β-Arrestin-based bret2 screening assay for the "nong" β-arrestin binding CB1 receptor

Journal of Biomolecular Screening

Volumn 14, Issue 4, 2009, Pages 371-380

  Vrecl, Milka ^a,b   Nørregaard, Pia Karina ^a   Almholt, Dorthe L C ^b   Elster, Lisbeth ^a   Pogaĉnik, Azra ^a   Heding, Anders ^b  

^a UNIVERSITY OF LJUBLJANA   (Slovenia)

^b 7TM Pharma ^*  (Denmark)

Author keywords

arrestin 2; 7TM receptors; BRET2; CB1R; Screening

Indexed keywords

BETA ARRESTIN; BETA ARRESTIN 2; BOMBESIN RECEPTOR; CANNABINOID 1 RECEPTOR; CARBOXY TERMINAL TELOPEPTIDE; VASOPRESSIN V2 RECEPTOR;

ARTICLE; BINDING AFFINITY; BIOLUMINESCENCE RESONANCE ENERGY TRANSFER; CARBOXY TERMINAL SEQUENCE; CONTROLLED STUDY; EMBRYO; HUMAN; HUMAN CELL; IC 50; PERFORMANCE; PRIORITY JOURNAL; PROTEIN ANALYSIS; PROTEIN BINDING; PROTEIN INTERACTION; SCREENING;

AMINO ACID SEQUENCE; ARRESTINS; BIOLOGICAL ASSAY; CELL LINE; FLUORESCENCE RESONANCE ENERGY TRANSFER; HUMANS; MOLECULAR SEQUENCE DATA; PROTEIN BINDING; PROTEIN STRUCTURE, TERTIARY; RECEPTOR, CANNABINOID, CB1; RECEPTORS, BOMBESIN; SIGNAL TRANSDUCTION; SMALL MOLECULE LIBRARIES;

EID: 65449156031     PISSN: 10870571     EISSN: 1552454X     Source Type: Journal    
DOI: 10.1177/1087057109333101     Document Type: Article

References (40)

