caudate nucleus with equal affinity but with different kinetics. Mol. Pharm. 22:648-656.
41. Whistler, J. L., H. H. Chuang, P. Chu, L. Y. Jan, and M. von Zastrow. 1999. Functional dissociation of μ-opioid receptor signaling and endocytosis: Implications for the biology of opiate tolerance and addiction. Neuron. 23:737-746.
42. Yu, Y., L. Zhang, X. Yin, H. Sun, G. R. Uhl, and J. B. Wang. 1997. μ-opioid receptor phosphorylation, desensitization, and ligand efficacy. J. Biol. Chem. 272:28869-28874.
43. Zhang, J., S. S. G. Ferguson, L. S. Barak, S. R. Bodduluri, S. A. Laporte, P. Law, and M. G. Caron. 1998. Role for G-protein-coupled receptor kinase in agonist-specific regulation of μ-opioid receptor responsiveness. Neurobiology. 95:7157-7162.