525
Views
31
CrossRef citations to date
0
Altmetric
Research Article

Determination of Affinity and Activity of Ligands at the Human Neuropeptide Y Y4 Receptor by Flow Cytometry and Aequorin Luminescence

, , , , , & show all
Pages 217-233 | Published online: 10 Oct 2008

REFERENCES

  • von Horsten S, Hoffmann T, Alfalah M, Wrann C D, Karl T, Pabst R, Bedoui S. PP, PYY and NPY: Synthesis, storage, release and degradation. Neuropeptide Y and Related Peptides. Handbook of Experimental Pharmacology 162, M C Michel. Springer, Berlin, Heidelberg, New York 2004; 23–44
  • Cox H M. Peptidergic regulation of intestinal ion transport. A major role for neuropeptide Y and the pancreatic polypeptides. Digestion 1998; 59: 395–399
  • Schwartz T W. Pancreatic polypeptide: A hormone under vagal control. Gastroenterology 1983; 85: 1411–1425
  • Hazelwood R L. The pancreatic polypeptide (PP-fold) family: gastrointestinal, vascular, and feeding behavioral implications. Proc Soc Exp Biol Med 1993; 202: 44–63
  • Feletou M, Nicolas J P, Rodriguez M, Beauverger P, Galizzi J P, Boutin J A, Duhault J. NPY receptor subtype in the rabbit isolated ileum. Br J Pharmacol 1999; 127: 795–801
  • Pheng L H, Perron A, Quirion R, Cadieux A, Fauchere J L, Dumont Y, Regoli D. Neuropeptide Y-induced contraction is mediated by neuropeptide Y Y2 and Y4 receptors in the rat colon. Eur J Pharmacol 1999; 374: 85–91
  • Campbell R E, Smith M S, Allen S E, Grayson B E, Ffrench-Mullen J M, Grove K L. Orexin neurons express a functional pancreatic polypeptide Y4 receptor. J Neurosci 2003; 23: 1487–1497
  • Clark J T, Kalra P S, Crowley W R, Kalra S P, Neuropeptide Y. and human pancreatic polypeptide stimulate feeding behavior in rats. Endocrinology 1984; 115: 427–429
  • Asakawa A, Inui A, Ueno N, Fujimiya M, Fujino M A, Kasuga M. Mouse pancreatic polypeptide modulates food intake, while not influencing anxiety in mice. Peptides 1999; 20: 1445–1448
  • Katsuura G, Asakawa A, Inui A. Roles of pancreatic polypeptide in regulation of food intake. Peptides 2002; 23: 323–329
  • Inui A, Okita M, Nakajima M, Inoue T, Sakatani N, Oya M, Morioka H, Okimura Y, Chihara K, Baba S. Neuropeptide regulation of feeding in dogs. Am J Physiol 1991; 261: R588–594
  • Asakawa A, Inui A, Yuzuriha H, Ueno N, Katsuura G, Fujimiya M, Fujino M A, Niijima A, Meguid M M, Kasuga M. Characterization of the effects of pancreatic polypeptide in the regulation of energy balance. Gastroenterology 2003; 124: 1325–1336
  • Moran T H. Pancreatic polypeptide: more than just another gut hormone?. Gastroenterology 2003; 124: 1542–1544
  • Batterham R L, Le Roux C W, Cohen M A, Park A J, Ellis S M, Patterson M, Frost G S, Ghatei M A, Bloom S R. Pancreatic polypeptide reduces appetite and food intake in humans. J Clin Endocrinol Metab 2003; 88: 3989–3992
  • Michel M C, Beck-Sickinger A, Cox H, Doods H N, Herzog H, Larhammar D, Quirion R, Schwartz T, Westfall T. XVI. International Union of Pharmacology recommendations for the nomenclature of neuropeptide Y, peptide YY, and pancreatic polypeptide receptors. Pharmacol Rev 1998; 50: 143–150
  • Walker M W, Smith K E, Bard J, Vaysse P J, Gerald C, Daouti S, Weinshank R L, Branchek T A. A structure-activity analysis of the cloned rat and human Y4 receptors for pancreatic polypeptide. Peptides 1997; 18: 609–612
  • Yan H, Yang J, Marasco J, Yamaguchi K, Brenner S, Collins F, Karbon W. Cloning and functional expression of cDNAs encoding human and rat pancreatic polypeptide receptors. Proc Natl Acad Sci USA 1996; 93: 4661–4665
  • Berglund M M, Lundell I, Eriksson H, Soll R, Beck-Sickinger A G, Larhammar D. Studies of the human, rat, and guinea pig Y4 receptors using neuropeptide Y analogues and two distinct radioligands. Peptides 2001; 22: 351–356
  • Eriksson H, Berglund M M, Holmberg S K, Kahl U, Gehlert D R, Larhammar D. The cloned guinea pig pancreatic polypeptide receptor Y4 resembles more the human Y4 than does the rat Y4. Regul Pept 1998; 75–76: 29–37
