Molecular pharmacology of histamine H4 receptors

Frontiers in Bioscience

Volumn 17, Issue 6, 2012, Pages 2089-2106

  Nijmeijer, Saskia ^a   De Graaf, Chris ^a   Leurs, Rob ^a   Vischer, Henry F ^a  

^a VU UNIVERSITY AMSTERDAM   (Netherlands)

Author keywords

Dimerization; GPCR; Histamine; Histamine H4 receptor; Inflammation; Review

Indexed keywords

EID: 84860380065     PISSN: 27686701     EISSN: 27686698     Source Type: Journal    
DOI: 10.2741/4039     Document Type: Article

References (111)

1. W. Vogt. Ber. dtsch. chem. Ges., 40 (1907).
2. G. Barger and H. H. Dale: Chemical structure and sympathomimetic action of amines. J Physiol, 41 (1-2), 19-59 (1910).
3. H. H. Dale and P. P. Laidlaw: The physiological action of beta-iminazolylethylamine. J Physiol, 41 (5), 318-44 (1910).
4. J. P. Kinet: The high-affinity IgE receptor (Fc epsilon RI): from physiology to pathology. Annu Rev Immunol, 17, 931-72 (1999).
5. A. S. Ash and H. O. Schild: Receptors mediating some actions of histamine. Br J Pharmacol Chemother, 27 (2), 427-39 (1966).
6. J. W. Black, W. A. Duncan, C. J. Durant, C. R. Ganellin and E. M. Parsons: Definition and antagonism of histamine H 2 -receptors. Nature, 236 (5347), 385-90 (1972).
7. J. M. Arrang, M. Garbarg and J. C. Schwartz: Autoinhibition of brain histamine release mediated by a novel class (H3) of histamine receptor. Nature, 302 (5911), 832-7 (1983). (Pubitemid 13125123)
8. R. Leurs, R. C. Vollinga and H. Timmerman: The medicinal chemistry and therapeutic potentials of ligands of the histamine H3 receptor. Prog Drug Res, 45, 107-65 (1995).
9. T. A. Esbenshade, K. E. Browman, R. S. Bitner, M. Strakhova, M. D. Cowart and J. D. Brioni: The histamine H3 receptor: an attractive target for the treatment of cognitive disorders. Br J Pharmacol, 154 (6), 1166-81 (2008). (Pubitemid 351992052)
10. T. W. Lovenberg, B. L. Roland, S. J. Wilson, X. Jiang, J. Pyati, A. Huvar, M. R. Jackson and M. G. Erlander: Cloning and functional expression of the human histamine H3 receptor. Mol Pharmacol, 55 (6), 1101-7 (1999). (Pubitemid 29252378)
11. T. Nakamura, H. Itadani, Y. Hidaka, M. Ohta and K. Tanaka: Molecular cloning and characterization of a new human histamine receptor, HH4R. Biochem Biophys Res Commun, 279 (2), 615-20 (2000). (Pubitemid 32016763)
12. T. Oda and S. Matsumoto: Identification and characterization of histamine H4 receptor. Nippon Yakurigaku Zasshi, 118 (1), 36-42 (2001).
13. T. Nguyen, D. A. Shapiro, S. R. George, V. Setola, D. K. Lee, R. Cheng, L. Rauser, S. P. Lee, K. R. Lynch, B. L. Roth and B. F. O'Dowd: Discovery of a novel member of the histamine receptor family. Mol Pharmacol, 59 (3), 427- 33 (2001). (Pubitemid 32179919)
14. Y. Zhu, D. Michalovich, H. Wu, K. B. Tan, G. M. Dytko, I. J. Mannan, R. Boyce, J. Alston, L. A. Tierney, X. Li, N. C. Herrity, L. Vawter, H. M. Sarau, R. S. Ames, C. M. Davenport, J. P. Hieble, S. Wilson, D. J. Bergsma and L. R. Fitzgerald: Cloning, expression, and pharmacological characterization of a novel human histamine receptor. Mol Pharmacol, 59 (3), 434-41 (2001). (Pubitemid 32179920)
15. K. L. Morse, J. Behan, T. M. Laz, R. E. West, Jr., S. A. Greenfeder, J. C. Anthes, S. Umland, Y. Wan, R. W. Hipkin, W. Gonsiorek, N. Shin, E. L. Gustafson, X. Qiao, S. Wang, J. A. Hedrick, J. Greene, M. Bayne and F. J. Monsma, Jr.: Cloning and characterization of a novel human histamine receptor. J Pharmacol Exp Ther, 296 (3), 1058-66 (2001). (Pubitemid 32187382)
16. C. Liu, X. Ma, X. Jiang, S. J. Wilson, C. L. Hofstra, J. Blevitt, J. Pyati, X. Li, W. Chai, N. Carruthers and T. W. Lovenberg: Cloning and pharmacological characterization of a fourth histamine receptor (H (4)) expressed in bone marrow. Mol Pharmacol, 59 (3), 420-6 (2001). (Pubitemid 32179918)
17. F. Coge, S. P. Guenin, H. Rique, J. A. Boutin and J. P. Galizzi: Structure and expression of the human histamine H4-receptor gene. Biochem Biophys Res Commun, 284 (2), 301-9 (2001). (Pubitemid 32917975)
18. B. Yu, Y. Shao, P. Li, J. Zhang, Q. Zhong, H. Yang, X. Hu, B. Chen, X. Peng, Q. Wu, Y. Chen, M. Guan, J. Wan and W. Zhang: Copy number variations of the human histamine H4 receptor gene are associated with systemic lupus erythematosus. Br J Dermatol, 163 (5), 935-40 (2010).
