In vitro pharmacological characterization of RXFP3 allosterism: An example of probe dependency

PLoS ONE

Volumn 7, Issue 2, 2012, Pages

  Alvarez Jaimes, Lily ^a   Sutton, Steven W ^a   Nepomuceno, Diane ^a   Motley, S Timothy ^a   Cik, Miroslav ^a   Stocking, Emily ^a   Shoblock, James ^a   Bonaventure, Pascal ^a  

^a JOHNSON AND JOHNSON PHARMACEUTICAL RESEARCH AND DEVELOPMENT   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

3 [3,5 BIS(TRIFLUOROMETHYL)PHENYL] 1 (3,4 DICHLOROBENZYL) 1 [2 (5 METHOXY 1H INDOL 3 YL)ETHYL]UREA; CYCLIC AMP; G PROTEIN COUPLED RECEPTOR; IODINE 125; RADIOLIGAND; RECOMBINANT RELAXIN; RELAXIN 3; RELAXIN 3 B CHAIN; RELAXIN 3 RECEPTOR AGONIST; RXFP3 RECEPTOR; RXFP4 RECEPTOR; UNCLASSIFIED DRUG; RELAXIN; RLN3 PROTEIN, HUMAN; RXFP3 PROTEIN, HUMAN;

ALLOSTERISM; ARTICLE; CALCIUM MOBILIZATION; CELL LINE; CONCENTRATION (PARAMETERS); CONTROLLED STUDY; DRUG ACTIVITY; DRUG STRUCTURE; DRUG SYNTHESIS; HUMAN; HUMAN CELL; IC 50; IN VITRO STUDY; MEDIAN EFFECTIVE CONCENTRATION; MOLECULAR CLONING; MOLECULAR PROBE; PROTEIN FUNCTION; BINDING SITE; CALCIUM SIGNALING; CHEMISTRY; METABOLISM;

ALLOSTERIC REGULATION; ALLOSTERIC SITE; CALCIUM SIGNALING; CELL LINE; CYCLIC AMP; HUMANS; MOLECULAR PROBES; RECEPTORS, G-PROTEIN-COUPLED; RELAXIN;

EID: 84856690544     PISSN: None     EISSN: 19326203     Source Type: Journal    
DOI: 10.1371/journal.pone.0030792     Document Type: Article

References (49)

