Fluorescence- and luminescence-based methods for the determination of affinity and activity of neuropeptide Y2 receptor ligands

European Journal of Pharmacology

Volumn 551, Issue 1-3, 2006, Pages 10-18

  Ziemek, Ralf ^a   Brennauer, Albert ^a   Schneider, Erich ^a   Cabrele, Chiara ^a   Beck Sickinger, Annette G ^b   Bernhardt, Günther ^a   Buschauer, Armin ^a  

^a UNIVERSITY OF REGENSBURG   (Germany)

^b UNIVERSITY OF LEIPZIG   (Germany)

Author keywords

Aequorin; BIIE0246; Chimeric G protein; Flow cytometry; Fluorescent probe; Neuropeptide Y; Y2 receptor

Indexed keywords

AEQUORIN; CALCIUM; FURA 2; GUANINE NUCLEOTIDE BINDING PROTEIN; LIGAND; N [2 [1,2 DIHYDRO 3,5(4H) DIOXO 1,2 DIPHENYL 1,2,4 TRIAZOL 4 YL]ETHYL] N2 [[1 [2 [4 [5,11 DIHYDRO 6(6H) OXODIBENZ[B,E]AZEPIN 11 YL] 1 PIPERAZINYL] 2 OXOETHYL]CYCLOPENTYL]ACETYL]ARGININAMIDE; NEUROPEPTIDE Y; NEUROPEPTIDE Y2 RECEPTOR; RADIOLIGAND;

ANIMAL CELL; ARTICLE; BINDING ASSAY; CHO CELL; CONCENTRATION RESPONSE; CONFOCAL MICROSCOPY; CONTROLLED STUDY; DRUG ACTIVITY; DRUG RECEPTOR BINDING; DRUG SELECTIVITY; FLOW CYTOMETRY; FLUORESCENCE; INCUBATION TIME; LUMINESCENCE; MITOCHONDRION; NONHUMAN; PRIORITY JOURNAL; PROTEIN EXPRESSION; PROTEIN STABILITY; RECEPTOR AFFINITY; SPECTROFLUOROMETRY;

AEQUORIN; ANIMALS; APOPROTEINS; ARGININE; BENZAZEPINES; BINDING, COMPETITIVE; CALCIUM SIGNALING; CHO CELLS; CRICETINAE; CRICETULUS; DOSE-RESPONSE RELATIONSHIP, DRUG; FLOW CYTOMETRY; FLUORESCENT DYES; GTP-BINDING PROTEIN ALPHA SUBUNITS, GQ-G11; LIGANDS; MICROSCOPY, CONFOCAL; NEUROPEPTIDE Y; PEPTIDE FRAGMENTS; PEPTIDE YY; PROTEIN BINDING; RADIOLIGAND ASSAY; RECEPTORS, NEUROPEPTIDE Y; RECOMBINANT FUSION PROTEINS; RECOMBINANT PROTEINS; REPRODUCIBILITY OF RESULTS; SPECTROMETRY, FLUORESCENCE; SWINE; TRANSFECTION;

EID: 33750431756     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejphar.2006.08.075     Document Type: Article

References (38)