19. P. Wiedemann, H. Bonisch, F. Oerters and M. Bruss: Structure of the human histamine H3 receptor gene (HRH3) and identification of naturally occurring variations. J Neural Transm, 109 (4), 443-53 (2002). (Pubitemid 34280403)
20. M. D. De Backer, I. Loonen, P. Verhasselt, J. M. Neefs and W. H. Luyten: Structure of the human histamine H1 receptor gene. Biochem J, 335 ( Pt 3), 663-70 (1998). (Pubitemid 28515422)
21. H. Murakami, G. H. Sun-Wada, M. Matsumoto, T. Nishi, Y. Wada and M. Futai: Human histamine H2 receptor gene: multiple transcription initiation and tissuespecific expression. FEBS Lett, 451 (3), 327-31 (1999). (Pubitemid 29243801)
22. R. M. van Rijn, A. van Marle, P. L. Chazot, E. Langemeijer, Y. Qin, F. C. Shenton, H. D. Lim, O. P. Zuiderveld, K. Sansuk, M. Dy, M. J. Smit, C. P. Tensen, R. A. Bakker and R. Leurs: Cloning and characterization of dominant negative splice variants of the human histamine H4 receptor. Biochem J, 414 (1), 121-31 (2008).
23. B. Yu, Y. Shao, J. Zhang, X. L. Dong, W. L. Liu, H. Yang, L. Liu, M. H. Li, C. F. Yue, Z. Y. Fang, C. Zhang, X. P. Hu, B. C. Chen, Q. Wu, Y. W. Chen, W. Zhang and J. Wan: Polymorphisms in human histamine receptor H4 gene are associated with atopic dermatitis. Br J Dermatol, 162 (5), 1038-43 (2010).
24. C. Liu, S. J. Wilson, C. Kuei and T. W. Lovenberg: Comparison of human, mouse, rat, and guinea pig histamine H4 receptors reveals substantial pharmacological species variation. J Pharmacol Exp Ther, 299 (1), 121-30 (2001). (Pubitemid 32905126)
25. W. Jiang, H. D. Lim, M. Zhang, P. Desai, H. Dai, P. M. Colling, R. Leurs and R. L. Thurmond: Cloning and pharmacological characterization of the dog histamine H4 receptor. Eur J Pharmacol, 592 (1-3), 26-32 (2008).
26. T. Oda, S. Matsumoto, M. Matsumoto, J. Takasaki, M. Kamohara, T. Soga, H. Hiyama, M. Kobori and M. Katoh: Molecular cloning of monkey histamine H4 receptor. J Pharmacol Sci, 98 (3), 319-22 (2005). (Pubitemid 41296414)
27. T. Oda, S. Matsumoto, Y. Masuho, J. Takasaki, M. Matsumoto, M. Kamohara, T. Saito, T. Ohishi, T. Soga, H. Hiyama, H. Matsushime and K. Furuichi: cDNA cloning and characterization of porcine histamine H4 receptor. Biochim Biophys Acta, 1575 (1-3), 135-8 (2002). (Pubitemid 34521787)
28. H. D. Lim, C. De Graaf, W. Jiang, P. Sadek, P. M. McGovern, E. P. Istyastono, R. A. Bakker, I. J. de Esch, R. L. Thurmond and R. Leurs: Molecular determinants of ligand binding to H4R species variants. Mol Pharmacol, 77 (5), 734-43 (2010).
