Histamine H4 Receptor: A Novel Target for Inflammation Therapy

Mini-Reviews in Medicinal Chemistry

Volumn 11, Issue 2, 2011, Pages 143-158

  Saravanan, C ^a   Bharti, S K ^a   Jaggi, S ^a   Singh, S K ^a  

^a BANARAS HINDU UNIVERSITY   (India)

Author keywords

Agonist; Antagonist; G protein coupled receptor (GPCR); Histamine H4 receptor; Inflammation; JNJ7777120; Structure activity relationship (SAR)

Indexed keywords

(1 [(5 CHLORO 1H INDOL 2 YL)CARBONYL] 4 METHYLPIPERAZINE; 1 (5 CHLORO 2 BENZIMIDAZOLYLCARBONYL) 4 METHYLPIPERAZINE; 1 (5 CHLORO 2 INDOLYLCARBONYL) 4 METHYLPIPERAZINE; 1 [(1H INDOL 2 YL)CARBONYL] 4 METHYL PIPERAZINE; 2,4 DIAMINOPYRIMIDINE DERIVATIVE; 4 METHYLHISTAMINE; 9 (TETRAHYDRO 2 FURYL)ADENINE; A 987306; ALPHA METHYLHISTAMINE; ANTIINFLAMMATORY AGENT; ASPARAGINE; BENZIMIDAZOLE DERIVATIVE; CLOBENPROPIT; CLOZAPINE; CYCLOPROPANE; G PROTEIN COUPLED RECEPTOR; HISTAMINE H3 RECEPTOR ANTAGONIST; HISTAMINE H4 RECEPTOR; HISTAMINE H4 RECEPTOR ANTAGONIST; INDOLE; LIGAND; QUINAZOLINE; QUINOXALINE DERIVATIVE; SERINE; SP 9144; THIOPERAMIDE; THREONINE; UNCLASSIFIED DRUG; VUF 10148; VUF 10214; HISTAMINE RECEPTOR; HRH4 PROTEIN, HUMAN;

ACYLATION; ANTIINFLAMMATORY ACTIVITY; BINDING SITE; CELL NUCLEUS; GENETIC CODE; HUMAN; IN VIVO STUDY; INFLAMMATION; NONHUMAN; PROTEIN EXPRESSION; PROTEIN STRUCTURE; REVIEW; SEQUENCE HOMOLOGY; SIGNAL TRANSDUCTION; STRUCTURE ACTIVITY RELATION; DRUG EFFECT; IMMUNOLOGY; LEUKOCYTE; MAST CELL; METABOLISM;

ANTI-INFLAMMATORY AGENTS; HUMANS; INFLAMMATION; LEUKOCYTES; MAST CELLS; RECEPTORS, G-PROTEIN-COUPLED; RECEPTORS, HISTAMINE;

EID: 79951707693     PISSN: 13895575     EISSN: None     Source Type: Journal    
DOI: 10.2174/138955711794519519     Document Type: Review

References (96)

1. Dale, H.H.; Laidlaw, P.P. The physiological actions of β-iminazolethylamine. J. Physiol., 1910, 41, 318-344.
2. Schayer, R.W. In The origin and fate of histamine in the body; Wolstenholme, G.E.W.; O'Connor, C.M. Ed.; J. and A. ChurchillLtd.: London, 1956; pp. 183-188.
3. Lewis, T.; Grant, R.T. Vascular reactions of the skin to injury. Part11. The liberation of histamine-like substance in the injured skin, the underlying cause of factitious urticaria and of wheals producedby burning: and observations upon the nervous control of certainskin reactions. Heart, 1924, 11, 209-265.
4. Haas, H.; Panula, P. The role of histamine and the tuberomamillarynucleus in the nervous system. Nat. Rev. Neurosci., 2003, 4, 121-130.
5. Ramirez, M.S.R. New concepts of histamine receptors and actions. Curr. Allergy Asthma Rep., 2003, 3, 227-231.
6. Debacker, M. D.; Gommeren, W.; Moereels, H.; Nobels, G.; Vangompel, P.; Leysen, J.E.; Luyten, W.H.M.L. Genomic cloning, heterologousexpression and pharmacological characterization of ahuman histamine H1 receptor. Biochem. Biophys. Res. Commun., 1993, 197, 1601-1608.
7. Gantz, I.; Schaffer, M.; DelValle, J.; Logsdon, C.; Campbell, V.; Uhler, M.; Yamada, T. Molecular cloning of a gene encoding thehistamine H2 receptor. Proc. Natl. Acad. Sci. U. S. A., 1991, 88, 429-433.
8. 3 receptor. Mol. Pharmacol., 1999, 55, 1101-1107.
9. 3 Receptor; A Target for NewDrugs, 1st ed.; Elsevier Science: Amsterdam, 1998.
10. 3 receptor ligandsbreak ground in a remarkable plethora of therapeutic areas. ExpertOpin. Investig. Drugs, 2007, 16, 967-985.
11. 3 receptor antagonistsgo to clinics. Biol. Pharm. Bull., 2008, 31, 2163-2181.
12. Oda, T.; Morikawa, N.; Saito, Y.; Masuho, Y.; Matsumoto, S. Molecular cloning and characterization of a novel type of histaminereceptor preferentially expressed in leukocytes. J. Biol. Chem. 2000, 275, 36781-36786.
13. Nguyen, T.; Shapiro, D. A.; George, S. R.; Setola, V.; Lee, D. K.; Cheng, R.; Rauser, L.; Lee, S. P.; Lynch, K. R.; Roth, B. L.; O'Dowd, B. F. Discovery of a novel member of the histamine receptorfamily. Mol. Pharmacol. 2001, 59, 427-433.
14. 4 expressed in bone marrow. Mol. Pharmacol. 2001, 59, 420-426.
15. Morse, K. L.; Behan, J.; Laz, T. M.; West, R.E. Jr.; Greenfeder, S.A.; Anthes, J. C.; Umland, S.; Wan, Y.; Hipkin, R. W.; Gonsiorek, W.; Shin, N.; Gustafson, E. L.; Qiao, X.; Wang, S.; