Binding pockets of the β1- and β1-adrenergic receptors for subtype- selective agonists

Molecular Pharmacology

Volumn 56, Issue 5, 1999, Pages 875-885

  Isogaya, Masafumi ^a,b   Sugimoto, Yoshiyuki ^a   Tanimura, Ryuji ^b   Tanaka, Rie ^a   Kikkawa, Hideo ^a,c   Nagao, Taku ^a   Kurose, Hitoshi ^a  

^a UNIVERSITY OF TOKYO   (Japan)

^b TORAY INDUSTRIES INC   (Japan)

^c MITSUBISHI TANABE PHARMA CORPORATION   (Japan)

Author keywords

[No Author keywords available]

Indexed keywords

3 HYDROXYDENOPAMINE; ALANINE; BETA 1 ADRENERGIC RECEPTOR; BETA 2 ADRENERGIC RECEPTOR; BETA ADRENERGIC RECEPTOR STIMULATING AGENT; DENOPAMINE; FORMOTEROL; PROCATEROL; PROPRANOLOL; RECEPTOR SUBTYPE; RHODOPSIN; TYROSINE;

ADRENERGIC SYSTEM; ARTICLE; BINDING AFFINITY; DRUG RECEPTOR BINDING; DRUG SELECTIVITY; HUMAN; HUMAN CELL; HYDROGEN BOND; PRIORITY JOURNAL; RECEPTOR INTRINSIC ACTIVITY;

EID: 0032726893     PISSN: 0026895X     EISSN: None     Source Type: Journal    
DOI: 10.1124/mol.56.5.875     Document Type: Article

References (29)

1. Abdulaev NG and Ridge KD (1998) Light-induced exposure of the cytoplasmic end of transmembrane helix seven in rhodopsin. Proc Natl Acad Sci USA 95:12854-12859.
2. Baldwin JM, Schertler GFX and Unger VM (1997) An α-carbon template for the transmembrane helices in the rhodopsin family of G-protein-coupled receptors. J Mol Biol 272:144-164.
3. Ballesteros J, Kitanovic S, Guarnieri F, Davies P, Fromme BJ, Konvicka K, Chi L, Millar RP, Davidson JS, Weinstein H and Sealfon SC (1998) Functional microdomains in G-protein-coupled receptors. The conserved arginine-cage motif in the gonadotropin-releasing hormone receptor. J Biol Chem 273:10445-10453.
4. Clackson T and Wells JA (1995) A hot spot of binding energy in a hormone-receptor interface. Science 267:383-386.
5. Cullen BR (1987) Use of eukaryotic expression technology in the functional analysis of cloned genes. Methods Enzymol 152:684-704.
6. Desmet J, De Maeyer M, Hazes B and Lasters I (1992) The dead-end elimination theorem and its use in protein side-chain positioning. Nature (Lond) 356:539-542.
7. Dixon RAF, Hill WS, Candelore MR, Rands E, Diehl RE, Marshall MS, Sigal IS and Strader CD (1989) Genetic analysis of the molecular basis for β-adrenergic receptor subtype specificity. Proteins 6:267-274.
8. Dixon RAF, Sigal IS, Rands E, Register RB, Canderolore MR, Blak AD and Strader CD (1987) Ligand binding to the β-adrenergic receptor involves its rhodopsin-like core. Nature (Lond) 326:73-77.
9. 2-adrenergic receptor. Biochemistry 27:1813-1817.
10. 2-adrenergic receptors. Proc Natl Acad Sci USA 85:9494-9498.
11. Higuchi R (1989) Using PCR to engineer DNA, in PCR Technology (Erlich HA ed) pp 61-70, Stockton Press, New York.
12. 2-adrenergic receptor ligand binding pocket. Mol Pharmacol 49:1021-1032.
13. Holst B, Zoffmann S, Elling CE, Hjorth SA and Schwartz TW (1998) Steric hindrance mutagenesis versus alanine scan in mapping of ligand binding sites in the tachykinin NK1 receptor. Mol Pharmacol 53:166-175.
14. 2-adrenergic receptor for high affinity binding of salmeterol. Mol Pharmacol 54:616-622.
15. 2-selective agonist TA-2005. Mol Pharmacol 53:128-134.
16. Lowry OH, Rosebrough NJ, Fair AL and Randall RJ (1951) Protein measurement with the Folin phenol reagent. J Biol Chem 193:265-275.
17. 2-adrenergic receptors involves multiple subsites. EMBO J 9:1471-1476.
18. Perlman JH, Colson A-O, Wang W, Bence K, Osman R and Gershengorn MC (1997) Interactions between conserved residues in transmembrane helices 1, 2, and 7 of the thyrotropin-releasing hormone receptor. J Biol Chem 272:11937-11942.
19. Sanger F, Nicklen S and Coulson AR (1977) DNA sequencing with chain-terminating inhibitors. Proc Natl Acad Sci USA 74:5463-5467.
20. Savarese TM and Fraser CM (1992) In vitro mutagenesis and the search for structure-function relationships among G protein-coupled receptors. Biochem J 283:1-19.
21. 2A receptor. J Biol Chem 270:16683-16688.
22. Strader CD, Candelore MR, Hill WS, Sigal IS and Dixon RAF (1989) Identification of two serine residues involved in agonist activation of the β-adrenergic receptor. J Biol Chem 264:13572-13578.
23. Strader CD, Fong TM, Tota MR and Underwood D (1994) Structure and function of G protein-coupled receptors. Annu Rev Biochem 63:101-132.
24. Strader CD, Sigal IS, Candelore MR, Rands E, Hill WS and Dixon RAF (1988) Conserved aspartic acid residues 79 and 113 of the β-adrenergic receptor have different roles in receptor function. J Biol Chem 263:10267-10271.
25. Tanimura R, Kidera A and Nakamura H (1994) Determinants of protein side-chain packing. Protein Science 3:2358-2365.
26. Wess J, Nanavati S, Vogel Z and Maggio R (1993) Functional role of proline and tryptophan residues highly conserved among G protein-coupled receptors studied by mutational analysis of the m3 muscarinic receptor. EMBO J 12:331-338.
27. 2-adrenergic receptor. Proc Natl Acad Sci USA 93:9276-9281.
28. Wong SK-F, Slaughter C, Ruoho AE and Ross EM (1988) The catecholamine binding site of the β-adrenergic receptor is formed by juxtaposed membrane-spanning domains. J Biol Chem 263:7925-7928.
29. Zhou W, Flanagan C, Ballesteros JA, Konvicka K, Davidson JS, Weinstein H, Millar RP and Sealfon SC (1994) A reciprocal mutation supports helix 2 and helix 7 proximity in the gonadotropin-releasing hormone receptor. Mol Pharmacol 45: 165-170.