Engineered G protein coupled receptors reveal independent regulation of internalization, desensitization and acute signaling

BMC Biology

Volumn 3, Issue , 2005, Pages

  Scearce Levie, Kimberly ^a   Lieberman, Michael D ^a   Elliott, Heather H ^a   Conklin, Bruce R ^a,b  

^a GLADSTONE INSTITUTE OF NEUROLOGICAL DISEASE   (United States)

^b UNIVERSITY OF CALIFORNIA   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ADENYLATE CYCLASE; CYCLIC AMP; G PROTEIN COUPLED RECEPTOR; KAPPA OPIATE RECEPTOR; LIGAND; MU OPIATE RECEPTOR; SPIRADOLINE; PYRROLIDINE DERIVATIVE;

ARTICLE; CARBOXY TERMINAL SEQUENCE; CELL STRAIN HEK293; CHIMERA; CONTROLLED STUDY; DESENSITIZATION; ENZYME ACTIVATION; ENZYME LINKED IMMUNOSORBENT ASSAY; GENE MUTATION; HUMAN; HUMAN CELL; IN VITRO STUDY; IN VIVO STUDY; INTERNALIZATION; LONG TERM CARE; PROTEIN ENGINEERING; PROTEIN EXPRESSION; PROTEIN PHOSPHORYLATION; SIGNAL TRANSDUCTION; AGONISTS; AMINO ACID SEQUENCE; ANTAGONISTS AND INHIBITORS; CELL LINE; COMPARATIVE STUDY; DOSE RESPONSE; DRUG EFFECTS; MOLECULAR GENETICS; PHYSIOLOGY; PROCEDURES;

AMINO ACID SEQUENCE; CELL LINE; DOSE-RESPONSE RELATIONSHIP, DRUG; HUMANS; MOLECULAR SEQUENCE DATA; PROTEIN ENGINEERING; PYRROLIDINES; RECEPTORS, G-PROTEIN-COUPLED; SIGNAL TRANSDUCTION;

EID: 27544460207     PISSN: 17417007     EISSN: 17417007     Source Type: Journal    
DOI: 10.1186/1741-7007-3-3     Document Type: Article

References (34)

