The effect of ligand efficacy on the formation and stability of a GPCR-G protein complex

Proceedings of the National Academy of Sciences of the United States of America

Volumn 106, Issue 23, 2009, Pages 9501-9506

  Xiao, Jie Yao ^a   Ruiz, Gisselle Vélez ^b   Whorton, Matthew R ^b   Rasmussen, Søren G F ^a   DeVree, Brian T ^b   Deupi, Xavier ^c   Sunahara, Roger K ^b   Kobilka, Brian ^a  

^a STANFORD UNIVERSITY SCHOOL OF MEDICINE   (United States)

^b UNIVERSITY OF MICHIGAN MEDICAL SCHOOL   (United States)

^c UNIVERSITAT AUTÒNOMA DE BARCELONA   (Spain)

Author keywords

Adrenergic; Conformation; Constitutive activity; Inverse agonist; Receptor

Indexed keywords

BETA 2 ADRENERGIC RECEPTOR; G PROTEIN COUPLED RECEPTOR; GUANINE NUCLEOTIDE; GUANINE NUCLEOTIDE BINDING PROTEIN; HIGH DENSITY LIPOPROTEIN; ISOPRENALINE;

ARTICLE; COMPLEX FORMATION; CONFORMATIONAL TRANSITION; PRIORITY JOURNAL; PROTEIN PROTEIN INTERACTION; PROTEIN STABILITY; SIGNAL TRANSDUCTION; STOICHIOMETRY;

BICYCLO COMPOUNDS; GTP-BINDING PROTEINS; HUMANS; LIGANDS; PROTEIN STABILITY; RECEPTORS, ADRENERGIC, BETA-2; SIGNAL TRANSDUCTION;

EID: 67249125561     PISSN: 00278424     EISSN: 10916490     Source Type: Journal    
DOI: 10.1073/pnas.0811437106     Document Type: Article

References (50)