29. W. Baumer, S. Wendorff, R. Gutzmer, T. Werfel, D. Dijkstra, P. Chazot, H. Stark and M. Kietzmann: Histamine H4 receptors modulate dendritic cell migration through skin-immunomodulatory role of histamine. Allergy, 63 (10), 1387-94 (2008).
30. D. Dijkstra, R. Leurs, P. Chazot, F. C. Shenton, H. Stark, T. Werfel and R. Gutzmer: Histamine downregulates monocyte CCL2 production through the histamine H4 receptor. J Allergy Clin Immunol, 120 (2), 300-7 (2007). (Pubitemid 47102370)
31. D. Dijkstra, H. Stark, P. L. Chazot, F. C. Shenton, R. Leurs, T. Werfel and R. Gutzmer: Human inflammatory dendritic epidermal cells express a functional histamine H4 receptor. J Invest Dermatol, 128 (7), 1696-703 (2008). (Pubitemid 351847377)
32. R. M. van Rijn, P. L. Chazot, F. C. Shenton, K. Sansuk, R. A. Bakker and R. Leurs: Oligomerization of recombinant and endogenously expressed human histamine H (4) receptors. Mol Pharmacol, 70 (2), 604-15 (2006). (Pubitemid 44092321)
33. G. Morini, G. Becchi, F. C. Shenton, P. L. Chazot and D. Grandi: Histamine H3 and H4 receptors are expressed on distinct endocrine cell types in the rat fundic mucosa. Inflamm Res, 57 Suppl 1, S57-8 (2008).
34. L. E. Sander, A. Lorentz, G. Sellge, M. Coeffier, M. Neipp, T. Veres, T. Frieling, P. N. Meier, M. P. Manns and S. C. Bischoff: Selective expression of histamine receptors H1R, H2R, and H4R, but not H3R, in the human intestinal tract. Gut, 55 (4), 498-504 (2006).
35. W. M. Connelly, F. C. Shenton, N. Lethbridge, R. Leurs, H. J. Waldvogel, R. L. Faull, G. Lees and P. L. Chazot: The histamine H4 receptor is functionally expressed on neurons in the mammalian CNS. Br J Pharmacol, 157 (1), 55-63 (2009).
36. T. Oda, N. Morikawa, Y. Saito, Y. Masuho and S. Matsumoto: Molecular cloning and characterization of a novel type of histamine receptor preferentially expressed in leukocytes. J Biol Chem, 275 (47), 36781-6 (2000). (Pubitemid 32002087)
37. M. Gschwandtner, K. Rossbach, D. Dijkstra, W. Baumer, M. Kietzmann, H. Stark, T. Werfel and R. Gutzmer: Murine and human Langerhans cells express a functional histamine H4 receptor: modulation of cell migration and function. Allergy, 65 (7), 840-9.
38. R. Gutzmer, C. Diestel, S. Mommert, B. Kother, H. Stark, M. Wittmann and T. Werfel: Histamine H4 receptor stimulation suppresses IL-12p70 production and mediates chemotaxis in human monocyte-derived dendritic cells. J Immunol, 174 (9), 5224-32 (2005). (Pubitemid 40593160)
39. N. L. Lethbridge and P. L. Chazot: Immunological identification of the mouse H4 histamine receptor on spinal cord motor neurons using a novel anti-mouse H4R antibody. Inflamm Res, 59 Suppl 2, S197-8.
40. M. Nakaya, N. Takeuchi and K. Kondo: Immunohistochemical localization of histamine receptor subtypes in human inferior turbinates. Ann Otol Rhinol Laryngol, 113 (7), 552-7 (2004). (Pubitemid 38902552)
41. K. Boer, E. Helinger, A. Helinger, P. Pocza, Z. Pos, P. Demeter, Z. Baranyai, K. Dede, Z. Darvas and A. Falus: Decreased expression of histamine H1 and H4 receptors suggests disturbance of local regulation in human colorectal tumours by histamine. Eur J Cell Biol, 87 (4), 227-36 (2008).
