Identification of key residues in transmembrane 4 responsible for the secondary, low-affinity conformation of the human β1-adrenoceptor

Molecular Pharmacology

Volumn 85, Issue 5, 2014, Pages 811-829

  Baker, Jillian G ^a   Proudman, Richard G W ^a   Hill, Stephen J ^a  

^a UNIVERSITY OF NOTTINGHAM   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

4 (3 TERT BUTYLAMINO 2 HYDROXYPROPOXY) 2 BENZIMIDAZOLONE; ALKALINE PHOSPHATASE PLACENTA ISOENZYME; BETA 1 ADRENERGIC RECEPTOR; BETA 2 ADRENERGIC RECEPTOR; CIMATEROL; PINDOLOL; PROTEIN; TRANSMEMBRANE 4 PROTEIN; UNCLASSIFIED DRUG; BETA ADRENERGIC RECEPTOR BLOCKING AGENT; BETA ADRENERGIC RECEPTOR STIMULATING AGENT;

ACTION POTENTIAL; ANIMAL CELL; ARTICLE; CHO CELL LINE; CONTROLLED STUDY; CYCLIC AMP RESPONSIVE ELEMENT; EC50; ENZYME RELEASE; FEMALE; NONHUMAN; POINT MUTATION; PRIORITY JOURNAL; PROTEIN CONFORMATION; REPORTER GENE; SITE DIRECTED MUTAGENESIS; WILD TYPE; ANIMAL; CHEMISTRY; CRICETULUS; DOSE RESPONSE; HAMSTER; HUMAN; METABOLISM; PROTEIN SECONDARY STRUCTURE;

ADRENERGIC BETA-AGONISTS; ADRENERGIC BETA-ANTAGONISTS; ANIMALS; CHO CELLS; CRICETINAE; CRICETULUS; DOSE-RESPONSE RELATIONSHIP, DRUG; HUMANS; PROTEIN CONFORMATION; PROTEIN STRUCTURE, SECONDARY; RECEPTORS, ADRENERGIC, BETA-1;

EID: 84900458270     PISSN: 0026895X     EISSN: 15210111     Source Type: Journal    
DOI: 10.1124/mol.114.091587     Document Type: Article

References (36)

