Signal transduction mechanism of biased ligands at histamine H2 receptors

Biochemical Journal

Volumn 459, Issue 1, 2014, Pages 117-126

  Alonso, Natalia ^a,c   Monczor, Federico ^b,c   Echeverría, Emiliana ^b   Davio, Carlos ^b,c   Shayo, Carina ^a,c   Fernández, Natalia ^b,c  

^a INST DE BIOL Y MED EXPERIMENTAL   (Argentina)

^b UNIVERSIDAD DE BUENOS AIRES   (Argentina)

^c Facultad de Ciencias Naturales e Instituto M Lillo   (Argentina)

Author keywords

Biased agonism; G protein coupled receptor internalization (GPCR internalization); Mitogen activated protein kinase (MAPK); Pluridimensional efficacy; Seven transmembrane receptor (7TMR)

Indexed keywords

ADENYLATE CYCLASE; AMTHAMINE; CIMETIDINE; DYNAMIN; G PROTEIN COUPLED RECEPTOR KINASE 2; HISTAMINE AGONIST; HISTAMINE H2 RECEPTOR; HISTAMINE H2 RECEPTOR AGONIST; HISTAMINE H2 RECEPTOR LIGAND; LIGAND; MITOGEN ACTIVATED PROTEIN KINASE 1; MITOGEN ACTIVATED PROTEIN KINASE 3; RANITIDINE; RETINA S ANTIGEN; TIOTIDINE; UNCLASSIFIED DRUG;

ARTICLE; CARCINOMA CELL; CONTROLLED STUDY; DESENSITIZATION; DRUG CONFORMATION; DRUG EFFICACY; DRUG MECHANISM; GENETIC TRANSFECTION; HUMAN; HUMAN CELL; INTERNALIZATION; MEDIATOR; PRIORITY JOURNAL; PROTEIN FUNCTION; PROTEIN PHOSPHORYLATION; RECEPTOR DOWN REGULATION; SIGNAL TRANSDUCTION; STOMACH ADENOCARCINOMA; TUMOR CELL LINE;

CELL LINE, TUMOR; DRUG INVERSE AGONISM; HEK293 CELLS; HISTAMINE H2 ANTAGONISTS; HUMANS; LIGANDS; RANITIDINE; RECEPTORS, HISTAMINE H2; SIGNAL TRANSDUCTION;

EID: 84896110570     PISSN: 02646021     EISSN: 14708728     Source Type: Journal    
DOI: 10.1042/BJ20131226     Document Type: Article

References (44)