42. C. de Graaf, N. Foata, O. Engkvist and D. Rognan: Molecular modeling of the second extracellular loop of Gprotein coupled receptors and its implication on structurebased virtual screening. Proteins-Structure Function and Bioinformatics, 71 (2), 599-620 (2008). (Pubitemid 351430001)
43. Ballesteros and Weinstein. Methods Neurosci, 25, 366- 428 (1995).
44. K. Kaupmann, B. Malitschek, V. Schuler, J. Heid, W. Froestl, P. Beck, J. Mosbacher, S. Bischoff, A. Kulik, R. Shigemoto, A. Karschin and B. Bettler: GABA (B)- receptor subtypes assemble into functional heteromeric complexes. Nature, 396 (6712), 683-7 (1998). (Pubitemid 29003947)
45. J. H. White, A. Wise, M. J. Main, A. Green, N. J. Fraser, G. H. Disney, A. A. Barnes, P. Emson, S. M. Foord and F. H. Marshall: Heterodimerization is required for the formation of a functional GABA (B) receptor. Nature, 396 (6712), 679-82 (1998). (Pubitemid 29003946)
46. K. A. Jones, B. Borowsky, J. A. Tamm, D. A. Craig, M. M. Durkin, M. Dai, W. J. Yao, M. Johnson, C. Gunwaldsen, L. Y. Huang, C. Tang, Q. Shen, J. A. Salon, K. Morse, T. Laz, K. E. Smith, D. Nagarathnam, S. A. Noble, T. A. Branchek and C. Gerald: GABA (B) receptors function as a heteromeric assembly of the subunits GABA (B)R1 and GABA (B)R2. Nature, 396 (6712), 674-9 (1998). (Pubitemid 29003945)
47. J. P. Pin, J. Kniazeff, V. Binet, J. Liu, D. Maurel, T. Galvez, B. Duthey, M. Havlickova, J. Blahos, L. Prezeau and P. Rondard: Activation mechanism of the heterodimeric GABA (B) receptor. Biochem Pharmacol, 68 (8), 1565-72 (2004). (Pubitemid 39286461)
48. H. F. Vischer, A. O. Watts, S. Nijmeijer and R. Leurs: G protein-coupled receptors: walking hand-in-hand, talking hand-in-hand? Br J Pharmacol, 163 (2), 246-60 (2011).
49. J. J. Carrillo, J. Pediani and G. Milligan: Dimers of class A G protein-coupled receptors function via agonistmediated trans-activation of associated G proteins. J Biol Chem, 278 (43), 42578-87 (2003). (Pubitemid 37310531)
50. R. A. Bakker, G. Dees, J. J. Carrillo, R. G. Booth, J. F. Lopez-Gimenez, G. Milligan, P. G. Strange and R. Leurs: Domain swapping in the human histamine H1 receptor. J Pharmacol Exp Ther, 311 (1), 131-8 (2004). (Pubitemid 39287792)
51. Y. Fukushima, T. Asano, T. Saitoh, M. Anai, M. Funaki, T. Ogihara, H. Katagiri, N. Matsuhashi, Y. Yazaki and K. Sugano: Oligomer formation of histamine H2 receptors expressed in Sf9 and COS7 cells. FEBS Lett, 409 (2), 283-6 (1997). (Pubitemid 27273893)
52. F. C. Shenton, V. Hann and P. L. Chazot: Evidence for native and cloned H3 histamine receptor higher oligomers. Inflamm Res, 54 Suppl 1, S48-9 (2005). (Pubitemid 40880787)
53. S. Nijmeijer, R. Leurs, M. J. Smit and H. F. Vischer: The Epstein-Barr virus-encoded G protein-coupled receptor BILF1 hetero-oligomerizes with human CXCR4, scavenges Galphai proteins, and constitutively impairs CXCR4 functioning. J Biol Chem, 285 (38), 29632-41 (2010).
54. H. D. Lim, R. M. van Rijn, P. Ling, R. A. Bakker, R. L. Thurmond and R. Leurs: Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist. J Pharmacol Exp Ther, 314 (3), 1310-21 (2005). (Pubitemid 41205997)
55. I. J. de Esch, R. L. Thurmond, A. Jongejan and R. Leurs: The histamine H4 receptor as a new therapeutic target for inflammation. Trends Pharmacol Sci, 26 (9), 462-9 (2005). (Pubitemid 41207878)
56. R. A. Smits, I. J. de Esch, O. P. Zuiderveld, J. Broeker, K. Sansuk, E. Guaita, G. Coruzzi, M. Adami, E. Haaksma and R. Leurs: Discovery of quinazolines as histamine H4 receptor inverse agonists using a scaffold hopping approach. J Med Chem, 51 (24), 7855-65 (2008).
