Approaches to assess functional selectivity in gpcrs: Evaluating g protein signaling in an endogenous environment

Methods in Molecular Biology

Volumn 1335, Issue , 2015, Pages 177-189

  Bohn, Laura M ^a   Zhou, Lei ^a   Ho, Jo Hao ^a  

^a NONE

Author keywords

Brain; Endogenous receptors; G protein coupling; GDP; GPCR; GTP gamma S; Neuropharmacology; Opioid receptors; Radioactivity assays; Receptor pharmacology; Striatum

Indexed keywords

G PROTEIN COUPLED RECEPTOR; BETA ARRESTIN; GUANINE NUCLEOTIDE BINDING PROTEIN; GUANOSINE 5' O (3 THIOTRIPHOSPHATE); RETINA S ANTIGEN;

ADAPTATION; ARTICLE; BINDING ASSAY; BRAIN TISSUE; CELL ASSAY; CONTROLLED STUDY; PRIMARY CULTURE; PRIORITY JOURNAL; PROTEIN ANALYSIS; SIGNAL TRANSDUCTION; TISSUE CULTURE; ANIMAL; BRAIN; CELL LINE; ENZYME SPECIFICITY; IMMUNOPRECIPITATION; METABOLISM; MOUSE;

ANIMALS; ARRESTINS; BETA-ARRESTINS; BRAIN; CELL LINE; GTP-BINDING PROTEINS; GUANOSINE 5'-O-(3-THIOTRIPHOSPHATE); IMMUNOPRECIPITATION; MICE; RECEPTORS, G-PROTEIN-COUPLED; SIGNAL TRANSDUCTION; SUBSTRATE SPECIFICITY;

EID: 84938899930     PISSN: 10643745     EISSN: None     Source Type: Book Series    
DOI: 10.1007/978-1-4939-2914-6_12     Document Type: Article

References (33)