1. Gainetdinov, R. R., Premont, R. T., Bohn, L. M., Lefkowitz, R. J. and Caron, M. G. (2004) Desensitization of G protein-coupled receptors and neuronal functions. Annu. Rev. Neurosci. 27, 107-144 (Pubitemid 39050399)
2. Overington, J. P., Al-Lazikani, B. and Hopkins, A. L. (2006) How many drug targets are there? Nat. Rev. Drug Discov. 5, 993-996 (Pubitemid 44835126)
3. Rask-Andersen, M., Almen, M. S. and Schioth, H. B. (2011) Trends in the exploitation of novel drug targets. Nat. Rev. Drug Discov. 10, 579-590
4. Kenakin, T. P. (2012) Biased signalling and allosteric machines: new vistas and challenges for drug discovery. Br. J. Pharmacol. 165, 1659-1669
5. 2 adrenergic receptor. J. Biol. Chem. 276, 24433-24436
6. Kenakin, T. and Miller, L. J. (2010) Seven transmembrane receptors as shapeshifting proteins: the impact of allosteric modulation and functional selectivity on new drug discovery. Pharmacol. Rev. 62, 265-304
7. 2 adrenergic receptor ligands toward adenylyl cyclase and mitogen-activated protein kinase reveals the pluridimensionality of efficacy. Mol. Pharmacol. 70, 1575-1584
8. Luttrell, L. M. and Kenakin, T. P. (2011) Refining efficacy: allosterism and bias in G protein-coupled receptor signaling. Methods Mol. Biol. 756, 3-35
9. 2-adrenergic receptor. Nat. Chem. Biol. 7, 692-700
10. Andresen, B. T. (2011) A pharmacological primer of biased agonism. Endocr. Metab. Immune Disord. Drug Targets. 11, 92-98
11. Shi, C. W., Asch, S. M., Fielder, E., Gelberg, L. and Nichol, M. B. (2004) Consumer knowledge of over-the-counter phenazopyridine. Ann. Fam. Med. 2, 240-244 (Pubitemid 39318004)
12. Kaufman, D. W., Kelly, J. P., Rosenberg, L., Anderson, T. E. and Mitchell, A. A. (2002) Recent patterns of medication use in the ambulatory adult population of the United States: the Slone survey. JAMA 287, 337-344 (Pubitemid 34251967)
13. 2 receptor desensitization: involvement of a select array of G protein-coupled receptor kinases. Mol. Pharmacol. 60, 1049-1056
14. 2 histamine receptors in N-nitroso-N-methylurea (NMU)-induced carcinomas with atypical coupling to signal transducers. Biochem. Pharmacol. 50, 91-96
15. 2 receptor inverse agonist that binds with high affinity to an inactive G-protein-coupled form of the receptor: experimental support for the cubic ternary complex model. Mol. Pharmacol. 64, 512-520
16. 2 receptors. Proc. Natl. Acad. Sci. U.S.A. 93, 6802-6807
17. 2 receptor internalization. Mol. Pharmacol. 74, 1109-1118
18. Werry, T. D., Sexton, P. M. and Christopoulos, A. (2005) "Ins and outs" of seven-transmembrane receptor signalling to ERK. Trends Endocrinol. Metab. 16, 26-33 (Pubitemid 40037724)
19. Shenoy, S. K. and Lefkowitz, R. J. (2005) Seven-transmembrane receptor signaling through β-arrestin. Sci. STKE 2005, cm10
20. 2-induced hypertrophy of cardiac myocytes involves EP4 receptor-dependent activation of p42/44 MAPK and EGFR transactivation. Am. J. Physiol. Heart Circ. Physiol. 288, H2111-H2117
21. Pierce, K. L., Luttrell, L. M. and Lefkowitz, R. J. (2001) New mechanisms in heptahelical receptor signaling to mitogen activated protein kinase cascades. Oncogene 20, 1532-1539 (Pubitemid 32336840)
22. Rubio, I., Rodriguez-Viciana, P., Downward, J. and Wetzker, R. (1997) Interaction of Ras with phosphoinositide 3-kinase γ. Biochem. J. 326, 891-895
23. 1 receptor involves c-Src, protein kinase C, and ERK signaling. J. Biol. Chem. 279, 53196-53204
24. Crespo, P., Xu, N., Simonds, W. F. and Gutkind, J. S. (1994) Ras-dependent activation of MAP kinase pathway mediated by G-protein βγ subunits. Nature 369, 418-420 (Pubitemid 24184058)
25. Inglese, J., Koch, W. J., Touhara, K. and Lefkowitz, R. J. (1995) Gβγ interactions with PH domains and Ras-MAPK signaling pathways. Trends Biochem. Sci. 20, 151-156