57. R. A. Smits, H. D. Lim, B. Stegink, R. A. Bakker, I. J. de Esch and R. Leurs: Characterization of the histamine H4 receptor binding site. Part 1. Synthesis andpharmacological evaluation of dibenzodiazepine derivatives. J Med Chem, 49 (15), 4512-6 (2006). (Pubitemid 44162677)
58. H. D. Lim, R. A. Smits, R. A. Bakker, C. M. van Dam, I. J. de Esch and R. Leurs: Discovery of S- (2- guanidylethyl)-isothiourea (VUF 8430) as a potent nonimidazole histamine H4 receptor agonist. J Med Chem, 49 (23), 6650-1 (2006). (Pubitemid 44749731)
59. T. Hashimoto, S. Harusawa, L. Araki, O. P. Zuiderveld, M. J. Smit, T. Imazu, S. Takashima, Y. Yamamoto, Y. Sakamoto, T. Kurihara, R. Leurs, R. A. Bakker and A. Yamatodani: A selective human H (4)-receptor agonist: (-)- 2-cyano-1-methyl-3- ( (2R, 5R)-5- (1H-imidazol-4 (5)- yl)tetrahydrofuran-2-y) methylguanidine. J Med Chem, 46 (14), 3162-5 (2003).
60. P. Igel, R. Geyer, A. Strasser, S. Dove, R. Seifert and A. Buschauer: Synthesis and structure-activity relationships of cyanoguanidine-type and structurally related histamine H4 receptor agonists. J Med Chem, 52 (20), 6297-313 (2009).
61. P. Igel, S. Dove and A. Buschauer: Histamine H4 receptor agonists. Bioorg Med Chem Lett, 20 (24), 7191-9 (2010).
62. F. W. Yu, R L; Wei, J; Desai, P J; McGovern, P M; Dunford, P J; Karlsson, L; Thurmond, R L: Pharmacological characterization of oxime agonists of the histamine H4 receptor. Journal of Receptor, Ligand and Channel Research, 3, 37-49 (2010).
63. B. M. Savall, J. P. Edwards, J. D. Venable, D. J. Buzard, R. Thurmond, M. Hack and P. McGovern: Agonist/antagonist modulation in a series of 2-aryl benzimidazole H4 receptor ligands. Bioorg Med Chem Lett, 20 (11), 3367-71 (2010).
64. K. F. Buckland, T. J. Williams and D. M. Conroy: Histamine induces cytoskeletal changes in human eosinophils via the H (4) receptor. Br J Pharmacol, 140 (6), 1117-27 (2003). (Pubitemid 37475978)
65. C. L. Hofstra, P. J. Desai, R. L. Thurmond and W. P. Fung-Leung: Histamine H4 receptor mediates chemotaxis and calcium mobilization of mast cells. J Pharmacol Exp Ther, 305 (3), 1212-21 (2003). (Pubitemid 36618001)
66. K. Takeshita, K. B. Bacon and F. Gantner: Critical role of L-selectin and histamine H4 receptor in zymosaninduced neutrophil recruitment from the bone marrow: comparison with carrageenan. J Pharmacol Exp Ther, 310 (1), 272-80 (2004). (Pubitemid 38812721)
67. B. B. Damaj, C. B. Becerra, H. J. Esber, Y. Wen and A. A. Maghazachi: Functional expression of H4 histamine receptor in human natural killer cells, monocytes, and dendritic cells. J Immunol, 179 (11), 7907-15 (2007).
68. J. A. Jablonowski, C. A. Grice, W. Chai, C. A. Dvorak, J. D. Venable, A. K. Kwok, K. S. Ly, J. Wei, S. M. Baker, P. J. Desai, W. Jiang, S. J. Wilson, R. L. Thurmond, L. Karlsson, J. P. Edwards, T. W. Lovenberg and N. I. Carruthers: The first potent and selective non-imidazole human histamine H4 receptor antagonists. J Med Chem, 46 (19), 3957-60 (2003). (Pubitemid 37122442)
69. R. L. Thurmond, P. J. Desai, P. J. Dunford, W. P. Fung-Leung, C. L. Hofstra, W. Jiang, S. Nguyen, J. P. Riley, S. Sun, K. N. Williams, J. P. Edwards and L. Karlsson: A potent and selective histamine H4 receptor antagonist with anti-inflammatory properties. J Pharmacol Exp Ther, 309 (1), 404-13 (2004). (Pubitemid 38393154)
70. R. Seifert, E. H. Schneider, S. Dove, I. Brunskole, D. Neumann, A. Strasser and A. Buschauer: Paradoxical stimulatory effects of the standard histamine H4-receptor antagonist JNJ7777120: The H4-receptor joins the club of 7TM receptors exhibiting functional selectivity. Mol Pharmacol (2011).