1. Rajagopal S, Rajagopal K, Lefkowitz RJ (2010) Teaching old receptors new tricks: biasing seven-transmembrane receptors. Nat Rev Drug Discov 9:373-386
2. Wisler J, Xiao K, Thomsen A, Lefkowitz R (2014) Recent developments in biased agonism. Curr Opin Cell Biol 27:18
3. Zhou L, Lovell KM, Frankowski KJ, Slauson SR, Phillips AM, Streicher JM, Stahl E, Schmid CL, Hodder P, Madoux F (2013) Development of functionally selective, small molecule agonists at kappa opioid receptors. J Biol Chem 288:36703-36716
4. Rahmeh R, Damian M, Cottet M, Orcel H, Mendre C, Durroux T, Sharma KS, Durand G, Pucci B, Trinquet E (2012) Structural insights into biased G proteincoupled receptor signaling revealed byfl uorescence spectroscopy. Proc Natl Acad Sci 109:6733-6738
5. Rivero G, Llorente J, McPherson J, Cooke A, Mundell SJ, McArdle CA, Rosethorne EM, Charlton SJ, Krasel C, Bailey CP (2012) Endomorphin-2: a biased agonist at the μ-opioid receptor. Mol Pharmacol 82:178-188
6. Hurowitz EH, Melnyk JM, Chen Y-J, Kouros- Mehr H, Simon MI, Shizuya H (2000) Genomic characterization of the human heterotrimeric G protein α, β, and γ subunit genes. DNA Res 7:111-120
7. Baltoumas FA, Theodoropoulou MC, Hamodrakas SJ (2013) Interactions of the α-subunits of heterotrimeric G-proteins with GPCRs, effectors and RGS proteins: a critical review and analysis of interacting surfaces, conformational shifts, structural diversity and electrostatic potentials. J Struct Biol 182:209-218
8. Schmid CL, Streicher JM, Groer CE, Munro TA, Zhou L, Bohn LM (2013) Functional selectivity of 6′-guanidinonaltrindole (6′- GNTI) at κ-opioid receptors in striatal neurons. J Biol Chem 288:22387-22398
9. Bohn LM, Lefkowitz RJ, Gainetdinov RR, Peppel K, Caron MG, Lin F-T (1999) Enhanced morphine analgesia in mice lacking β-arrestin 2. Science 286:2495-2498
10. Dennis I, Whalley BJ, Stephens GJ (2008) Effects of Δ9‐tetrahydrocannabivarin on [35S] GTPγS binding in mouse brain cerebellum and piriform cortex membranes. Br J Pharmacol 154:1349-1358
11. Hungund B, Vinod K, Kassir S, Basavarajappa B, Yalamanchili R, Cooper T, Mann J, Arango V (2004) Upregulation of CB1 receptors and agonist-stimulated [35S]GTPγS binding in the prefrontal cortex of depressed suicide victims. Mol Psychiatry 9:184-190
12. Jin LQ, Wang HY, Friedman E (2001) Stimulated D1 dopamine receptors couple to multiple Gα proteins in different brain regions. J Neurochem 78:981-990
13. Márki Á, Monory K, Ötvös F, Tóth G, Krassnig R, Schmidhammer H, Traynor JR, Roques BP, Maldonado R, Borsodi A (1999) μ-Opioid receptor specifi c antagonist cyprodime: characterization by in vitro radioligand and [35S] GTPγS binding assays. Eur J Pharmacol 383:209-214
14. Panchalingam S, Undie AS (2000) Optimized binding of [35S] GTPγS to Gq-like proteins stimulated with dopamine D1-like receptor agonists. Neurochem Res 25:759-767
15. Szekeres PG, Traynor JR (1997) Delta opioid modulation of the binding of guanosine-5′-O- (3-[35S] thio) triphosphate to NG108-15 cell membranes: characterization of agonist and inverse agonist effects. J Pharmacol Exp Ther 283:1276-1284
16. Odagaki Y, Toyoshima R (2006) Dopamine D 2 receptor-mediated G protein activation assessed by agonist-stimulated [35S] guanosine 5′-O-(γ-thiotriphosphate) binding in rat striatal membranes. Prog Neuro-Psychopharmacol Biol Psychiatr 30:1304-1312
17. Wang Y, Tang K, Inan S, Siebert D, Holzgrabe U, Lee DY, Huang P, Li J-G, Cowan A, Liu- Chen L-Y (2005) Comparison of pharmacological activities of three distinct κ ligands (salvinorin A, TRK-820 and 3FLB) on κ opioid receptors in vitro and their antipruritic and antinociceptive activities in vivo. J Pharmacol Exp Ther 312:220-230
18. Savinainen JR, Järvinen T, Laine K, Laitinen JT (2001) Despite substantial degradation, 2‐ arachidonoylglycerol is a potent full effi cacy agonist mediating CB1 receptor‐dependent Gprotein activation in rat cerebellar membranes. Br J Pharmacol 134:664-672
19. Sim-Selley L, Daunais J, Porrino L, Childers S (1999) Mu and kappa 1 opioid-stimulated [35S] guanylyl-5′-O-(γ-THIO)-triphosphate binding in cynomolgus monkey brain. Neuroscience 94:651-662
20. Rinken A, Finnman U-B, Fuxe K (1999) Pharmacological characterization of dopaminestimulated [35S]-guanosine 5′-(γ-thiotriphosphate)([35S] GTPγS) binding in rat striatal membranes. Biochem Pharmacol 57:155-162
21. Albrecht E, Samovilova NN, Oswald S, Baeger I, Berger H (1998) Nociceptin (orphanin FQ): high-affi nity and high-capacity binding site coupled to low-potency stimulation of guanylyl-5′-O-(γ-thio)-triphosphate binding in rat brain membranes. J Pharmacol Exp Ther 286:896-902
22. Zhu J, Luo L-Y, Li J-G, Chen C, Liu-Chen L-Y (1997) Activation of the cloned human kappa opioid receptor by agonists enhances [35S] GTPγS binding to membranes: determination of potencies and effi cacies of ligands. J Pharmacol Exp Ther 282:676-684
23. Selley DE, Sim LJ, Xiao R, Liu Q, Childers SR (1997) μ-Opioid receptor-stimulated guanosine-5′-O-(γ-thio)-triphosphate binding in rat thalamus and cultured cell lines: signal transduction mechanisms underlying agonist effi cacy. Mol Pharmacol 51:87-96
24. Traynor JR, Nahorski SR (1995) Modulation by mu-opioid agonists of guanosine-5′-O- (3-[35S] thio) triphosphate binding tomembranes from human neuroblastoma SH-SY5Y cells. Mol Pharmacol 47:848-854
25. Sim LJ, Selley DE, Childers SR (1995) In vitro autoradiography of receptor-activated G proteins in rat brain by agonist-stimulated guanylyl 5′-[gamma-[35S] thio]-triphosphate binding. Proc Natl Acad Sci 92:7242-7246
26. Wettschureck N, Offermanns S (2005) Mammalian G proteins and their cell type specifi c functions. Physiol Rev 85:1159-1204
27. Hinton DR, Blanks JC, Fong H, Casey PJ, Hildebrandt E, Simons MI (1990) Novel localization of a G protein, Gz-alpha, in neurons of brain and retina. J Neurosci 10: 2763-2770
28. Matesic D, Manning D, Wolfe B, Luthin G (1989) Pharmacological and biochemical characterization of complexes of muscarinic acetylcholine receptor and guanine nucleotide-binding protein. J Biol Chem 264:21638-21645
29. Law SF, Manning D, Reisine T (1991) Identifi cation of the subunits of GTP-binding proteins coupled to somatostatin receptors. J Biol Chem 266:17885-17897
30. Law S, Reisine T (1992) Agonist binding to rat brain somatostatin receptors alters the interaction of the receptors with guanine nucleotidebinding regulatory proteins. Mol Pharmacol 42:398-402
31. Chalecka Franaszek E, Weems HB, Crowder AT, Cox BM, Côté TE (2000) Immunoprecipitation of high‐affi nity, guanine nucleotide‐sensitive, solubilized μ‐opioid receptors from rat brain. J Neurochem 74: 1068-1078
32. Sidhu A, Kimura K, Uh M, White BH, Patel S (1998) Multiple coupling of human D5 dopamine receptors to guanine nucleotide binding proteins Gs and Gz. J Neurochem 70: 2459-2467
33. Georgoussi Z, Milligan G, Zioudrou C (1995) Immunoprecipitation of opioid receptor-Goprotein complexes using specifi c GTP-bindingprotein antisera. Biochem J 306:71-75