Measurements of β-arrestin recruitment to activated seven transmembrane receptors using enzyme complementation

Methods in Molecular Biology

Volumn 897, Issue , 2012, Pages 181-203

  Bassoni, Daniel L ^a   Raab, William J ^a   Achacoso, Philip L ^a   Loh, Chin Yee ^a   Wehrman, Tom S ^a  

^a DiscoveRx Corporation   (United States)

Author keywords

Agonist; Antagonist; Arrestin; Assay; Biased agonism; Enzyme complementation; Functional selectivity; GPCR; High throughput screening (HTS); Ligand bias; PathHunter

Indexed keywords

ADENOSINE RECEPTOR; ADRENERGIC RECEPTOR; ANGIOTENSIN RECEPTOR; APELIN RECEPTOR; BETA ARRESTIN; BETA GALACTOSIDASE; BILE ACID; BRADYKININ; BRADYKININ B1 RECEPTOR; BRADYKININ B2 RECEPTOR; CALCITONIN RECEPTOR; CANNABINOID; CHEMOKINE RECEPTOR; CHOLECYSTOKININ RECEPTOR; CHOLINERGIC RECEPTOR; CORTICOTROPIN RECEPTOR; DOPAMINE RECEPTOR; ENDOTHELIN RECEPTOR; FORMYLPEPTIDE RECEPTOR; GALANIN RECEPTOR; GHRELIN RECEPTOR; GLUCAGON RECEPTOR; GUANINE NUCLEOTIDE BINDING PROTEIN; HISTAMINE RECEPTOR; LEUKOTRIENE RECEPTOR; LYSOPHOSPHOLIPID RECEPTOR; MELANOCORTIN RECEPTOR; MEMBRANE RECEPTOR; SEROTONIN RECEPTOR; UNINDEXED DRUG; G PROTEIN COUPLED RECEPTOR; RETINA S ANTIGEN;

ARTICLE; HIGH THROUGHPUT SCREENING; MAMMAL CELL; PRIORITY JOURNAL; PROTEIN ANALYSIS; PROTEIN PROTEIN INTERACTION; RECEPTOR DOWN REGULATION; REPRODUCIBILITY; ANIMAL; CELL LINE; DRUG DEVELOPMENT; HUMAN; METABOLISM; METHODOLOGY; PROTEIN BINDING;

ANIMALS; ARRESTINS; BETA-GALACTOSIDASE; CELL LINE; DRUG DISCOVERY; HUMANS; PROTEIN BINDING; RECEPTORS, G-PROTEIN-COUPLED;

EID: 84867290208     PISSN: 10643745     EISSN: None     Source Type: Book Series    
DOI: 10.1007/978-1-61779-909-9_9     Document Type: Article

References (45)