71. E. M. Rosethorne and S. J. Charlton: Agonist-biased signaling at the histamine H4 receptor: JNJ7777120 recruits beta-arrestin without activating G proteins. Mol Pharmacol, 79 (4), 749-57 (2011).
72. N. Terzioglu, R. M. van Rijn, R. A. Bakker, I. J. De Esch and R. Leurs: Synthesis and structure-activity relationships of indole and benzimidazole piperazines as histamine H (4) receptor antagonists. Bioorg Med Chem Lett, 14 (21), 5251-6 (2004). (Pubitemid 39348908)
73. J. D. Venable, H. Cai, W. Chai, C. A. Dvorak, C. A. Grice, J. A. Jablonowski, C. R. Shah, A. K. Kwok, K. S. Ly, B. Pio, J. Wei, P. J. Desai, W. Jiang, S. Nguyen, P. Ling, S. J. Wilson, P. J. Dunford, R. L. Thurmond, T. W. Lovenberg, L. Karlsson, N. I. Carruthers and J. P. Edwards: Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: potent human histamine h (4) antagonists. J Med Chem, 48 (26), 8289-98 (2005). (Pubitemid 43032536)
74. H. Liu, R. J. Altenbach, T. L. Carr, P. Chandran, G. C. Hsieh, L. G. Lewis, A. M. Manelli, I. Milicic, K. C. Marsh, T. R. Miller, M. I. Strakhova, T. A. Vortherms, B. D. Wakefield, J. M. Wetter, D. G. Witte, P. Honore, T. A. Esbenshade, J. D. Brioni and M. D. Cowart: cis-4- (Piperazin-1-yl)-5, 6, 7a, 8, 9, 10, 11, 11a-octahydrobenzofuro (2, 3-h)quina zolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia. J Med Chem, 51 (22), 7094-8 (2008).
75. W. C. Lumma, Jr., R. D. Hartman, W. S. Saari, E. L. Engelhardt, V. J. Lotti and C. A. Stone: Piperazinylquinoxalines with central serotoninmimetic activity. J Med Chem, 24 (1), 93-101 (1981). (Pubitemid 11189908)
76. R. A. Smits, H. D. Lim, A. Hanzer, O. P. Zuiderveld, E. Guaita, M. Adami, G. Coruzzi, R. Leurs and I. J. de Esch: Fragment based design of new H4 receptor-ligands with anti-inflammatory properties in vivo. J Med Chem, 51 (8), 2457-67 (2008). (Pubitemid 351628507)
77. R. A. Smits, M. Adami, E. P. Istyastono, O. P. Zuiderveld, C. M. van Dam, F. J. de Kanter, A. Jongejan, G. Coruzzi, R. Leurs and I. J. de Esch: Synthesis and QSAR of quinazoline sulfonamides as highly potent human histamine H4 receptor inverse agonists. J Med Chem, 53 (6), 2390-400 (2010).
78. R. A. Smits, R. Leurs and I. J. de Esch: Major advances in the development of histamine H4 receptor ligands. Drug Discov Today, 14 (15-16), 745-53 (2009).
79. H. Engelhardt, R. A. Smits, R. Leurs, E. Haaksma and I. J. de Esch: A new generation of anti-histamines: Histamine H4 receptor antagonists on their way to the clinic. Curr Opin Drug Discov Devel, 12 (5), 628-43 (2009).
80. H. D. Lim, A. Jongejan, R. A. Bakker, E. Haaksma, I. J. de Esch and R. Leurs: Phenylalanine 169 in the second extracellular loop of the human histamine H4 receptor is responsible for the difference in agonist binding between human and mouse H4 receptors. J Pharmacol Exp Ther, 327 (1), 88-96 (2008).
81. J. S. Surgand, J. Rodrigo, E. Kellenberger and D. Rognan: A chemogenomic analysis of the transmembrane binding cavity of human G-protein-coupled receptors. Proteins-Structure Function and Bioinformatics, 62 (2), 509-538 (2006). (Pubitemid 43054370)
82. E. P. Istyastono, C. de Graaf, I. J. de Esch and R. Leurs: Molecular Determinants of Selective Agonist and Antagonist Binding to the Histamine H (4) Receptor. Curr Top Med Chem (2011).
