Influence of the N-terminus and the E2-loop onto the binding kinetics of the antagonist mepyramine and the partial agonist phenoprodifen to H 1R

Biochemical Pharmacology

Volumn 82, Issue 12, 2011, Pages 1910-1918

  Wittmann, Hans Joachim ^a   Seifert, Roland ^b   Strasser, Andrea ^a  

^a UNIVERSITY OF REGENSBURG   (Germany)

^b HANNOVER MEDICAL SCHOOL   (Germany)

Author keywords

Binding kinetics; Extracellular surface; Gibbs energy; Histamine H 1 receptor; Molecular dynamics; Molecular modelling

Indexed keywords

G PROTEIN COUPLED RECEPTOR; GUANINE NUCLEOTIDE BINDING PROTEIN; HISTAMINE H1 RECEPTOR; HISTAMINE H1 RECEPTOR AGONIST; MEPYRAMINE; PHENOPRODIFEN; RADIOLIGAND; UNCLASSIFIED DRUG;

AMINO TERMINAL SEQUENCE; ANIMAL CELL; ANIMAL EXPERIMENT; ARTICLE; BINDING AFFINITY; BINDING KINETICS; CHIMERA; CONTROLLED STUDY; DISSOCIATION CONSTANT; DRUG RECEPTOR BINDING; EXPERIMENTAL GUINEA PIG; INSECT CELL; MOLECULAR DYNAMICS; NONHUMAN; PRIORITY JOURNAL; PROTEIN EXPRESSION; SIMULATION; WILD TYPE;

AMINO ACID SEQUENCE; ANIMALS; CELL LINE; CELL MEMBRANE; HISTAMINE; HISTAMINE AGONISTS; HISTAMINE H1 ANTAGONISTS; IMIDAZOLES; MODELS, MOLECULAR; MOLECULAR STRUCTURE; PROTEIN BINDING; PYRILAMINE; RECEPTORS, HISTAMINE H1; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 80555131116     PISSN: 00062952     EISSN: 18732968     Source Type: Journal    
DOI: 10.1016/j.bcp.2011.09.005     Document Type: Article

References (35)

1. 1-histamine receptor cDNA in chinese hamster ovary cells. Pharmacological characterization of the protein, tissue distribution of messenger RNA and chromosomal localisation of the gene Eur J Biochem 224 1994 489 495 (Pubitemid 24282832)
2. S.M. Foord, T.I. Bonner, R.R. Neubig, E.M. Rosser, J.P. Pin, and A.P. Davenport International union of pharmacology. XLVI. G protein-coupled receptor list Pharmacol Rev 57 2005 279 288 (Pubitemid 41043887)
3. S.J. Hill, C.R. Ganellin, H. Timmerman, J.C. Schwartz, N.P. Shankley, and J.M. Young International union of pharmacology. XIII. Classification of histamine receptors Pharmacol Rev 49 1997 253 278 (Pubitemid 27414915)
4. 1-receptor J Pharmacol Exp Ther 305 2003 1104 1115 (Pubitemid 36617989)
5. 1 receptor Mol Pharmacol 67 2005 1045 1052
6. 1 receptor species isoforms J Pharmacol Exp Ther 324 2008 60 71 (Pubitemid 350294157)
7. 1-receptor J Pharmacol Exp Ther 326 2008 783 791
8. 1-receptor Mol Pharmacol 75 2009 454 465
9. 1-receptor agonists J Med Chem 43 2000 1071 1084 (Pubitemid 30173733)
10. 1-receptor agonists J Med Chem 46 2003 5458 5470 (Pubitemid 37490378)
11. 1-receptor binding pocket of histaprodifens Eur J Pharmacol 487 2004 55 63 (Pubitemid 38368981)
12. 1 receptor Arch Pharm Chem Life Sci 338 2005 248 259 (Pubitemid 40957263)
13. 1-receptor species Mol Inf 29 2010 3333 3341
14. 1 receptor complex with doxepin Nature 475 2011 65 70
15. 2 adrenergic G-protein-coupled receptor Nature 450 2007 383 387 (Pubitemid 350126755)
16. 2 adrenergic receptor-Gs protein complex. Nature, in press, doi:10.1038/nature10361.
17. 1-receptor Mol Pharmacol 76 2009 25 37
18. 3H]mepyramine Neurobiology 75 1978 6290 6294 (Pubitemid 9100993)
19. 1-receptor Mol Pharmacol 23 1982 60 66 (Pubitemid 13110708)
20. 3H]-mepyramine Br J Pharmacol 94 1988 811 822
21. 1 receptors in isolated rabbit arteries Naunyn-Schmiedeberg's Arch Pharmacol 341 1990 316 323 (Pubitemid 20137885)
22. 194 Mol Pharmacol 61 2002 391 399 (Pubitemid 34112814)
23. 1 receptor antagonists Eur J Pharmacol 530 2006 205 214 (Pubitemid 43075490)
24. 4 receptor in receptor activation. Naunyn-Schmiedeberg's Arch Pharmacol, in press, doi:10.1007/s00210- 011-0673-3.
25. M.P. Bokoch, Y. Zou, S.G.F. Rasmussen, C.W. Liu, R. Nygaard, and D.M. Rosenbaum Ligand-specific regulation of the extracellular surface of a G-protein-coupled receptor Nature 463 2010 108 114
26. C. Houston, K. Wenzel-Seifert, T. Bürckstümmer, and R. Seifert The human histamine H2-receptor couples more efficiently to Sf9 insect cell Gs-proteins than to insect cell Gq-proteins: limitations of Sf9 cells for the analysis of receptor/Gq-protein coupling J Neurochem 80 2002 678 696 (Pubitemid 34809976)
27. H.J. Motulsky, and L.C. Mahan The kinetics of competitive radioligand binding predicted by the law of mass action Mol Pharmacol 25 1983 1 9 (Pubitemid 14223246)
28. H. Eyring The activated complex in chemical reactions J Chem Phys 3 1935 107 115
29. K.J. Laidler, and M.C. King The development of transition state theory J Phys Chem 87 1983 2657 2664
30. P. Scheerer, J.H. Park, P.W. Hildebrand, Y.J. Kim, N. Krauß, and H.W. Choe Crystal structure of opsin in its G-protein-interacting conformation Nature 455 2008 497 503
31. Wittmann HJ, Seifert R, Strasser A. Nα-methylated phenylhistamines exhibit affinity to the hH4R - a pharmacological and molecular modelling study. Nauny-Schmiedeberg's Arch Pharmacol, in press, doi:10.1007/s00210-011-0671-5.
32. J.A. Ballesteros, L. Shi, and J.A. Javitch Structural mimicry in G protein-coupled receptors: implications of the high-resolution structure of rhodopsin for structure-function analysis of rhodopsin-like receptors Mol Pharmacol 60 2011 1 19
33. B.K. Kobilka, and X. Deupi Conformational complexity of G-protein-coupled receptors Trends Pharmacol Sci 28 2007 397 406 (Pubitemid 47087966)
34. X. Deupi, and B.K. Kobilka Energy landscapes as a tool to integrate GPCR structure, dynamics and function Physiology (Bethesda) 25 2010 293 303
35. M.C. Peeters, G.J.P. van Westen, Q. Li, and A.P. Ijzerman Importance of the extracellular loops in G protein-coupled receptors for ligand recognition and receptor activation Trends Pharmacol Sci 32 2011 35 42