1. Abbott C.R., Small C.J., Kennedy A.R., Neary N.M., Sajedi A., Ghatei M.A., and Bloom S.R. Blockade of the neuropeptide Y Y2 receptor with the specific antagonist BIIE0246 attenuates the effect of endogenous and exogenous peptide YY(3-36) on food intake. Brain Res. 1043 (2005) 139-144
2. Batterham R.L., Cowley M.A., Small C.J., Herzog H., Cohen M.A., Dakin C.L., Wren A.M., Brynes A.E., Low M.J., Ghatei M.A., Cone R.D., and Bloom S.R. Gut hormone PYY(3-36) physiologically inhibits food intake. Nature 418 (2002) 650-654
3. Beck-Sickinger A.G., Grouzmann E., Hoffmann E., Gaida W., van Meir E.G., Waeber B., and Jung G. A novel cyclic analog of neuropeptide Y specific for the Y2 receptor. Eur. J. Biochem. 206 (1992) 957-964
4. Blinks J.R. Applications of calcium-sensitive photoproteins in experimental biology. Photochem. Photobiol. 27 (1978) 423-432
5. Brini M., Marsault R., Bastianutto C., Alvarez J., Pozzan T., and Rizzuto R. Transfected aequorin in the measurement of cytosolic Ca2+ concentration ([Ca2+]c). A critical evaluation. J. Biol. Chem. 270 (1995) 9896-9903
6. Button D., and Brownstein M. Aequorin-expressing mammalian cell lines used to report Ca2+ mobilization. Cell Calcium 14 (1993) 663-671
7. Cabrele C., Wieland H.A., Langer M., Stidsen C.E., and 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 22 (2001) 365-378
8. I) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction. Biochem. Pharmacol. 22 (1973) 3099-3108
9. Coward P., Chan S.D.H., Wada H.G., Humphries G.M., and Conklin B.R. Chimeric G proteins allow a high-throughput signaling assay of Gi-coupled receptors. Anal. Biochem. 270 (1999) 242-248
10. Dautzenberg F.M. Stimulation of neuropeptide Y-mediated calcium responses in human SMS-KAN neuroblastoma cells endogenously expressing Y2 receptors by co-expression of chimeric G proteins. Biochem. Pharmacol. 69 (2005) 1493-1499
11. Dautzenberg F.M., and Neysari S. Irreversible binding kinetics of neuropeptide Y ligands to Y2 but not to Y1 and Y5 receptors. Pharmacology 75 (2005) 21-29
12. Dautzenberg F.M., Higelin J., Pflieger P., Neidhart W., and 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 48 (2005) 1043-1055
13. Dollinger H., Esser F., Mihm G., Rudolf K., Schnorrenberg G., Gaida W., and Doods H.N. Preparation of novel peptides for use as NPY antagonists. Boehringer Ingelheim Pharma, Ger. Offen. DE 19816929. Chem. Abstr. 131 (1999) 286832
14. Doods H., Gaida W., Wieland H.A., Dollinger H., Schnorrenberg G., Esser F., Engel W., Eberlein W., and Rudolf K. BIIE0246: a selective and high affinity neuropeptide Y Y2 receptor antagonist. Eur. J. Pharmacol. 384 (1999) R3-R5
15. Dumont Y., Gaudreau P., Mazzuferi M., Langlois D., Chabot J.G., Fournier A., Simonato M., and Quirion R. BODIPY-conjugated neuropeptide Y ligands: new fluorescent tools to tag Y1, Y2, Y4 and Y5 receptor subtypes. Br. J. Pharmacol. 146 (2005) 1069-1081
16. Dupriez V.J., Maes K., Le Poul E., Burgeon E., and Detheux M. Aequorin-based functional assays for G-protein-coupled receptors, ion channels, and tyrosine kinase receptors. Recept. Channels 8 (2002) 319-330
17. Edwards B.S., Oprea T., Prossnitz E.R., and Sklar L.A. Flow cytometry for high-throughput, high-content screening. Curr. Opin. Chem. Biol. 8 (2004) 392-398
18. Edwards B.S., Bologa C., Young S.M., Balakin K.V., Prossnitz E.R., Savchuck N.P., Sklar L.A., and Oprea T.I. Integration of virtual screening with high-throughput flow cytometry to identify novel small molecule formylpeptide receptor antagonists. Mol. Pharmacol. 68 (2005) 1301-1310
19. Gerald C., Walker M.W., Vaysse P.J.-J., He C., Branchek T.A., and Weinshank R.L. Expression cloning and pharmacological characterization of a human hippocampal neuropeptide Y/peptide YY Y2 receptor subtype. J. Biol. Chem. 270 (1995) 26758-26761
20. Goumain M., Voisin T., Lorinet A.-M., Ducroc R., Tsocas A., Roze C., Rouet-Benzineb P., Herzog H., Balasubramaniam A., and Laburthe M. The peptide YY-preferring receptor mediating inhibition of small intestinal secretion is a peripheral Y2 receptor: pharmacological evidence and molecular cloning. Mol. Pharmacol. 60 (2001) 124-134