83. A. Jongejan, H. D. Lim, R. A. Smits, I. J. de Esch, E. Haaksma and R. Leurs: Delineation of agonist binding to the human histamine H4 receptor using mutational analysis, homology modeling, and ab initio calculations. J Chem Inf Model, 48 (7), 1455-63 (2008).
84. N. Shin, E. Coates, N. J. Murgolo, K. L. Morse, M. Bayne, C. D. Strader and F. J. Monsma, Jr.: Molecular modeling and site-specific mutagenesis of the histaminebinding site of the histamine H4 receptor. Mol Pharmacol, 62 (1), 38-47 (2002). (Pubitemid 34680514)
85. L. Shi and J. A. Javitch: The binding site of aminergic G protein-coupled receptors: the transmembrane segments and second extracellular loop. Annu Rev Pharmacol Toxicol, 42, 437-67 (2002). (Pubitemid 34162546)
86. E. P. Istyastono, C. de Graaf, I. J. de Esch and R. Leurs: Molecular determinants of selective agonist and antagonist binding to the histamine H receptor. Curr Top Med Chem, 11 (6), 661-79 (2011).
87. T. Werner, K. Sander, Y. Tanrikulu, T. Kottke, E. Proschak, H. Stark and G. Schneider: In silico characterization of ligand binding modes in the human histamine H4 receptor and their impact on receptor activation. Chembiochem, 11 (13), 1850-5 (2010).
88. E. H. Schneider and R. Seifert: Histamine H (4) receptor-RGS fusion proteins expressed in Sf9 insect cells: a sensitive and reliable approach for the functional characterization of histamine H (4) receptor ligands. Biochem Pharmacol, 78 (6), 607-16 (2009).
89. R. A. Bakker, K. Wieland, H. Timmerman and R. Leurs: Constitutive activity of the histamine H (1) receptor reveals inverse agonism of histamine H (1) receptor antagonists. Eur J Pharmacol, 387 (1), R5-R7 (2000). (Pubitemid 30035384)
90. M. J. Smit, R. Leurs, A. E. Alewijnse, J. Blauw, G. P. Van Nieuw Amerongen, Y. Van De Vrede, E. Roovers and H. Timmerman: Inverse agonism of histamine H2 antagonist accounts for upregulation of spontaneously active histamine H2 receptors. Proc Natl Acad Sci U S A, 93 (13), 6802-7 (1996). (Pubitemid 26230391)
91. K. Wieland, G. Bongers, Y. Yamamoto, T. Hashimoto, A. Yamatodani, W. M. Menge, H. Timmerman, T. W. Lovenberg and R. Leurs: Constitutive activity of histamine h (3) receptors stably expressed in SK-N-MC cells: display of agonism and inverse agonism by H (3) antagonists. J Pharmacol Exp Ther, 299 (3), 908-14 (2001). (Pubitemid 33104958)
92. S. Morisset, A. Rouleau, X. Ligneau, F. Gbahou, J. Tardivel-Lacombe, H. Stark, W. Schunack, C. R. Ganellin, J. C. Schwartz and J. M. Arrang: High constitutive activity of native H3 receptors regulates histamine neurons in brain. Nature, 408 (6814), 860-4 (2000). (Pubitemid 32016096)
93. R. A. Clark, J. I. Gallin and A. P. Kaplan: The selective eosinophil chemotactic activity of histamine. J Exp Med, 142 (6), 1462-76 (1975).
94. M. O'Reilly, R. Alpert, S. Jenkinson, R. P. Gladue, S. Foo, S. Trim, B. Peter, M. Trevethick and M. Fidock: 0Identification of a histamine H4 receptor on human eosinophils-role in eosinophil chemotaxis. J Recept Signal Transduct Res, 22 (1-4), 431-48 (2002). (Pubitemid 36169163)
95. P. Ling, K. Ngo, S. Nguyen, R. L. Thurmond, J. P. Edwards, L. Karlsson and W. P. Fung-Leung: Histamine H4 receptor mediates eosinophil chemotaxis with cell shape change and adhesion molecule upregulation. Br J Pharmacol, 142 (1), 161-71 (2004). (Pubitemid 38698205)
96. R. Barnard, A. Barnard, G. Salmon, W. Liu and S. Sreckovic: Histamine-induced actin polymerization in human eosinophils: an imaging approach for histamine H4 receptor. Cytometry A, 73 (4), 299-304 (2008). (Pubitemid 351522112)
97. T. Kohyama, Y. Yamauchi, H. Takizawa, S. Kamitani, S. Kawasaki and T. Nagase: Histamine stimulates human lung fibroblast migration. Mol Cell Biochem, 337 (1-2), 77- 81.