1. Liu C, Eriste E, Sutton S, Chen J, Roland B, et al. (2003) Identification of Relaxin-3/INSL7 as an Endogenous Ligand for the Orphan G-protein-coupled Receptor GPCR135. Journal of Biological Chemistry 278: 50754-50764.
2. Boels K, Hermans-Borgmeyer I, Schaller HC, (2004) Identification of a mouse orthologue of the G-protein-coupled receptor SALPR and its expression in adult mouse brain and during development. Dev Brain Res 152: 265-268.
3. Bathgate RA, Ivell R, Sanborn BM, Sherwood OD, Summers RJ, (2006) International union of pharmacology LVII: recommendations for the nomenclature of receptors for relaxin family peptides. Pharmacological Reviews 58: 7-31.
4. Sutton SW, Bonaventure P, Kuei C, Roland B, Chen J, et al. (2004) Distribution of G-Protein-Coupled Receptor (GPCR)135 Binding Sites and Receptor mRNA in the Rat Brain Suggests a Role for Relaxin-3 in Neuroendocrine and Sensory Processing. Neuroendocrinology 80: 298-307.
5. Ma S, Sang Q, Lanciego JL, Gundlach AL, (2009) Localization of relaxin-3 in brain of Macaca fascicularis: identification of a nucleus incertus in primate. J Comp Neurol 517: 856-872.
6. Smith CM, Shen PJ, Banerjee A, Bonaventure P, Ma S, et al. (2010) Distribution of relaxin-3 and RXFP3 within arousal, stress, affective, and cognitive circuits of mouse brain. J Comp Neurol 518: 4016-4045.
7. Liu C, Kuei C, Sutton S, Chen J, Bonaventure P, et al. (2005) INSL5 is a high affinity specific agonist for GPCR142 (GPR100). Journal of Biological Chemistry 280: 292-300.
8. Chen J, Kuei C, Sutton SW, Bonaventure P, Nepomuceno D, et al. (2005) Pharmacological characterization of relaxin-3/INSL7 receptors GPCR135 and GPCR142 from different mammalian species. Journal of Pharmacology and Experimental Therapeutics 312: 83-95.
9. Sutton SW, Bonaventure P, Kuei C, Nepomuceno D, Wu J, et al. (2005) G-Protein-Coupled Receptor (GPCR)-142 Does Not Contribute to Relaxin-3 Binding in the Mouse Brain: Further Support that Relaxin-3 Is the Physiological Ligand for GPCR135. Neuroendocrinology 82: 139-150.
10. Hsu Sheau Y, Nakabayashi K, Nishi S, Kumagai J, Kudo M, et al. (2002) Activation of orphan receptors by the hormone relaxin. Science 295: 671-674.
11. Sherwood OD, (2004) Relaxin's physiological roles and other diverse actions. Endocr Rev 25: 205-234.
12. Royce SG, Miao YR, Lee M, Samuel CS, Tregear GW, et al. (2009) Relaxin reverses airway remodeling and airway dysfunction in allergic airways disease. Endocrinology 150: 2692-2699.
13. Dschietzig T, Teichman S, Unemori E, Wood S, Boehmer J, et al. (2009) Intravenous recombinant human relaxin in compensated heart failure: a safety, tolerability, and pharmacodynamic trial. J Card Fail 15: 182-190.
14. Bathgate RAD, Samuel CS, Burazin TCD, Layfield S, Claasz AA, et al. (2002) Human relaxin gene 3 (H3) and the equivalent mouse relaxin (M3) gene: novel members of the relaxin peptide family. Journal of Biological Chemistry 277: 1148-1157.
15. Banerjee A, Shen PJ, Ma S, Bathgate RA, Gundlach AL, (2010) Swim stress excitation of nucleus incertus and rapid induction of relaxin-3 expression via CRF1 activation. Neuropharmacology 58: 145-155.
16. Ma S, Olucha-Bordonau FE, Hossain MA, Lin F, Kuei C, et al. (2009) Modulation of hippocampal theta oscillations and spatial memory by relaxin-3 neurons of the nucleus incertus. Learn Mem 16: 730-742.
17. Hida T, Takahashi E, Shikata K, Hirohashi T, Sawai T, et al. (2006) Chronic intracerebroventricular administration of Relaxin-3 increases body weight in rats. Journal of Receptors and Signal Transduction 26: 147-158.
18. McGowan BM, Stanley SA, Ghatei MA, Bloom SR, (2009) Relaxin-3 and its role in neuroendocrine function. Ann N Y Acad Sci 1160: 250-255.
19. van der Westhuizen ET, Halls ML, Samuel CS, Bathgate RA, Unemori EN, et al. (2008) Relaxin family peptide receptors-from orphans to therapeutic targets. Drug Discov Today 13: 640-651.
20. Ma S, Kastman H, Olucha-Bordonau FE, Capogna M, Hossain MA, et al. Relaxin-3 Receptor Activation in the Central Amygdala Enhances Fear Extinction in the Rat: Implications for Relaxin-3 Control of Emotion.; 2010; San Diego, CA, USA.
21. Kuei C, Sutton S, Bonaventure P, Pudiak C, Shelton J, et al. (2007) R3(BD23-27)R/I5 Chimeric Peptide, a Selective Antagonist for GPCR135 and GPCR142 over Relaxin Receptor LGR7: In Vitro and In Vivo characterization. Journal of Biological Chemistry 282: 25425-25435.
22. Liu C, Chen J, Kuei C, Sutton S, Nepomuceno D, et al. (2005) Relaxin-3/insulin-like peptide 5 chimeric peptide, a selective ligand for G protein-coupled receptor (GPCR)135 and GPCR142 over leucine-rich repeat-containing G protein-coupled receptor 7. Molecular Pharmacology 67: 231-240.
23. Christopoulos A, Kenakin T, (2002) G protein-coupled receptor allosterism and complexing. Pharmacol Rev 54: 323-374.
