Aspartate138 is required for the high-affinity ligand binding site but not for the low-affinity binding site of the β1-adrenoceptor

Naunyn-Schmiedeberg's Archives of Pharmacology

Volumn 370, Issue 3, 2004, Pages 223-226

  Joseph, Shirin S ^a   Colledge, William H ^a   Kaumann, Alberto J ^a  

^a UNIVERSITY OF CAMBRIDGE   (United Kingdom)

Author keywords

( ) Bupranolol; ( ) CGP12177; ( ) Isoprenaline; Asp138 1 adrenoceptor and Glu138 1 adrenoceptor; Two receptor sites

Indexed keywords

4 (3 TERT BUTYLAMINO 2 HYDROXYPROPOXY) 2 BENZIMIDAZOLONE; ASPARTIC ACID; BETA 1 ADRENERGIC RECEPTOR; BUPRANOLOL; CYCLIC AMP; ISOPRENALINE; PROPRANOLOL;

ADRENERGIC SYSTEM; ALLOSTERISM; AMINO ACID METABOLISM; AMINO ACID SUBSTITUTION; ANIMAL CELL; ARTICLE; BINDING AFFINITY; BINDING SITE; CONTROLLED STUDY; DRUG POTENCY; GENE MUTATION; GENETIC TRANSFECTION; INHIBITION KINETICS; LIGAND BINDING; NONHUMAN; RECEPTOR BINDING; STATISTICAL SIGNIFICANCE;

ADRENERGIC BETA-AGONISTS; ADRENERGIC BETA-ANTAGONISTS; ANIMALS; ASPARTIC ACID; BINDING SITES; BUPRANOLOL; CHO CELLS; CRICETINAE; CRICETULUS; DRUG INTERACTIONS; ISOPROTERENOL; LIGANDS; PROPANOLAMINES; RECEPTORS, ADRENERGIC, BETA-1;

EID: 5444244316     PISSN: 00281298     EISSN: None     Source Type: Journal    
DOI: 10.1007/s00210-004-0962-1     Document Type: Article

References (20)

1. 1-adrenoceptor. Mol Pharmacol 63:1312-1321
2. Barik S (1998) Mutagenesis by megaprimer PCR. In: Horton RM, Tait RC (eds) Genetic engineering with PCR. Horizon Scientific, Wymondham, pp 25-37
3. Bristow MR, Ginsburg R, Minobe W, Cubiciotti RS, Sageman WS, Lurie K, Billingham ME, Harrison DC, Stinson EB (1982) Decreased catecholamine sensitivity and β-adrenergic receptor density in failing human hearts. N Engl J Med 307:205-211
4. Gossen M, Bujard H (1992) Tight control gene expression in mammalian cells by tetracycline responsive promoters. Proc Soc Acad Sci USA 89:5547-5551
5. 1-adrenoceptor in human atrium and recombinant receptors. Naunyn-Schmiedeberg's Arch Pharmacol 368:496-503
6. 1-adrenoceptors and interaction with β-blockers. Naunyn-Schmiedeberg's Arch Pharmacol 369:525-532
7. 1-adrenoceptors. Br J Pharmacol 142:51-56
8. Kaumann AJ (1989) Is there a third heart β-adrenoceptor? Trends Pharmacol Sci 10:316-320
9. Kaumann AJ (1996) (-)-CGP12177-induced increase of human atrial contraction through a putative third β-adrenoceptor. Br J Pharmacol 117:93-98
10. Kaumann AJ (2000) Gs protein coupled receptors in human heart. In: Kenakin T, Angus JA (eds) The pharmacology of functional, biochemical, and recombinant receptor systems. Handbook of experimental pharmacology, vol 148. Springer, Berlin Heidelberg New York, pp 73-116
11. 4-adrenoceptor pharmacology. Naunyn-Schmiedeberg's Arch Pharmacol 363:87-93
12. 3-adrenergic-independent effects of CGP12177 in brown adipose tissue. Mol Pharmacol 57:252-258
13. 1-adrenoceptor in ferret ventricular myocardium. Br J Pharmacol 135:451-461
14. Mason DA, Moore JD, Green SA, Liggett SB (1999) A gain of function polymorphism in a G-protein coupling domain of human beta1-adrenergic receptor. J Biol Chem 274:12670-12674
15. 1-adrenergic receptors. J Recept Signal Transduct Res 16:1-23
16. 3H]-CGP12177 binding. Br J Pharmacol 128:1445-1460
17. 1-adrenoceptor. Naunyn-Schmiedeberg's Arch Pharmacol 367:10-21
18. Strader CD, Sigal IS, Register RB, Candelore MR, Rands E, Dixon EAF (1987) Identification of residues required for ligand binding to the β-adrenergic receptors. Proc Natl Acad Sci USA 84:4384-4388
19. Strader CD, Sigal IS, Candelore MR, Hill WS, 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
20. Strader CD, Candelore MR, Hill WS, Dixon RAF, Sigal IS (1989) A single amino acid substitution in the β-adrenergic receptor promotes partial agonist activity from antagonists. J Biol Chem 264:16470-16477