1. Arch JR (2004) Do low-affinity states of beta-adrenoceptors have roles in physiology and medicine? Br J Pharmacol 143:517-518.
2. Baker JG, Hall IP, and Hill SJ (2002) Pharmacological characterization of CGP 12177 at the human β(2)-adrenoceptor. Br J Pharmacol 137:400-408.
3. Baker JG (2005a) Site of action of β-ligands at the human β1-adrenoceptor. J Pharmacol Exp Ther 313:1163-1171.
4. Baker JG (2005b) Evidence for a secondary state of the human β3-adrenoceptor. Mol Pharmacol 68:1645-1655.
5. Baker JG (2010a) The selectivity of β-adrenoceptor agonists at the human β1, β2 and β3 adrenoceptors. Br J Pharmacol 160:148-161.
6. Baker JG (2010b) A full pharmacological analysis of the three turkey β-adrenoceptors and comparison with the human β-adrenoceptors. PLoS ONE 5:e15487 10.1371/Journal.pone.0015487.
7. Baker JG, Hall IP, and Hill SJ (2003) Agonist actions of "β-blockers" provide evidence for two agonist activation sites or conformations of the human β1-adrenoceptor. Mol Pharmacol 63:1312-1321.
8. Baker JG, Proudman RGW, Hawley NC, Fischer PM, and Hill SJ (2008) Role of key transmembrane residues in agonist and antagonist actions at the two conformations of the human β1-adrenoceptor. Mol Pharmacol 74:1246-1260.
9. Baker JG, Proudman RGW, and Hill SJ (2013) Impact of polymorphic variants on the molecular pharmacology of the two-agonist conformations of the human β1-adrenoceptor. PLoS ONE 8:e77582.
10. Granneman JG (2001) The putative beta4-adrenergic receptor is a novel state of the beta1-adrenergic receptor. Am J Physiol Endocrinol Metab 280:E199-E202.
11. Huang J, Chen S, Zhang JJ, and Huang XY (2013) Crystal structure of oligomeric β1-adrenergic G protein-coupled receptors in ligand-free basal state. Nat Struct Mol Biol 20:419-425.
12. Isogaya M, Sugimoto Y, Tanimura R, Tanaka R, Kikkawa H, Nagao T, and Kurose H (1999) Binding pockets of the beta(1)- and beta(2)-adrenergic receptors for subtype-selective agonists. Mol Pharmacol 56:875-885.
13. Joseph SS, Lynham JA, Molenaar P, Grace AA, Colledge WH, and Kaumann AJ (2003) Intrinsic sympathomimetic activity of (-)-pindolol mediated through a (-)- propranolol-resistant site of the beta1-adrenoceptor in human atrium and recombinant receptors. Naunyn Schmiedebergs Arch Pharmacol 368:496-503.
14. Joseph SS, Lynham JA, Colledge WH, and Kaumann AJ (2004a) Binding of (-)-[3H]-CGP12177 at two sites in recombinant human beta 1-adrenoceptors and interaction with beta-blockers. Naunyn Schmiedebergs Arch Pharmacol 369:525-532.
15. Joseph SS, Colledge WH, and Kaumann AJ (2004b) Aspartate138 is required for the high-affinity ligand binding site but not for the low-affinity binding site of the beta1-adrenoceptor. Naunyn Schmiedebergs Arch Pharmacol 370:223-226.
16. Kaumann AJ (1973) Adrenergic receptors of cardiac muscle. Two different mechanisms of β-blockers as partial agonists. Acta Physiol Lat Am 23:619-620.
17. Kaumann AJ (1983) Cardiac β receptors - experimental aspects [in German]. Z Kardiol 72:63-82.
18. Kaumann AJ and Blinks JR (1980) beta-Adrenoceptor blocking agents as partial agonists in isolated heart muscle: dissociation of stimulation and blockade. Naunyn Schmiedebergs Arch Pharmacol 311:237-248.
19. Kaumann AJ, Engelhardt S, Hein L, Molenaar P, and Lohse M (2001) Abolition of (-)-CGP 12177-evoked cardiostimulation in double beta1/beta2-adrenoceptor knockout mice. Obligatory role of beta1-adrenoceptors for putative beta4-adrenoceptor pharmacology. Naunyn Schmiedebergs Arch Pharmacol 363:87-93.
20. Kaumann AJ and Molenaar P (2008) The low-affinity site of the beta1-adrenoceptor and its relevance to cardiovascular pharmacology. Pharmacol Ther 118:303-336.
21. Kompa AR and Summers RJ (1999) Desensitization and resensitization of beta 1- and putative beta 4-adrenoceptor mediated responses occur in parallel in a rat model of cardiac failure. Br J Pharmacol 128:1399-1406.
22. Konkar AA, Zhu Z, and Granneman JG (2000) Aryloxypropanolamine and catecholamine ligand interactions with the β(1)-adrenergic receptor: evidence for interaction with distinct conformations of β(1)-adrenergic receptors. J Pharmacol Exp Ther 294:923-932.
23. Kozłowska H, Schlicker E, Kozłowski M, Baranowska M, and Malinowska B (2006) Potential involvement of a propranolol-insensitive atypical beta-adrenoceptor the vasodilator effect of cyanopindolol in the human pulmonary artery. J Physiol Pharmacol 57:317-328.
24. Kozłowska H, Szymska U, Schlicker E, and Malinowska B (2003) Atypical beta-adrenoceptors, different from beta 3-adrenoceptors and probably from the low-affinity state of beta 1-adrenoceptors, relax the rat isolated mesenteric artery. Br J Pharmacol 140:3-12.
25. Lowe MD, Lynham JA, Grace AA, and Kaumann AJ (2002) Comparison of the affinity of β-blockers for two states of the β 1-adrenoceptor in ferret ventricular myocardium. Br J Pharmacol 135:451-461.
26. Malinowska B and Schlicker E (1996) Mediation of the positive chronotropic effect of CGP 12177 and cyanopindolol in the pithed rat by atypical beta-adrenoceptors, different from beta 3-adrenoceptors. Br J Pharmacol 117:943-949.
27. Mallem MY, Toumaniantz G, Serpillon S, Gautier F, Gogny M, Desfontis JC, and Gauthier C (2004) Impairment of the low-affinity state beta1-adrenoceptor-induced relaxation in spontaneously hypertensive rats. Br J Pharmacol 143: 599-605.
28. Molenaar P (2003) The 'state' of beta-adrenoceptors. Br J Pharmacol 140:1-2.
29. Molenaar P, Chen L, Semmler AB, Parsonage WA, and Kaumann AJ (2007) Human heart beta-adrenoceptors: beta1-adrenoceptor diversification through 'affinity states' and polymorphism. Clin Exp Pharmacol Physiol 34:1020-1028.
30. Pak MD and Fishman PH (1996) Anomalous behavior of CGP 12177A on beta 1-adrenergic receptors. J Recept Signal Transduct Res 16:1-23.
31. Sarsero D, Russell FD, Lynham JA, Rabnott G, Yang I, Fong KM, Li L, Kaumann AJ, and Molenaar P (2003) (-)-CGP 12177 increases contractile force and hastens relaxation of human myocardial preparations through a propranolol-resistant state of the beta 1-adrenoceptor. Naunyn Schmiedebergs Arch Pharmacol 367:10-21.
32. Stephenson RP (1956) A modification of receptor theory. Br Pharmacol Chemother 11:379-393.
33. Staehelin M, Simons P, Jaeggi K, and Wigger N (1983) CGP-12177. A hydrophilic beta-adrenergic receptor radioligand reveals high affinity binding of agonists to intact cells. J Biol Chem 258:3496-3502.
34. Sawangkoon S, Miyamoto M, Nakayama T, and Hamlin RL (2000) Acute cardiovascular effects and pharmacokinetics of carvedilol in healthy dogs. Am J Vet Res 61:57-60.
35. Walter M, Lemoine H, and Kaumann AJ (1984) Stimulant and blocking effects of optical isomers of pindolol on the sinoatrial node and trachea of guinea pig. Role of beta-adrenoceptor subtypes in the dissociation between blockade and stimulation. Naunyn Schmiedebergs Arch Pharmacol 327:159-175.
36. Zakrzeska A, Schlicker E, Kwolek G, Kozłowska H, and Malinowska B (2005) Positive inotropic and lusitropic effects mediated via the low-affinity state of beta1-adrenoceptors in pithed rats. Br J Pharmacol 146:760-768.