24. Conn PJ, Christopoulos A, Lindsley CW, (2009) Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders. Nat Rev Drug Discov 8: 41-54.
25. Kenakin T, (2007) Allosteric theory: taking therapeutic advantage of the malleable nature of GPCRs. Curr Neuropharmacol 5: 149-156.
26. Burford NT, Watson J, Bertekap R, Alt A, (2011) Strategies for the identification of allosteric modulators of G-protein-coupled receptors. Biochem Pharmacol 81: 691-702.
27. Keov P, Sexton PM, Christopoulos A, (2011) Allosteric modulation of G protein-coupled receptors: a pharmacological perspective. Neuropharmacology 60: 24-35.
28. Vale W, Vaughan J, Jolley D, Yamamoto G, Bruhn T, et al. (1986) Assay of Growth Hormone-releasing Factor Methods in Enzymology: Academic Press pp. 389-401.
29. Liu C, Chen J, Sutton S, Roland B, Kuei C, et al. (2003) Identification of Relaxin-3/INSL7 as a Ligand for GPCR142. Journal of Biological Chemistry 278: 50765-50770.
30. Conklin BR, Farfel Z, Lustig KD, Julius D, Bourne HR, (1993) Substitution of three amino acids switches receptor specificity of Gq alpha to that of Gi alpha. Nature 363: 274-276.
31. Matsumoto M, Kamohara M, Sugimoto T, Hidaka K, Takasaki J, et al. (2000) The novel G-protein coupled receptor SALPR shares sequence similarity with somatostatin and angiotensin receptors. Gene 248: 183-189.
32. Van der Westhuizen Emma T, Sexton Patrick M, Bathgate Ross AD, Summers Roger J, (2005) Responses of GPCR135 to human gene 3 (H3) relaxin in CHO-K1 cells determined by microphysiometry. Ann N Y Acad Sci FIELD Full Journal Title:Annals of the New York Academy of Sciences 1041: 332-337.
33. Leach K, Sexton PM, Christopoulos A, (2011) Quantification of Allosteric Interactions at G Protein-Coupled Receptors Using Radioligand Binding Assays. In: Enna SJ, editors. Current Protocols in Pharmacology pp. 1.22.21-21.22.41 March 2011 ed: Wiley Online Library.
34. Hokfelt T, Bartfai T, Bloom F, (2003) Neuropeptides: opportunities for drug discovery. Lancet Neurol 2: 463-472.
35. Rivier J, Rivier C, Vale W, (1984) Synthetic competitive antagonists of corticotropin-releasing factor: effect on ACTH secretion in the rat. Science 224: 889-891.
36. May LT, Leach K, Sexton PM, Christopoulos A, (2007) Allosteric modulation of G protein-coupled receptors. Annu Rev Pharmacol Toxicol 47: 1-51.
37. Holst B, Brandt E, Bach A, Heding A, Schwartz TW, (2005) Nonpeptide and peptide growth hormone secretagogues act both as ghrelin receptor agonist and as positive or negative allosteric modulators of ghrelin signaling. Mol Endocrinol 19: 2400-2411.
38. Knudsen LB, Kiel D, Teng M, Behrens C, Bhumralkar D, et al. (2007) Small-molecule agonists for the glucagon-like peptide 1 receptor. Proc Natl Acad Sci U S A 104: 937-942.
39. Smith CM, Ryan PJ, Hosken IT, Ma S, Gundlach AL, (2011) Relaxin-3 systems in the brain- the first 10 years. Journal of Chemical Neuroanatomy In press.
40. Impey S, Obrietan K, Storm DR, (1999) Making new connections: role of ERK/MAP kinase signaling in neuronal plasticity. Neuron 23: 11-14.
41. van der Westhuizen ET, Werry TD, Sexton PM, Summers RJ, (2007) The relaxin family peptide receptor 3 activates extracellular signal-regulated kinase 1/2 through a protein kinase C-dependent mechanism. Molecular Pharmacology 71: 1618-1629.
42. Rosengren KJ, Lin F, Bathgate RAD, Tregear GW, Daly NL, et al. (2006) Solution Structure and Novel Insights into the Determinants of the Receptor Specificity of Human Relaxin-3. Journal of Biological Chemistry 281: 5845-5851.
43. Wade JD, Lin F, Hossain MA, Shabanpoor F, Zhang S, et al. (2009) The chemical synthesis of relaxin and related peptides. Ann N Y Acad Sci 1160: 11-15.
44. Kenakin T, G protein coupled receptors as allosteric proteins and the role of allosteric modulators. J Recept Signal Transduct Res 30: 313-321.
45. Suratman S, Leach K, Sexton P, Felder C, Loiacono R, et al. (2011) Impact of species variability and 'probe-dependence' on the detection and in vivo validation of allosteric modulation at the M4 muscarinic acetylcholine receptor. Br J Pharmacol 162: 1659-1670.
46. Leach K, Davey AE, Felder CC, Sexton PM, Christopoulos A, (2011) The role of transmembrane domain 3 in the actions of orthosteric, allosteric, and atypical agonists of the M4 muscarinic acetylcholine receptor. Mol Pharmacol 79: 855-865.
47. Watson C, Jenkinson S, Kazmierski W, Kenakin T, (2005) The CCR5 receptor-based mechanism of action of 873140, a potent allosteric noncompetitive HIV entry inhibitor. Mol Pharmacol 67: 1268-1282.
48. Shimizu N, Gojobori T, (2000) How can human and simian immunodeficiency viruses utilize chemokine receptors as their coreceptors? Gene 259: 199-205.
49. Wootten D, Simms J, Koole C, Woodman OL, Summers RJ, et al. (2011) Modulation of the glucagon-like peptide-1 receptor signaling by naturally occurring and synthetic flavonoids. J Pharmacol Exp Ther 336: 540-550.