1. Lefkowitz RJ, Shenoy SK (2005) Transduction of receptor signals by beta-arrestins. Science 308:512-517.
2. Luttrell LM, Lefkowitz RJ (2002) The role of beta-arrestins in the termination and transduction of G-protein-coupled receptor signals. J Cell Sci 115:455-465. (Pubitemid 34182973)
3. Azzi M, et al. (2003) Beta-arrestin-mediated activation of MAPK by inverse agonists reveals distinct active conformations for G protein-coupled receptors. Proc Natl Acad Sci USA 100:11406-11411. (Pubitemid 37205948)
4. sα. Science 278:1943-1947.
5. Sondek J, Lambright DG, Noel JP, Hamm HE, Sigler PB (1994) GTPase mechanism of G-proteins from the 1.7-Å crystal structure of transducin α-GDP AIF-4. Nature 372:276-279. (Pubitemid 2152279)
6. Kreutz B, et al. (2006) A new approach to producing functional G alpha subunits yields the activated and deactivated structures of G alpha(12/13) proteins. Biochemistry 45:167-174. (Pubitemid 43054094)
7. Palczewski K, et al. (2000) Crystal structure of rhodopsin: A G protein-coupled receptor. Science 289:739-745. (Pubitemid 30650186)
8. Okada T, et al. (2000) X-ray diffraction analysis of three-dimensional crystals of bovine rhodopsin obtained from mixed micelles. J Struct Biol 130:73-80. (Pubitemid 30470799)
9. Okada T, et al. (2002) Functional role of internal water molecules in rhodopsin revealed by X-ray crystallography. Proc Natl Acad Sci USA 99:5982-5987. (Pubitemid 34493251)
10. Teller DC, Okada T, Behnke CA, Palczewski K, Stenkamp RE (2001) Advances in determination of a high-resolution three-dimensional structure of rhodopsin, a model of G-protein-coupled receptors (GPCRs). Biochemistry 40:7761-7772. (Pubitemid 32622966)
11. Okada T, et al. (2004) The retinal conformation and its environment in rhodopsin in light of a new 2.2 Å crystal structure. J Mol Biol 342:571-583. (Pubitemid 39149759)
12. Li J, Edwards PC, Burghammer M, Villa C, Schertler GF (2004) Structure of bovine rhodopsin in a trigonal crystal form. J Mol Biol 343:1409-1438. (Pubitemid 39387834)
13. Murakami M, Kouyama T (2008) Crystal structure of squid rhodopsin. Nature 453:363-367. (Pubitemid 351693128)
14. Shimamura T, et al. (2008) Crystal structure of squid rhodopsin with intracellularly extended cytoplasmic region. J Biol Chem 283:17753-17756.
15. Park JH, Scheerer P, Hofmann KP, Choe HW, Ernst OP (2008) Crystal structure of the ligand-free G-protein-coupled receptor opsin. Nature 454:183-187. (Pubitemid 351969893)
16. Scheerer P, et al. (2008) Crystal structure of opsin in its G-protein-interacting conformation. Nature 455:497-502.
17. 2 adrenergic G-protein-coupled receptor. Nature 450:383-387.
18. 2-adrenergic receptor function. Science 318:1266-1273.
19. 2-adrenergic G protein-coupled receptor. Science 318:1258-1265.
20. 1-adrenergic G-protein-coupled receptor. Nature 454:486-491.
21. 2A adenosine receptor bound to an antagonist. Science 322:1211-1217.
22. Ross EM, Maguire ME, Sturgill TW, Biltonen RL, Gilman AG (1977) Relationship between the β-adrenergic receptor and adenylate cyclase. Studies of ligand binding and enzyme activity in purified membranes of S49 lymphoma cells. J Biol Chem 252:5761-5775. (Pubitemid 8177752)
23. De Lean A, Stadel JM, Lefkowitz RJ (1980) A ternary complex model explains the agonist-specific binding properties of the adenylate cyclase-coupled beta-adrenergic receptor. J Biol Chem 255:7108-7117. (Pubitemid 11232874)
24. sα has properties of a constitutively active receptor. J Biol Chem 273:5109-5116.
25. Hein P, Frank M, Hoffmann C, Lohse MJ, Bunemann M (2005) Dynamics of receptor/G protein coupling in living cells. EMBO J 24:4106-4114. (Pubitemid 41752879)
26. Nobles M, Benians A, Tinker A (2005) Heterotrimeric G proteins precouple with G protein-coupled receptors in living cells. Proc Natl Acad Sci USA 102:18706-18711. (Pubitemid 43011290)
27. Gales C, et al. (2005) Real-time monitoring of receptor and G-protein interactions in living cells. Nat Methods 2:177-184. (Pubitemid 41122124)
28. Peveri P, Heyworth PG, Curnutte JT (1992) Absolute requirement for GTP in activation of human neutrophil NADPH oxidase in a cell-free system: Role of ATP in regenerating GTP. Proc Natl Acad Sci USA 89:2494-2498.
29. McKee EE, Bentley AT, Smith RM, Jr, Ciaccio CE (1999) Origin of guanine nucleotides in isolated heart mitochondria. Biochem Biophys Res Commun 257:466-472. (Pubitemid 29301467)
30. Kenakin TP (2008) Pharmacological onomastics: What's in a name? Br J Pharmacol 153:432-438.
31. Whorton MR, et al. (2007) A monomeric G protein-coupled receptor isolated in a high-density lipoprotein particle efficiently activates its G protein. Proc Natl Acad Sci USA 104:7682-7687. (Pubitemid 47185966)
32. 2 adrenergic receptor. Proc Natl Acad Sci USA 98:5997-6002.
33. 2 adrenoceptor: Kinetic evidence for intermediate conformational states. J Biol Chem 279:686-691.
34. 2 adrenoceptor binding site with catechol reveals differences in binding and activation by agonists and partial agonists. J Biol Chem 280:22165-22171.
35. 2-adrenoceptor. Nat Chem Biol 2:417-422.
36. Altenbach C, Kusnetzow AK, Ernst OP, Hofmann KP, Hubbell WL (2008) High-resolution distance mapping in rhodopsin reveals the pattern of helix movement due to activation. Proc Natl Acad Sci USA 105:7439-7444. (Pubitemid 351830036)
37. 2 adrenoceptor. EMBO J 16:6737-6747.
38. 2 adrenergic receptor mapped by site-selective fluorescent labeling. J Biol Chem 276:9279-9290.
39. 2- adrenergic receptor involves disruption of an ionic lock between the cytoplasmic ends of transmembrane segments 3 and 6. J Biol Chem 276:29171-29177.
40. Chidiac P, Hebert TE, Valiquette M, Dennis M, Bouvier M (1994) Inverse agonist activity of beta-adrenergic antagonists. Mol Pharmacol 45:490-499. (Pubitemid 24094939)
41. Wisler JW, et al. (2007) A unique mechanism of β-blocker action: Carvedilol stimulates β-arrestin signaling. Proc Natl Acad Sci USA 104:16657-16662. (Pubitemid 350211072)
42. 2-adrenoceptor: Insights from fluorescence resonance energy transfer studies. J Biol Chem 282:13895-13905.
43. Vilardaga JP, Steinmeyer R, Harms GS, Lohse MJ (2005) Molecular basis of inverse agonism in a G protein-coupled receptor. Nat Chem Biol 1:25-28.
44. Ghanouni P, et al. (2001) Functionally different agonists induce distinct conformations in the G protein coupling domain of the β2 adrenergic receptor. J Biol Chem 276:24433-24436. (Pubitemid 33659028)
45. 2- adrenergic receptor. Mol Pharmacol 45:390-394.
46. 2- adrenoceptor. Nature 374:272-276.
47. Azzi M, et al. (2001) Allosteric effects of G protein overexpression on the binding of beta-adrenergic ligands with distinct inverse efficacies. Mol Pharmacol 60:999-1007. (Pubitemid 33027435)
48. z. J Biol Chem 270:1734-1741.
49. Ballesteros JA, Weinstein H (1995) Integrated methods for the construction of three-dimensional models and computational probing of structure-function relations in G protein coupled receptors. Meth Neurosci 25:366-428.
50. Dundas J, et al. (2006) CASTp: Computed atlas of surface topography of proteins with structural and topographical mapping of functionally annotated residues. Nucleic Acids Res 34(Web Server issue):W116-W118. (Pubitemid 44529746)