1. Cooke D., Bloom S.: The obesity pipeline: current strategies in the development of anti-obesity drugs. Nat Rev Drug Discov 2006 ; 5: 919-931.
2. Padwal RS, Majumdar SR: Drug treatments for obesity: orlistat, sibutramine, and rimonabant. Lancet 2007 ; 369: 71-77.
3. Howlett AC, Breivogel CS, Childers SR, Deadwyler SA, Hampson RE, Porrino LJ: Cannabinoid physiology and pharmacology: 30 years of progress. Neuropharmacology 2004 ; 47 (suppl 1). 345-358.
4. Brown AJ: Novel cannabinoid receptors. Br J Pharmacol 2007 ; 152: 567-575.
5. Matias I., Bisogno T., Di Marzo V.: Endogenous cannabinoids in the brain and peripheral tissues: regulation of their levels and control of food intake. Int J Obes 2006 ; 30: S7 - S12.
6. Di Marzo V.: The endocannabinoid system in obesity and type 2 diabetes. Diabetologia 2008 ; 51: 1356-1367.
7. Pagotto U., Pasquali R.: Endocannabinoids and energy metabolism. J Endocrinol Invest 2006 ; 29: 66-76.
8. Lim WK: GPCR drug discovery: novel ligands for CNS receptors. Recent Patents CNS Drug Discov 2007 ; 2: 107-112.
9. Bohn LM: Constitutive trafficking: more than just running in circles? Mol Pharmacol 2007 ; 71: 957-958.
10. Milligan G.: Principles: extending the utility of [35S]GTP gamma S binding assays. Trends Pharmacol Sci 2003 ; 24: 87-90.
11. Harrison C., Traynor JR: The [35S]GTP3S binding assay: approaches and applications in pharmacology. Life Sci 2003 ; 74: 489-508.
12. Heding A.: Use of the BRET 7TM receptor/β-arrestin assay in drug discovery and screening. Expert Rev Mol Diagn 2004 ; 4: 403-411.
13. Milligan G.: Applications of bioluminescence- and fluorescence resonance energy transfer to drug discovery at G protein-coupled receptors. Eur J Pharm Sci 2004 ; 21: 397-405.
14. Vrecl M., Jorgensen R., Pogacnik A., Heding A.: Development of a BRET2 screening assay using β-arrestin 2 mutants. J Biomol Screen 2004 ; 9: 322-333.
15. Jin W., Brown S., Roche JP, Hsieh C., Celver JP, Kovoor A., et al. Distinct domains of the CB1 cannabinoid receptor mediate desensitization and internalization. J Neurosci 1999 ; 19: 3773-3780.
16. Bakshi K., Mercier RW, Pavlopoulos S.: Interaction of a fragment of the cannabinoid CB1 receptor C-terminus with arrestin-2. FEBS Lett 2007 ; 581: 5009-5016.
17. Oakley RH, Laporte SA, Holt JA, Barak LS, Caron MG: Molecular determinants underlying the formation of stable intracellular G protein-coupled receptor-β-arrestin complexes after receptor endocytosis. J Biol Chem 2001 ; 276: 19452-19460.
18. Oakley RH, Laporte SA, Holt JA, Caron MG, Barak LS: Differential affinities of visual arrestin, βarrestin1, and βarrestin2 for G protein-coupled receptors delineate two major classes of receptors. J Biol Chem 2000 ; 275: 17201-17210.
19. Oakley RH, Laporte SA, Holt JA, Barak LS, Caron MG: Association of β-arrestin with G protein-coupled receptors during clathrin-mediated endocytosis dictates the profile of receptor resensitization. J Biol Chem 1999 ; 274: 32248-32257.
20. Hamdan FF, Audet M., Garneau P., Pelletier J., Bouvier M.: High-throughput screening of G protein-coupled receptor antagonists using a bioluminescence resonance energy transfer 1-based β-arrestin2 recruitment assay. J Biomol Screen 2005 ; 10: 463-475.
21. Heding A., Vrecl M., Bogerd J., McGregor A., Sellar R., Taylor PL, et al. Gonadotropin-releasing hormone receptors with intracellular carboxyl-terminal tails undergo acute desensitization of total inositol phosphate production and exhibit accelerated internalization kinetics. J Biol Chem 1998 ; 273: 11472-11477.
22. Heding A., Vrecl M., Hanyaloglu AC, Sellar R., Taylor PL, Eidne KA: The rat gonadotropin-releasing hormone receptor internalizes via a β-arrestin-independent, but dynamin-dependent, pathway: addition of a carboxyl-terminal tail confers β-arrestin dependency. Endocrinology 2000 ; 141: 299-306.
23. Hanyaloglu AC, Vrecl M., Kroeger KM, Miles LE, Qian H., Thomas WG, et al. Casein kinase II sites in the intracellular C-terminal domain of the thyrotropin-releasing hormone receptor and chimeric gonadotropin-releasing hormone receptors contribute to β-arrestin-dependent internalization. J Biol Chem 2001 ; 276: 18066-18074.
24. Liu JJ, Hartman DS, Bostwick JR: An immobilized metal ion affinity adsorption and scintillation proximity assay for receptor-stimulated phosphoinositide hydrolysis. Anal Biochem 2003 ; 318: 91-99.
25. Kostenis E., Martini L., Ellis J., Waldhoer M., Heydorn A., Rosenkilde MM, et al. A highly conserved glycine within linker I and the extreme C terminus of G protein ± subunits interact cooperatively in switching G protein-coupled receptor-to-effector specificity. J Pharmacol Exp Ther 2005 ; 313: 78-87.
26. Vrecl M., Drinovec L., Elling C., Heding A.: Opsin oligomerization in a heterologous cell system. J Recept Signal Transduct Res 2006 ; 26: 505-526.
27. Mukhopadhyay S., Shim JY, Assi AA, Norford D., Howlett AC: CB(1) cannabinoid receptor-G protein association: a possible mechanism for differential signaling. Chem Phys Lipids 2002 ; 121: 91-109.
28. Bertrand L., Parent S., Caron M., Legault M., Joly E., Angers S., et al. The BRET2/arrestin assay in stable recombinant cells: a platform to screen for compounds that interact with G protein-coupled receptors (GPCRS). J Recept Signal Transduct Res 2002 ; 22: 533-541.
29. Hsieh C., Brown S., Derleth C., Mackie K.: Internalization and recycling of the CB1 cannabinoid receptor. J Neurochem 1999 ; 73: 493-501.
30. Qian H., Pipolo L., Thomas WG: Association of β-arrestin 1 with the type 1A angiotensin II receptor involves phosphorylation of the receptor carboxyl terminus and correlates with receptor internalization. Mol Endocrinol 2001 ; 15: 1706-1719.
31. Ghosh RN, DeBiasio R., Hudson CC, Ramer ER, Cowan CL, Oakley RH: Quantitative cell-based high-content screening for vasopressin receptor agonists using transfluor technology. J Biomol Screen 2005 ; 10: 476-484.
32. Jensen RT, Battey JF, Spindel ER, Benya RV: International Union of Pharmacology. LXVIII. Mammalian bombesin receptors: nomenclature, distribution, pharmacology, signaling, and functions in normal and disease states. Pharmacol Rev 2008 ; 60: 1-42.
33. Choi G., Guo J., Makriyannis A.: The conformation of the cytoplasmic helix 8 of the CB1 cannabinoid receptor using NMR and circular dichroism. Biochim Biophys Acta 2005 ; 1668: 1-9.34.
34. Nie J., Lewis DL: The proximal and distal C-terminal tail domains of the CB1 cannabinoid receptor mediate G protein coupling. Neuroscience 2001 ; 107: 161-167.
35. Celver J., Vishnivetskiy SA, Chavkin C., Gurevich VV: Conservation of the phosphate-sensitive elements in the arrestin family of proteins. J Biol Chem 2002 ; 277: 9043-9048.
36. Kubale V., Abramovic Z., Pogacnik A., Heding A., Sentjurc M., Vrecl M.: Evidence for a role of caveolin-1 in neurokinin-1 receptor plasma-membrane localization, efficient signaling, and interaction with β-arrestin 2. Cell Tissue Res 2007 ; 330: 231-245.
37. Leterrier C., Bonnard D., Carrel D., Rossier J., Lenkei Z.: Constitutive endocytic cycle of the CB1 cannabinoid receptor. J Biol Chem 2004 ; 279: 36013-36021.
38. Pertwee RG: Inverse agonism and neutral antagonism at cannabinoid CB1 receptors. Life Sci 2005 ; 76: 1307-1324.
39. Milligan G.: Constitutive activity and inverse agonists of G protein-coupled receptors: a current perspective. Mol Pharmacol 2003 ; 64: 1271-1276.
40. Kostenis E., Waelbroeck M., Milligan G.: Techniques: promiscuous G± proteins in basic research and drug discovery. Trends Pharmacol Sci 2005 ; 26: 595-602.