26. Sawai, T., Hirakawa, T., Yamada, K. and Nishizawa, Y. (1999) Interaction between pleckstrin homology domains and G protein βγ-subunits: analyses of kinetic parameters by a biosensor-based method. Biol. Pharm. Bull. 22, 229-233 (Pubitemid 29171887)
27. 2 receptor and activation of extracellular signal-regulated kinases are dynamin-dependent. J. Neurochem. 107, 208-217
28. Clapham, D. E. and Neer, E. J. (1993) New roles for G-protein βγ-dimers in transmembrane signalling. Nature 365, 403-406 (Pubitemid 23311034)
29. Casey, P. J. and Gilman, A. G. (1988) G protein involvement in receptor-effector coupling. J. Biol. Chem. 263, 2577-2580 (Pubitemid 18062892)
30. Birnbaumer, L., Abramowitz, J. and Brown, A. M. (1990) Receptor-effector coupling by G proteins. Biochim. Biophys. Acta 1031, 163-224
31. Rebois, R. V., Warner, D. R. and Basi, N. S. (1997) Does subunit dissociation necessarily accompany the activation of all heterotrimeric G proteins? Cell. Signal. 9, 141-151 (Pubitemid 27186913)
32. Galandrin, S., Oligny-Longpre, G., Bonin, H., Ogawa, K., Gales, C. and Bouvier, M. (2008) Conformational rearrangements and signaling cascades involved in ligand-biased mitogen-activated protein kinase signaling through the β1-adrenergic receptor. Mol. Pharmacol. 74, 162-172 (Pubitemid 351872167)
33. Onaran, H. O. and Costa, T. (1997) Agonist efficacy and allosteric models of receptor action. Ann. N.Y. Acad. Sci. 812, 98-115 (Pubitemid 27309688)
34. Kenakin, T. and Onaran, O. (2002) The ligand paradox between affinity and efficacy: can you be there and not make a difference? Trends Pharmacol. Sci. 23, 275-280 (Pubitemid 34655733)
35. Roettger, B. F., Ghanekar, D., Rao, R., Toledo, C., Yingling, J., Pinon, D. and Miller, L. J. (1997) Antagonist-stimulated internalization of the G protein-coupled cholecystokinin receptor. Mol. Pharmacol. 51, 357-362 (Pubitemid 27118469)
36. Haribabu, B., Richardson, R. M., Fisher, I., Sozzani, S., Peiper, S. C., Horuk, R., Ali, H. and Snyderman, R. (1997) Regulation of human chemokine receptors CXCR4: role of phosphorylation in desensitization and internalization. J. Biol. Chem. 272, 28726-28731 (Pubitemid 27517830)
37. Zhang, X., Wang, F., Chen, X., Li, J., Xiang, B., Zhang, Y. Q., Li, B. M. and Ma, L. (2005) β-Arrestin1 and β-arrestin2 are differentially required for phosphorylation-dependent and -independent internalization of δ-opioid receptors. J. Neurochem. 95, 169-178 (Pubitemid 41384435)
38. Azzi, M., Charest, P. G., Angers, S., Rousseau, G., Kohout, T., Bouvier, M. and Pineyro, G. (2003) β-Arrestin-mediated activation of MAPK by inverse agonists reveals distinct active conformations for G protein-coupled receptors. Proc. Natl. Acad. Sci. U.S.A. 100, 11406-11411 (Pubitemid 37205948)
39. 2-adrenoceptor provide evidence for agonist-directed signaling. Mol. Pharmacol. 64, 1357-1369
40. Audet, N., Paquin-Gobeil, M., Landry-Paquet, O., Schiller, P. W. and Pineyro, G. (2005) Internalization and Src activity regulate the time course of ERK activation by δ opioid receptor ligands. J. Biol. Chem. 280, 7808-7816 (Pubitemid 40349675)
41. 2C receptor signaling to extracellular signal-regulated kinases 1 and 2. J. Neurochem. 93, 1603-1615
42. 2-receptor in human eosinophils and neutrophils. Biochem. Pharmacol. 84, 1174-1185
43. 2-receptor blockade by ranitidine on ulcer healing and gastric acid secretion in patients with gastric and duodenal ulcers. Eur. J. Clin. Pharmacol. 25, 195-198
44. Urban, J. D., Clarke, W. P., von Zastrow, M., Nichols, D. E., Kobilka, B., Weinstein, H., Javitch, J. A., Roth, B. L., Christopoulos, A., Sexton, P. M. et al. (2007) Functional selectivity and classical concepts of quantitative pharmacology. J. Pharmacol. Exp. Ther. 320, 1-13 (Pubitemid 46025713)