1. Fredriksson R, Lagerström MC, Lundin LG, Schiöth HB (2003) The G-protein-coupled receptors in the human genome form five main families. Phylogenetic analysis, paralogon groups, and fingerprints. Mol Pharmacol 63:1256-1272
2. Kenakin T (2011) Functional selectivity and biased receptor signaling. J Pharmacol Exp Ther 336:296-302
3. Williams C, Hill SJ (2009) GPCR signaling: understanding the pathway to successful drug discovery. Methods Mol Biol 552:39-50
4. Whalen EJ, Rajagopal S, Lefkowitz RJ (2011) Therapeutic potential of beta-arrestin-and G protein-biased agonists. Trends Mol Med 17:126-139
5. Rajagopal S, Rajagopal K, Lefkowitz RJ (2010) Teaching old receptors new tricks: biasing seven-transmembrane receptors. Nat Rev Drug Discov 9:373-386
6. DeWire SM, Ahn S, Lefkowitz RJ, Shenoy SK (2007) Beta-arrestins and cell signaling. Annu Rev Physiol 69:483-510
7. Gurevich VV, Gurevich EV, Cleghorn WM (2008) Arrestins as multi-functional signaling adaptors. Handb Exp Pharmacol 186:15-37
8. Kovacs JJ, Hara MR, Davenport CL, Kim J, Lefkowitz RJ (2009) Arrestin development: emerging roles for beta-arrestins in developmental signaling pathways. Dev Cell 17:443-458
9. Luttrell LM, Gesty-Palmer D (2010) Beyond desensitization: physiological relevance of arrestin-dependent signaling. Pharmacol Rev 62:305-330
10. Walters RW, Shukla AK, Kovacs JJ, Violin JD, DeWire SM, Lam CM, Chen JR, Muehlbauer MJ, Whalen EJ, Lefkowitz RJ (2009) beta-Arres-tin1 mediates nicotinic acid-induced flushing, but not its antilipolytic effect, in mice. J Clin Invest 119:1312-1321
11. Ferguson SS, Caron MG (2004) Green fluores-cent protein-tagged beta-arrestin translocation as a measure of G protein-coupled receptor activation. Methods Mol Biol 237:121-126
12. Ferguson SS, Downey WE III, Colapietro AM, Barak LS, Ménard L, Caron MG (1996) Role of beta-arrestin in mediating agonist-promoted G protein-coupled receptor internalization. Science 271:363-366
13. Oakley RH, Hudson CC, Cruickshank RD, Meyers DM, Payne RE Jr, Rhem SM, Loomis CR (2002) The cellular distribution of fluorescently labeled arrestins provides a robust, sensitive, and universal assay for screening G protein-coupled receptors. Assay Drug Dev Technol 1:21-30
14. Garippa RJ, Hoffman AF, Gradl G, Kirsch A (2006) High-throughput confocal microscopy for beta-arrestin-green fluorescent protein translocation G protein-coupled receptor assays using the Evotec Opera. Methods Enzymol 414:99-120
15. Heding A (2004) Use of the BRET 7TM receptor/beta-arrestin assay in drug discovery and screening. Expert Rev Mol Diagn 4:403-411
16. van der Lee MM, Blomenröhr M, van der Doelen AA, Wat JW, Smits N, Hanson BJ, van Koppen CJ, Zaman GJ (2009) Pharmacological characterization of receptor redistribution and beta-arrestin recruitment assays for the can-nabinoid receptor 1. J Biomol Screen 14: 811-823
17. Verkaar F, van Rosmalen JW, Blomenröhr M, van Koppen CJ, Blankensteijn WM, Smits JF, Zaman GJ (2008) G protein-independent cell-based assays for drug discovery on seven-trans-membrane receptors. Biotechnol Annu Rev 14:253-274
18. Cabantous S, Pédelacq JD, Mark BL, Naranjo C, Terwilliger TC, Waldo GS (2005) Recent advances in GFP folding reporter and split-GFP solubility reporter technologies. Application to improving the folding and solubility of recalcitrant proteins from Mycobacterium tuberculosis. J Struct Funct Genomics 6:113-119
19. Wehrman T, Kleaveland B, Her JH, Balint RF, Blau HM (2002) Protein-protein interactions monitored in mammalian cells via complementation of beta-lactamase enzyme fragments. Proc Natl Acad Sci USA 99:3469-3474
20. Galarneau A, Primeau M, Trudeau LE, Michnick SW (2002) Beta-lactamase protein fragment complementation assays as in vivo and in vitro sensors of protein protein interactions. Nat Biotechnol 20:619-622
21. Wehrman T, He X, Raab B, Dukipatti A, Blau H, Garcia KC (2007) Structural and mechanistic insights into nerve growth factor interactions with the TrkA and p75 receptors. Neuron 53:25-38
22. Wehrman TS, Casipit CL, Gewertz NM, Blau HM (2005) Enzymatic detection of protein translocation. Nat Methods 2:521-527
23. von Degenfeld G, Wehrman TS, Hammer MM, Blau HM (2007) A universal technology for monitoring G-protein-coupled receptor activation in vitro and noninvasively in live animals. FASEB J 21:3819-3826
24. Paulmurugan R, Gambhir SS (2005) Fire fly luciferase enzyme fragment complementation for imaging in cells and living animals. Anal Chem 77:1295-1302
25. Casanova E, Lemberger T, Fehsenfeld S, Mantamadiotis T, Schütz G (2003) Alpha complementation in the Cre recombinase enzyme. Genesis 37:25-29