98. V. Godot, M. Arock, G. Garcia, F. Capel, C. Flys, M. Dy, D. Emilie and M. Humbert: H4 histamine receptor mediates optimal migration of mast cell precursors to CXCL12. J Allergy Clin Immunol, 120 (4), 827-34 (2007). (Pubitemid 47531837)
99. M. Dy and E. Schneider: Histamine-cytokine connection in immunity and hematopoiesis. Cytokine Growth Factor Rev, 15 (5), 393-410 (2004). (Pubitemid 39140701)
100. E. Schneider, M. Rolli-Derkinderen, M. Arock and M. Dy: Trends in histamine research: new functions during immune responses and hematopoiesis. Trends Immunol, 23 (5), 255-63 (2002). (Pubitemid 34499563)
101. M. Jutel, T. Watanabe, S. Klunker, M. Akdis, O. A. Thomet, J. Malolepszy, T. Zak-Nejmark, R. Koga, T. Kobayashi, K. Blaser and C. A. Akdis: Histamine regulates T-cell and antibody responses by differential expression of H1 and H2 receptors. Nature, 413 (6854), 420-5 (2001). (Pubitemid 32928596)
102. B. Horr, H. Borck, R. Thurmond, S. Grosch and F. Diel: STAT1 phosphorylation and cleavage is regulated by the histamine (H4) receptor in human atopic and non-atopic lymphocytes. Int Immunopharmacol, 6 (10), 1577-85 (2006).
103. M. C. Leite-de-Moraes, S. Diem, M. L. Michel, H. Ohtsu, R. L. Thurmond, E. Schneider and M. Dy: Cutting edge: histamine receptor H4 activation positively regulates in vivo IL-4 and IFN-gamma production by invariant NKT cells. J Immunol, 182 (3), 1233-6 (2009).
104. P. Desai and R. L. Thurmond: Histamine H (4) receptor activation enhances LPS-induced IL-6 production in mast cells via ERK and PI3K activation. Eur J Immunol, 41 (6), 1764-73 (2011).
105. A. F. Petit-Bertron, F. Machavoine, M. P. Defresne, M. Gillard, P. Chatelain, P. Mistry, E. Schneider and M. Dy: H4 histamine receptors mediate cell cycle arrest in growth factor-induced murine and human hematopoietic progenitor cells. PLoS One, 4 (8), e6504 (2009).
106. G. A. Coruzzi, M.'Pozzoli, C.; Smits, R.; De Esch, I.; Leurs, R. Gastroprotective effects of histamine H4 receptor ligands in rodent ulcer models. Proceedings of the Britisch Pharmacological Society, 7 (4) (2010).
107. E. M. Rosethorne and S. J. Charlton: Agonist-biased signalling at the histamine H4 receptor: JNJ7777120 recruits beta-arrestin without activating G proteins. Mol Pharmacol (2010).
108. Y. Ikawa, M. Suzuki, S. Shiono, E. Ohki, H. Moriya, E. Negishi and K. Ueno: Histamine H4 receptor expression in human synovial cells obtained from patients suffering from rheumatoid arthritis. Biol Pharm Bull, 28 (10), 2016-8 (2005). (Pubitemid 41437104)
109. F. Cianchi, C. Cortesini, N. Schiavone, F. Perna, L. Magnelli, E. Fanti, D. Bani, L. Messerini, V. Fabbroni, G. Perigli, S. Capaccioli and E. Masini: The role of cyclooxygenase-2 in mediating the effects of histamine on cell proliferation and vascular endothelial growth factor production in colorectal cancer. Clin Cancer Res, 11 (19 Pt 1), 6807-15 (2005). (Pubitemid 41428735)
110. C. Varga, K. Horvath, A. Berko, R. L. Thurmond, P. J. Dunford and B. J. Whittle: Inhibitory effects of histamine H4 receptor antagonists on experimental colitis in the rat. Eur J Pharmacol, 522 (1-3), 130-8 (2005). (Pubitemid 41456659)
111. D. Maslinska, M. Laure-Kamionowska, K. T. Maslinski, K. Deregowski, G. Szewczyk and S. Maslinski: Histamine H (4) receptors on mammary epithelial cells of the human breast with different types of carcinoma. Inflamm Res, 55 Suppl 1, S77-8 (2006). (Pubitemid 43760602)