Identification of transmembrane domain 6 & 7 residues that contribute to the binding pocket of the urotensin II receptor

Biochemical Pharmacology

Volumn 77, Issue 8, 2009, Pages 1374-1382

  Holleran, Brian J ^a   Domazet, Ivana ^a   Beaulieu, Marie Eve ^a   Yan, Li Ping ^a   Guillemette, Gaétan ^a   Lavigne, Pierre ^a   Escher, Emanuel ^a   Leduc, Richard ^a  

^a UNIVERSITY OF SHERBROOKE   (Canada)

Author keywords

GPCR; Ligand binding pocket; Substituted cysteine accessibility method; Urotensin II; Urotensin II receptor

Indexed keywords

CYSTEINE; G PROTEIN COUPLED RECEPTOR; METHANETHIOSULFONATE ETHYLAMMONIUM; METHANETHIOSULFONATE ETHYLSULFONATE; UNCLASSIFIED DRUG; UROTENSIN II; UROTENSIN II RECEPTOR;

ANIMAL CELL; ARTICLE; CELL CULTURE; CELL STRAIN COS7; CONTROLLED STUDY; MOLECULAR MODEL; NONHUMAN; NUCLEOTIDE SEQUENCE; PRIORITY JOURNAL; RECEPTOR BINDING;

EID: 62549120729     PISSN: 00062952     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bcp.2009.01.013     Document Type: Article

References (36)