26. Sun YC, Li Y, Zhang H, Yan HQ, Dowling DN, Wang YP (2006) Reconstitution of the enzyme AroA and its glyphosate tolerance by fragment complementation. FEBS Lett 580:1521-1527
27. Djannatian MS, Galinski S, Fischer TM, Rossner MJ (2011) Studying G protein-coupled receptor activation using split-tobacco etch virus assays. Anal Biochem 412: 141-152
28. van Der Lee MM, Bras M, van Koppen CJ, Zaman GJ (2008) beta-Arrestin recruitment assay for the identification of agonists of the sphingosine 1-phosphate receptor EDG1. J Biomol Screen 13:986-998
29. McGuinness D, Malikzay A, Visconti R, Lin K, Bayne M, Monsma F, Lunn CA (2009) Characterizing cannabinoid CB2 receptor ligands using DiscoveRx PathHunter beta-arrestin assay. J Biomol Screen 14:49-58
30. Patel A, Murray J, McElwee-Whitmer S, Bai C, Kunapuli P, Johnson EN (2009) A combination of ultrahigh throughput PathHunter and cytokine secretion assays to identify glucocorticoid receptor agonists. Anal Biochem 385:286-292
31. Gao ZG, Jacobson KA (2008) Translocation of arrestin induced by human A(3) adenosine receptor ligands in an engineered cell line: comparison with G protein-dependent pathways. Pharmacol Res 57:303-311
32. Rosethorne EM, Charlton SJ (2011) Agonist-biased signaling at the histamine H4 receptor: JNJ7777120 recruits {beta}-arrestin without activating G proteins. Mol Pharmacol 79:749-757
33. Poulin B, Butcher A, McWilliams P, Bourgognon JM, Pawlak R, Kong KC, Bottrill A, Mistry S, Wess J, Rosethorne EM, Charlton SJ, Tobin AB (2010) The M3-muscarinic receptor regulates learning and memory in a receptor phosphory-lation/arrestin-dependent manner. Proc Natl Acad Sci USA 107:9440-9445
34. McPherson J, Rivero G, Baptist M, Llorente J, Al-Sabah S, Krasel C, Dewey WL, Bailey CP, Rosethorne EM, Charlton SJ, Henderson G, Kelly E (2010) mu-Opioid receptors: correlation of agonist ef ficacy for signalling with ability to activate internalization. Mol Pharmacol 78:756-766
35. Kong KC, Butcher AJ, McWilliams P, Jones D, Wess J, Hamdan FF, Werry T, Rosethorne EM, Charlton SJ, Munson SE, Cragg HA, Smart AD, Tobin AB (2010) M3-muscarinic receptor promotes insulin release via receptor phospho-rylation/arrestin-dependent activation of protein kinase D1. Proc Natl Acad Sci USA 107:21181-21186
36. Zhao X, Jones A, Olson KR, Peng K, Wehrman T, Park A, Mallari R, Nebalasca D, Young SW, Xiao SH (2008) A homogeneous enzyme fragment complementation-based beta-arrestin translocation assay for high-throughput screening of G-protein-coupled receptors. J Biomol Screen 13:737-747
37. Yin H, Chu A, Li W, Wang B, Shelton F, Otero F, Nguyen DG, Caldwell JS, Chen YA (2009) Lipid G protein-coupled receptor ligand identification using beta-arrestin PathHunter assay. J Biol Chem 284:12328-12338
38. Wehrman TS, Raab WJ, Casipit CL, Doyonnas R, Pomerantz JH, Blau HM (2006) A system for quantifying dynamic protein interactions de fines a role for Herceptin in modulating ErbB2 interactions. Proc Natl Acad Sci USA 103:19063-19068
39. Rajagopal S, Ahn S, Rominger DH, Gowen-Macdonald W, Lam CM, Dewire SM, Violin JD, Lefkowitz RJ (2011) Quantifying ligand bias at seven-transmembrane receptors. Mol Pharmacol 80:367-377
40. van Lith LH, Oosteromm J, van Elsas A, Zaman GJ (2009) C5a-stimulated recruitment of beta-arrestin2 to the nonsignaling 7-trans-membrane decoy receptor C5L2. J Biomol Screen 14:1067-1075
41. Zabel BA, Wang Y, Lewén S, Berahovich RD, Penfold ME, Zhang P, Powers J, Summers BC, Miao Z, Zhao B, Jalili A, Janowska-Wieczorek A, Jaen JC, Schall TJ (2009) Elucidation of CXCR7-mediated signaling events and inhibition of CXCR4-mediated tumor cell transend-othelial migration by CXCR7 ligands. J Immunol 183:3204-3211
42. Waterfield A, Kinloch R, Williams R, Young T, Nickolls S (2009) The DiscoveRx PathHunter β-arrestin assay; a measure of agonist affinity? pA2online 3:001
43. Charlton SJ, Vauquelin G (2010) Elusive equilibrium: the challenge of interpreting receptor pharmacology using calcium assays. Br J Pharmacol 161:1250-1265
44. Adham N, Ellerbrock B, Hartig P, Weinshank RL, Branchek T (1993) Receptor reserve masks partial agonist activity of drugs in a cloned rat 5-hydroxytryptamine1B receptor expression system. Mol Pharmacol 43:427-433
45. Masri B, Salahpour A, Didriksen M, Ghisi V, Beaulieu JM, Gainetdinov RR, Caron MG (2008) Antagonism of dopamine D2 receptor/beta-arrestin 2 interaction is a common property of clinically effective antipsychotics. Proc Natl Acad Sci USA 105:13656-13661