1. Ferguson SSG: Evolving concepts in G protein-coupled receptor endocytosis: The role in receptor desensitization and signaling. Pharmacol Rev 2001, 53:1-24.
2. Paing MM, Stutts AB, Kohout TA, Lefkowitz RJ, Trejo J: β-arrestins regulate protease-activated receptor-I desensitization but not internalization or down-regulation. J Biol Chem 2002, 277:1292-1300.
3. Avidor-Reiss T, Nevo I, Levy R, Pfeuffer T, Vogel Z: Chronic opioid treatment induces adenylyl cyclase V superactivation. J Biol Chem 1996, 271:21309-21315.
4. Kieffer BL, Evans CJ; Opioid tolerance - In search of the holy grail. Cell 2002, 108:587-590.
5. Borgland SL, Connor M, Osborne PB, Furness JB, Christie MJ: Opioid agonists have different efficacy profiles for G protein activation, rapid desensitization, and endocytosis of mu-opioid receptors. J Biol Chem 2003, 278:18776-18784.
6. Alvarez VA, Aritamangkul S, Dang V, Salem A, Whistler JL, Von Zastrow M, Grandy DK, Williams JT: mu-Opioid receptors: Ligand-dependent activation of potassium conductance, desensitization, and internalization. J Neurosci 2002, 22:5769-5776.
7. Zimmer M, Palmer A, Kohler J, Klein R: EphB-ephrinB bi-directional endocytosis terminates adhesion allowing contact mediated repulsion. Nat Cell Biol 2003, 5:869-878.
8. Haglund K, Sigismund S, Polo S, Szymkiewicz I, Di Fiore PP, Dikic I: Multiple monoubiquitination of RTKs is sufficient for their endocytosis and degradation. Nat Cell Biol 2003, 5:461-466.
9. Nong Y, Huang YQ, Ju W, Kalia LV, Ahmadian G, Wang YT, Salter MW: Glycine binding primes NMDA receptor internalization. Nature 2003, 422:302-307.
10. Braithwaite SP, Xia H, Malenka RC: Differential roles for NSF and GRIP/ABP in AMPA receptor cycling. Proc Natl Acad Sci USA 2002, 99:7096-7101.
11. St John PA, Gordon H: Agonists cause endocytosis of nicotinic acetylcholine receptors on Cultured myotubes. J Neurobiol 2001, 49:212-223.
12. i-coupled receptor. Proc Natl Acad Sci USA 1998, 95:352-357.
13. Scearce-Levie K, Coward P, Redfern CH, Conklin BR: Engineering receptors activated solely by synthetic ligands (RASSLs). Trends Pharmacol Sci 2001, 22:414-420.
14. i-coupled receptor in transgenic mice. Nat Biotechnol 1999, 17:165-169.
15. Zhao GQ, Zhang Y, Hoon MA, Chandrashekar J, Erlenbach I, Ryba NJ, Zuker CS: The receptors for mammalian sweet and umami taste. Cell 2003, 115:255-266.
16. Capeyrou R Riond J, Corbani M, Lepage J-F, Bertin B, Emorine LJ: Agonist-induced signaling and trafficking of the μ-opioid receptor: Role of serine and threonine residues in the third cytoplasmic loop and C-terminal domain. FEBS Lett 1997, 415:200-205.
17. 375 residues within the carboxyl tail differentially regulates μ-opioid receptor internalization. J Biol Chem 2001, 276:12774-12780.
18. Pak Y, O Dowd BF, George SR: Agonist-induced desensitization of the μ-opioid receptor is determined by threonine 394 preceded by acidic amino acids in the COOH-terminal tail. J Biol Chem 1997, 272:24961-24965.
19. Schulz R, Wehmeyer A, Schulz K: Visualizing preference of G protein-coupled receptor kinase 3 for the process of κ-opioid receptor sequestration. Mol Pharmacol 2002, 61:1444-1452.
20. iα, Nature 1993, 363:274-276.
21. Petäjä-Repo UE, Hogue M, Bhalla S, Laperriere A, Morello J-P, Bouvier M: Ligands act as pharmacological chaperones and increase the efficiency of δ opioid receptor maturation. EMBO J 2002, 21:1628-1637.
22. Morello J-P, Salahpour A, Laperrière A, Bernier V, Arthus M-F, Lonergan M, Petäjä-Repo U, Angers S, Morin D, Bichet DG, Bouvier M: Pharmacological chaperones rescue cell-surface expression and function of misfolded V2 vasopressin receptor mutants. J Clin Inyest 2000, 105:887-895.
23. McLaughlin JP, Xu M, Mackie K, Chavkin C: Phosphorylation of a carboxy-terminal serine within the kappa opioid receptor produces desensitization and internalization. J Biol Chem 2003, 278:34631-34640
24. 2-adrenergic receptor delays onset of agonist-promoted desensitization. Nature 1988, 333:370-373.
25. 2-adrenergic receptor sequestration. J Biol Chem 1995, 270:24782-24789.
26. Qiu Y, Law PY, Loh HH: μ-opioid receptor desensitization: Role of receptor phosphorylation, internalization and representation. J Biol Chem 2003, 278:36733-36739.
27. Wolf R, Koch T, Schulz S, Klutzny M, Schröder H, Raulf E, Bühling F, Höllt V: Replacement of threonine 394 by alanine facilitates internalization and resensitization of the rat μ opiod receptor. Mol Pharmacol 1999, 55:263-268.
28. Finn AK, Whistler JL: Endocytosis of the mu opioid receptor reduces tolerance and a cellular hallmark of opiate withdrawal. Neuron 2001, 32:829-839.
29. Chakrabarti S, Oppermann M, Gintzler AR: Chronic morphine induces the concomitant phosphorylation and altered association of multiple signaling proteins: A novel mechanism for modulating cell signaling. Proc Natl Acad Sci USA 2001, 98:4209-4214.
30. Pitcher JA, Freedman NJ, Lefkowitz RJ: G protein-coupled receptor kinases. Annu Rev Biochem 1998, 67:653-692.
31. Watts VJ: Molecular mechanisms for heterologous sensitization of adenylate cyclase. J Pharmacol Exp Ther 2002, 302:1-7.
32. Redfern CH, Degtyarev MY, Kwa AT, Salomonis N, Cotte N, Nanevicz T, Fidelman N, Desai K, Vranizan K, Lee EK, Coward P, Shah N, Warrington JA, Fishman GI, Bernstein D, Baker AJ, Conklin BR: Conditional expression of a Gi-coupled receptor causes ventricular conduction delay and a lethal cardiomyopathy. Proc Natl Acad Sci USA 2000, 97:4826-4831.
33. Whistler JL, Enquist J, Marley A, Fong J, Gladher F, Tsuruda P, Murray SR, von Zastrow M: Modulation of postenclocytic sorting of G protein-coupled receptors. Science 2002, 297:615-620.
34. Bohn LM, Gainetdinov RR, Lin FT, Lefkowitz RJ, Caron MG: Mu-opioid receptor desensitization by beta-arrestin-2 determines morphine tolerance but not dependence. Nature 2000, 408:720-723.