  • Parker M S, Lundell I, Parker S L. Pancreatic polypeptide receptors: Affinity, sodium sensitivity and stability of agonist binding. Peptides 2002; 23: 291–303
  • Parker M S, Sah R, Sheriff S, Balasubramaniam A, Parker S L. Internalization of cloned pancreatic polypeptide receptors is accelerated by all types of Y4 agonists. Regul Pept 2005; 132: 91–101
  • Dumont Y, Quirion R. [(125)I]-GR231118: a high affinity radioligand to investigate neuropeptide Y Y(1) and Y(4) receptors. Br J Pharmacol 2000; 129: 37–46
  • Dautzenberg F M, Higelin J, Pflieger P, Neidhart W, Guba W. Establishment of robust functional assays for the characterization of neuropeptide Y (NPY) receptors: identification of 3-(5-benzoyl-thiazol-2-ylamino)-benzonitrile as selective NPY type 5 receptor antagonist. Neuropharmacology 2005; 48: 1043–1055
  • Gehlert D R, Schober D A, Gackenheimer S L, Beavers L, Gadski R, Lundell I, Larhammar D. [125I]Leu31, Pro34-PYY is a high affinity radioligand for rat PP1/Y4 and Y1 receptors: Evidence for heterogeneity in pancreatic polypeptide receptors. Peptides 1997; 18: 397–401
  • Schneider E, Mayer M, Ziemek R, Li L, Hutzler C, Bernhardt G, Buschauer A. A simple and powerful flow cytometric method for the simultaneous determination of multiple parameters at G protein-coupled receptor subtypes. ChemBioChem 2006; 7: 1400–1409
  • Ziemek R, Brennauer A, Schneider E, Cabrele C, Beck-Sickinger A G, Bernhardt G, Buschauer A. Fluorescence- and luminescence-based methods for the determination of affinity and activity of neuropeptide Y2 receptor ligands. Eur J Pharmacol 2006; 551: 10–18
  • Lundell I, Blomqvist A G, Berglund M M, Schober D A, Johnson D, Statnick M A, Gadski R A, Gehlert D R, Larhammar D. Cloning of a human receptor of the NPY receptor family with high affinity for pancreatic polypeptide and peptide YY. J Biol Chem 1995; 270: 29123–29128
  • Voisin T, Goumain M, Lorinet A M, Maoret J J, Laburthe M. Functional and molecular properties of the human recombinant Y4 receptor: Resistance to agonist-promoted desensitization. J Pharmacol Exp Ther 2000; 292: 638–646
  • Coward P, Chan S DH, Wada H G, Humphries G M, Conklin B R. Chimeric G proteins allow a high-throughput signaling assay of Gi-coupled receptors. Anal Biochem 1999; 270: 242–248
  • Stables J, Green A, Marshall F, Fraser N, Knight E, Sautel M, Milligan G, Lee M, Rees S. A bioluminescent assay for agonist activity at potentially any G-protein-coupled receptor. Anal Biochem 1997; 252: 115–126
  • Ungrin M D, Singh L M, Stocco R, Sas D E, Abramovitz M. An automated aequorin luminescence-based functional calcium assay for G-protein-coupled receptors. Anal Biochem 1999; 272: 34–42
  • Dupriez V J, Maes K, Le Poul E, Burgeon E, Detheux M. Aequorin-based functional assays for G-protein-coupled receptors, ion channels, and tyrosine kinase receptors. Receptors Channels 2002; 8: 319–330
  • Knight P J, Grigliatti T A, Chimeric G. proteins extend the range of insect cell-based functional assays for human G protein-coupled receptors. J Recept Signal Transduct Res 2004; 24: 241–256
  • Kostenis E. Is Gα16 the optimal tool for fishing ligands of orphan G-protein-coupled receptors?. Trends Pharmacol Sci 2001; 22: 560–564
  • Balasubramaniam A, Dhawan V C, Mullins D E, Chance W T, Sheriff S, Guzzi M, Prabhakaran M, Parker E M. Highly selective and potent neuropeptide Y (NPY) Y1 receptor antagonists based on [Pro30, Tyr32, Leu34]NPY(28-36)-NH2 (BW1911U90). J Med Chem 2001; 44: 1479–1482
  • Cabrele C, Wieland H A, Langer M, Stidsen C E, Beck-Sickinger A G. Y-receptor affinity modulation by the design of pancreatic polypeptide/neuropeptide Y chimera led to Y(5)-receptor ligands with picomolar affinity. Peptides 2001; 22: 365–378
  • Ghorai P. Arpromidine-Related Acylguanidines: Synthesis and Structure-Activity Relationships of a New Class of Guanidine-Type Histamine H2 Receptor Agonists with Reduced Basicity. Doctoral thesis, University of Regensburg, Germany 2005, http://www.opus-bayern.de/uni-regensburg/volltexte/2006/561/
