Ser165 of transmembrane helix iv is not involved in the interaction of catecholamines with the alpha-2a-adrenoceptor

Pharmacology

Volumn 55, Issue 1, 1997, Pages 18-24

  Hehr, Andreas ^a   Hieble, J Paul ^a   Li, Ying Ou ^a   Bergsma, Derk J ^a   Swift, Ann M ^a   Ganguly, Subinay ^a   Ruffolo, Robert R ^a  

^a GLAXOSMITHKLINE   (United Kingdom)

Author keywords

Easson Stedman hypothesis, site directed; Mutagenesis Clonidine; Norepinephrine

Indexed keywords

ADRENALIN; ALANINE; ALPHA 2 ADRENERGIC RECEPTOR; CATECHOLAMINE; DOPAMINE; NORADRENALIN; SERINE; ALPHA 2A ADRENERGIC RECEPTOR; BETA 2 ADRENERGIC RECEPTOR; CYSTEINE; HYDROXYL GROUP; MEMBRANE PROTEIN; RECEPTOR SUBTYPE;

ANIMAL; ARTICLE; CELL STRAIN COS1; CHEMICAL STRUCTURE; CHEMISTRY; GENETICS; HUMAN; METABOLISM; MUTATION; RADIOASSAY; SITE DIRECTED MUTAGENESIS; AMINO ACID SUBSTITUTION; ANIMAL CELL; CONTROLLED STUDY; MOLECULAR MODEL; NONHUMAN; PRIORITY JOURNAL; RECEPTOR AFFINITY; RECEPTOR BINDING; STEREOCHEMISTRY;

ALANINE; ANIMALS; CATECHOLAMINES; COS CELLS; DOPAMINE; EPINEPHRINE; HUMANS; MODELS, MOLECULAR; MUTAGENESIS, SITE-DIRECTED; MUTATION; NOREPINEPHRINE; RADIOLIGAND ASSAY; RECEPTORS, ADRENERGIC, ALPHA-2; SERINE;

EID: 0030608863     PISSN: 00317012     EISSN: 14230313     Source Type: Journal    
DOI: 10.1159/000139508     Document Type: Article

References (20)

1. Strader CD, Fong TM, Tota MR. Underwood D: Structure and function of G protein coupled receptors. Annu Rev Biochcm 1994:63:101-132.
2. Donnelly D. Findlay JBC. Blundell TL: The evolution and structure of aminergic G protein-coupled receptors. Receptors Gtannels 1994:2: 61-78.
3. Trumpp-Kallmeycr S. Hoflack J. Bruinvcls A, Hibcrt M: Modeling of G-protein-couplcd receptors: Application to dopamine, adrenaline, serotonin, acetylcholine and mammalian opsin receptors. J Med Chem 1992;35:3448-3462.
4. Strader CD, Sigal IS, Candclorc MR. Rands E, Hill WS, Dixon RAF: Conserved aspartic acid residues 79 and 113 of the P-adrenergic receptor have different roles in receptor function. J Biol Chem 1988:263:10267-10271.
5. A-adrenergic receptors: Identification of amino acids involved in ligand binding and receptor activation by agonists. Mol Pharmacol 1991:40: 168-179.
6. Strader CD, Candelore MR. Hill WS. Sigal IS, Dixon RAF: Identification of two serine residues involved in agonist activation of the p adrenergic receptor. J Biol Chem 1989:264:13572-13578.
7. Lee NH. Pellegrino SM. Fraser CM: Site-directed mutagenesis of a-adrenergic receptors. Neuroprotocols 1994;4:20-31.
8. Ruffolo RR Jr. Stadel JM, Hieble JP: «-Adrenoceptors: Recent developments. Med Res Rev 1994:14: 229-270.
9. Easson LH. Stedman E: Studies on the relationship between chemical constitution and physiological action. V. Molecular dyssemetry and physiological activity. Biochem J 1933;27:1257-1266.
10. Strosberg AD: Structure, function and regulation of adrenergic receptors. Protein Sei 1993:2:1198-1209.
11. Maloney-Huss K. Lybrand TP: Three-dimensional structure for the p2-adrcncrgic receptor protein based on computer modeling studies. J Mol Biol 1992:225:859-871.
12. Wieland K, Ijzerman AP. Lohse MJ: Involvement of asparaginc-292 in the human beta-2 adrenergic in stereospecific agonist binding. Arch Pharmacol 1994:349(suppl):R10.
13. 90 of the second transmembranc helix of the as» adrenoceptor. Pharmacol Commun 1995:6:125-131.
14. Aiyar N. Bayer E, Wu H-L, Nambi P. Edwards RM. Trill JJ, Ellis C. Bergsma DJ: Human AT-1 receptor is a single copy gene: Characterization in a stable cell line. Mol Cell Biochcm 1994:131:75-86.
15. McCutchan JH. Pagano JS: Enhancement of the infectivity of simian virus 40 deoxyribonucleic acid with dethylaminoethyl-dextran. J Natl Cancer Inst 1968:41:351-357.
16. a-adre-noceptor vis site directed mutagenesis; in Lanier SM, Limbird LE (eds): «2-Adrcnergic Receptors: Structure. Function and Therapeutic Implications. New York. Harwood Academic Publishers, 1996. pp 43-51.
17. Nimit Y. Cantacuzcne D, Kink KL. Creveling CR. Daly JW: The binding of lluorocatecholamines to adrenergic and dopaminergic receptors in rat brain membranes. Life Sei 1980;27:1577-1585.
18. Kohli JD. Volkman PH. Goldberg LI. Cannon JG: Conformational requirements for vascular a-adrener-gic activity. Proc Soc Exp Biol Med 1978;158:28-31.
19. Volkman PH. Kohli JD. Goldberg LI, Cannon JG. Lee T: Conformational requirements for dopamine-induced vasodilation. Proc Natl Acad Sci USA 1977;74:3602-3606.
20. Macchia B. Balsamo A, Breschi MC. Lapucci A. Lucacchini A, Macchia F. Manera C. Martinelli A. Martini C, Martinotti E, Nencetti S: Conformational effects on the activity of drugs. 13. A revision of previously proposed models for the activation of a and P-adrenergic receptors. J Med Chem 1992:35:1009-1018.