1. Akabas M.H., Stauffer D.A., Xu M., and Karlin A. Acetylcholine receptor channel structure probed in cysteine-substitution mutants. Science 258 (1992) 307-310
2. Ames R.S., Sarau H.M., Chambers J.K., Willette R.N., Aiyar N.V., Romanic A.M., et al. Human urotensin-II is a potent vasoconstrictor and agonist for the orphan receptor GPR14. Nature 401 (1999) 282-286
3. Boucard A.A., Roy M., Beaulieu M.E., Lavigne P., Escher E., Guillemette G., et al. Constitutive activation of the angiotensin II type 1 receptor alters the spatial proximity of transmembrane 7 to the ligand-binding pocket. J Biol Chem 278 (2003) 36628-36636
4. Boucard A.A., Sauve S.S., Guillemette G., Escher E., and Leduc R. Photolabelling the rat urotensin II/GPR14 receptor identifies a ligand-binding site in the fourth transmembrane domain. Biochem J 370 (2003) 829-838
5. Carotenuto A., Grieco P., Campiglia P., Novellino E., and Rovero P. Unraveling the active conformation of urotensin II. J Med Chem 47 (2004) 1652-1661
6. Chen S., Lin F., Xu M., Riek R.P., Novotny J., and Graham R.M. Mutation of a single TMVI residue, Phe(282), in the beta(2)-adrenergic receptor results in structurally distinct activated receptor conformations. Biochemistry 41 (2002) 6045-6053
7. Cherezov V., Rosenbaum D.M., Hanson M.A., Rasmussen S.G., Thian F.S., Kobilka T.S., et al. High-resolution crystal structure of an engineered human beta2-adrenergic G protein-coupled receptor. Science 318 (2007) 1258-1265
8. Clement M., Martin S.S., Beaulieu M.E., Chamberland C., Lavigne P., Leduc R., et al. Determining the environment of the ligand binding pocket of the human angiotensin II type I (hAT1) receptor using the methionine proximity assay. J Biol Chem 280 (2005) 27121-27129
9. Coulouarn Y., Jegou S., Tostivint H., Vaudry H., and Lihrmann I. Cloning, sequence analysis and tissue distribution of the mouse and rat urotensin II precursors. FEBS Lett 457 (1999) 28-32
10. Coulouarn Y., Lihrmann I., Jegou S., Anouar Y., Tostivint H., Beauvillain J.C., et al. Cloning of the cDNA encoding the urotensin II precursor in frog and human reveals intense expression of the urotensin II gene in motoneurons of the spinal cord. Proc Natl Acad Sci USA 95 (1998) 15803-15808
11. Dauber-Osguthorpe P., Roberts V.A., Osguthorpe D.J., Wolff J., Genest M., and Hagler A.T. Structure and energetics of ligand binding to proteins: Escherichia coli dihydrofolate reductase-trimethoprim, a drug-receptor system. Proteins 4 (1988) 31-47
12. Dawson E.S., and Wells J.N. Determination of amino acid residues that are accessible from the ligand binding crevice in the seventh transmembrane-spanning region of the human A(1) adenosine receptor. Mol Pharmacol 59 (2001) 1187-1195
13. DeLano W.L. The PyMOL molecular graphics system (2002), Delano Scientific, San Carlos, CA
14. Desai N., Sajjad J., and Frishman W.H. Urotensin II: a new pharmacologic target in the treatment of cardiovascular disease. Cardiol Rev 16 (2008) 142-153
15. Douglas S.A. Human urotensin-II as a novel cardiovascular target: 'heart' of the matter or simply a fishy 'tail'?. Curr Opin Pharmacol 3 (2003) 159-167
16. Fraker P.J., and Speck Jr. J.C. Protein and cell membrane iodinations with a sparingly soluble chloroamide 1,3,4,6-tetrachloro-3a,6a-diphrenylglycoluril. Biochem Biophys Res Commun 80 (1978) 849-857
17. Fu D., Ballesteros J.A., Weinstein H., Chen J., and Javitch J.A. Residues in the seventh membrane-spanning segment of the dopamine D2 receptor accessible in the binding-site crevice. Biochemistry 35 (1996) 11278-11285
18. Holleran B.J., Beaulieu M.E., Proulx C.D., Lavigne P., Escher E., and Leduc R. Photolabelling the urotensin II receptor reveals distinct agonist- and partial-agonist-binding sites. Biochem J 402 (2007) 51-61
19. Jaakola V.P., Griffith M.T., Hanson M.A., Cherezov V., Chien E.Y., Lane J.R., et al. The 2.6 Angstrom crystal structure of a human A2A adenosine receptor bound to an antagonist. Science (2008)
20. Javitch J.A., Ballesteros J.A., Weinstein H., and Chen J. A cluster of aromatic residues in the sixth membrane-spanning segment of the dopamine D2 receptor is accessible in the binding-site crevice. Biochemistry 37 (1998) 998-1006
21. Javitch J.A., Li X., Kaback J., and Karlin A. A cysteine residue in the third membrane-spanning segment of the human D2 dopamine receptor is exposed in the binding-site crevice. Proc Natl Acad Sci USA 91 (1994) 10355-10359
22. Javitch J.A., Shi L., and Liapakis G. Use of the substituted cysteine accessibility method to study the structure and function of G protein-coupled receptors. Methods Enzymol 343 (2002) 137-156
23. Kinney W.A., Almond Jr. H.R., Qi J., Smith C.E., Santulli R.J., de Garavilla L., et al. Structure-function analysis of urotensin II and its use in the construction of a ligand-receptor working model. Angew Chem Int Ed Engl 41 (2002) 2940-2944
24. Martin S.S., Boucard A.A., Clement M., Escher E., Leduc R., and Guillemette G. Analysis of the third transmembrane domain of the human type 1 angiotensin II receptor by cysteine scanning mutagenesis. J Biol Chem 279 (2004) 51415-51423
25. Martin S.S., Holleran B.J., Escher E., Guillemette G., and Leduc R. Activation of the angiotensin II type 1 receptor leads to movement of the sixth transmembrane domain: analysis by the substituted cysteine accessibility method. Mol Pharmacol 72 (2007) 182-190
26. Ong K.L., Lam K.S., and Cheung B.M. Urotensin II: its function in health and its role in disease. Cardiovasc Drugs Ther 19 (2005) 65-75
27. Palczewski K., Kumasaka T., Hori T., Behnke C.A., Motoshima H., Fox B.A., et al. Crystal structure of rhodopsin: A G protein-coupled receptor. Science 289 (2000) 739-745
28. Papadopoulos P., Bousette N., and Giaid A. Urotensin-II and cardiovascular remodeling. Peptides 29 (2008) 764-769
29. Park J.H., Scheerer P., Hofmann K.P., Choe H.W., and Ernst O.P. Crystal structure of the ligand-free G-protein-coupled receptor opsin. Nature 454 (2008) 183-187
30. Pearson D., Shively J.E., Clark B.R., Geschwind I.I., Barkley M., Nishioka R.S., et al. Urotensin II: a somatostatin-like peptide in the caudal neurosecretory system of fishes. Proc Natl Acad Sci USA 77 (1980) 5021-5024
31. Proulx C.D., Holleran B.J., Lavigne P., Escher E., Guillemette G., and Leduc R. Biological properties and functional determinants of the urotensin II receptor. Peptides 29 (2008) 691-699
32. Schwartz T.W., Frimurer T.M., Holst B., Rosenkilde M.M., and Elling C.E. Molecular mechanism of 7TM receptor activation-a global toggle switch model. Annu Rev Pharmacol Toxicol 46 (2006) 481-519
33. Smit M.J., Vischer H.F., Bakker R.A., Jongejan A., Timmerman H., Pardo L., et al. Pharmacogenomic and structural analysis of constitutive g protein-coupled receptor activity. Annu Rev Pharmacol Toxicol 47 (2007) 53-87
34. Warne T., Serrano-Vega M.J., Baker J.G., Moukhametzianov R., Edwards P.C., Henderson R., et al. Structure of a beta1-adrenergic G-protein-coupled receptor. Nature 454 (2008) 486-491
35. Xu W., Campillo M., Pardo L., Kim de Riel J., and Liu-Chen L.Y. The seventh transmembrane domains of the delta and kappa opioid receptors have different accessibility patterns and interhelical interactions. Biochemistry 44 (2005) 16014-16025
36. Xu W., Li J., Chen C., Huang P., Weinstein H., Javitch J.A., et al. Comparison of the amino acid residues in the sixth transmembrane domains accessible in the binding-site crevices of mu, delta, and kappa opioid receptors. Biochemistry 40 (2001) 8018-8029