  • Cheng Y, Prusoff W H. Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction. Biochem Pharmacol 1973; 22: 3099–3108
  • Müller M, Knieps S, Gessele K, Dove S, Bernhardt G, Buschauer A. Synthesis and neuropeptide Y Y1 receptor antagonistic activity of N,N-disubstituted ω -guanidino- and ω -aminoalkanoic acid amides. Arch Pharm (Weinheim) 1997; 330: 333–342
  • Gehlert D R, Schober D A, Beavers L, Gadski R, Hoffman J A, Smiley D L, Chance R E, Lundell I, Larhammar D. Characterization of the peptide binding requirements for the cloned human pancreatic polypeptide-preferring receptor. Mol Pharmacol 1996; 50: 112–118
  • Parker M S, Berglund M M, Lundell I, Parker S L. Blockade of pancreatic polypeptide-sensitive neuropeptide Y (NPY) receptors by agonist peptides is prevented by modulators of sodium transport. Implications for receptor signaling and regulation. Peptides 2001; 22: 887–898
  • Schober D A, Gackenheimer S L, Heiman M L, Gehlert D R. Pharmacological characterization of (125)I-1229U91 binding to Y1 and Y4 neuropeptide Y/peptide YY receptors. J Pharmacol Exp Ther 2000; 293: 275–280
  • Carreras C W, Siani M A, Santi D V, Dillon S B. Stable expression of a synthetic gene for the human motilin receptor: Use in an aequorin-based receptor activation assay. Anal Biochem 2002; 300: 146–151
  • George S E, Schaeffer M T, Cully D, Beer M S, McAllister G. A high-throughput glow-type aequorin assay for measuring receptor-mediated changes in intracellular calcium levels. Anal Biochem 2000; 286: 231–237
  • Janecka A, Poels J, Fichna J, Studzian K, Vanden Broeck J. Comparison of antagonist activity of spantide family at human neurokinin receptors measured by aequorin luminescence-based functional calcium assay. Regul Pept 2005; 131: 23–28
  • Knight P JK, Pfeifer T A, Grigliatti T A. A functional assay for G-protein-coupled receptors using stably transformed insect tissue culture cell lines. Anal Biochem 2003; 320: 88–103
  • Le Poul E, Hisada S, Mizuguchi Y, Dupriez V J, Burgeon E, Detheux M. Adaptation of aequorin functional assay to high throughput screening. J Biomol Screen 2002; 7: 57–65
  • Torfs H, Detheux M, Oonk H B, Akerman K E, Poels J, Loy T V, Loof A D, Vassart G, Parmentier M, Broeck J V. Analysis of C-terminally substituted tachykinin-like peptide agonists by means of aequorin-based luminescent assays for human and insect neurokinin receptors. Biochem Pharmacol 2002; 63: 1675–1682
  • Conklin B R, Farfel Z, Lustig K D, Julius D, Bourne H R. Substitution of three amino acids switches receptor specificity of Gqα to that of Giα. Nature 1993; 363: 274–276
  • Schober D A, Van Abbema A M, Smiley D L, Bruns R F, Gehlert D R. The neuropeptide Y Y1 antagonist, 1229U91, a potent agonist for the human pancreatic polypeptide-preferring (NPY Y4) receptor. Peptides 1998; 19: 537–542
  • Parker E M, Babij C K, Balasubramaniam A, Burrier R E, Guzzi M, Hamud F, Mukhopadhyay G, Rudinski M S, Tao Z, Tice M, Xia L, Mullins D E, Salisbury B G. GR231118 (1229U91) and other analogues of the C-terminus of neuropeptide Y are potent neuropeptide Y Y1 receptor antagonists and neuropeptide Y Y4 receptor agonists. Eur J Pharmacol 1998; 349: 97–105
  • Cox H M, Tough I R, Zandvliet D W, Holliday N D. Constitutive neuropeptide Y Y(4) receptor expression in human colonic adenocarcinoma cell lines. Br J Pharmacol 2001; 132: 345–353
  • Berglund M M, Schober D A, Statnick M A, McDonald P H, Gehlert D R. The use of bioluminescence resonance energy transfer 2 to study neuropeptide Y receptor agonist-induced beta-arrestin 2 interaction. J Pharmacol Exp Ther 2003; 306: 147–156
  • Berglund M M, Schober D A, Esterman M A, Gehlert D R. Neuropeptide Y Y4 receptor homodimers dissociate upon agonist stimulation. J Pharmacol Exp Ther 2003; 307: 1120–1126

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.