21. Hatse S., Princen K., Liekens S., Vermeire K., De Clercq E., and Schols D. Fluorescent CXCL12AF647 as a novel probe for nonradioactive CXCL12/CXCR4 cellular interaction studies. Cytometry A 61 (2004) 178-188
22. Hazelwood R.L. The pancreatic polypeptide (PP-fold) family: gastrointestinal, vascular, and feeding behavioral implications. Proc. Soc. Exp. Biol. Med. 202 (1993) 44-63
23. Inouye S., Noguchi M., Sakaki Y., Takagi Y., Miyata T., Iwanaga S., Miyata T., and Tsuji F.I. Cloning and sequence analysis of cDNA for the luminescent protein aequorin. Proc. Natl. Acad. Sci. U. S. A. 82 (1985) 3154-3158
24. Le Poul E., Hisada S., Mizuguchi Y., Dupriez V.J., Burgeon E., and Detheux M. Adaptation of aequorin functional assay to high throughput screening. J. Biomol. Screen. 7 (2002) 57-65
25. Lynch J.W., Lemos V.S., Bucher B., Stoclet J.C., and Takeda K. A pertussis toxin-insensitive calcium influx mediated by neuropeptide Y2 receptors in a human neuroblastoma cell line. J. Biol. Chem. 269 (1994) 8226-8233
26. In: Michel M.C. (Ed). Neuropeptide Y and Related Peptides, Handbook of Experimental Pharmacology vol. 162 (2004), Springer, Berlin
27. Michel M.C., Beck-Sickinger A., Cox H., Doods H.N., Herzog H., Larhammar D., Quirion R., Schwartz T., and Westfall T. XVI. International Union of Pharmacology recommendations for the nomenclature of neuropeptide Y, peptide YY, and pancreatic polypeptide receptors. Pharmacol. Rev. 50 (1998) 143-150
28. Müller M., Knieps S., Gessele K., Dove S., Bernhardt G., and Buschauer A. Synthesis and neuropeptide Y Y1 receptor antagonistic activity of N,N-disubstituted omega-guanidino- and omega-aminoalkanoic acid amides. Arch. Pharm. (Weinh.) 330 (1997) 333-342
29. Neubig R.R., Spedding M., Kenakin T., and Christopoulos A. International union of pharmacology committee on receptor nomenclature and drug classification. XXXVIII. Update on terms and symbols in quantitative pharmacology. Pharmacol. Rev. 55 (2003) 597-606
30. Rose P.M., Fernandes P., Lynch J.S., Frazier S.T., Fisher S.M., Kodukula K., Kienzle B., and Seethala R. Cloning and functional expression of a cDNA encoding a human type 2 neuropeptide Y receptor. J. Biol. Chem. 270 (1995) 22661-22664
31. Schaeffer M.T., Cully D., Chou M., Liu J., Van der Ploeg L.H., and Fong T.M. Use of bioluminescent aequorin for the pharmacological characterization of 5HT receptors. J. Recept. Signal Transduct. Res. 19 (1999) 927-938
32. Schneider, E., 2005. Development of Fluorescence-Based Methods for the Determination of Ligand Affinity, Selectivity and Activity at G-Protein Coupled Receptors. Doctoral thesis, University of Regensburg.
33. Schneider E.S., Mayer M., Ziemek R., Li L., Hutzler C., Bernhardt G., and Buschauer A. A Simple and Powerful Flow Cytometric Method for the Simultaneous Determination of Multiple Parameters at G-Protein-coupled Receptor Subtypes. ChemBioChem 7 (2006) 1400-1409
34. Stables J., Green A., Marshall F., Fraser N., Knight E., Sautel M., Milligan G., Lee M., and Rees S. A bioluminescent assay for agonist activity at potentially any G-protein-coupled receptor. Anal. Biochem. 252 (1997) 115-126
35. Stables J., Mattheakis L.C., Chang R., and Rees S. Recombinant aequorin as reporter of changes in intracellular calcium in mammalian cells. Methods Enzymol. 327 (2000) 456-471
36. Stein R.A., Wilkinson J.C., Guyer C.A., and Staros J.V. An analytical approach to the measurement of equilibrium binding constants: application to EGF binding to EGF receptors in intact cells measured by flow cytometry. Biochemistry 40 (2001) 6142-6154
37. Torfs H., Poels J., Detheux M., Dupriez V., Van Loy T., Vercammen L., Vassart G., Parmentier M., and Vanden Broeck J. Recombinant aequorin as a reporter for receptor-mediated changes of intracellular Ca2+-levels in Drosophila S2 cells. Invertebr. Neurosci. 4 (2002) 119-124
38. Ungrin M.D., Singh L.M., Stocco R., Sas D.E., and Abramovitz M. An automated aequorin luminescence-based functional calcium assay for G-protein-coupled receptors. Anal. Biochem. 272 (1999) 34-42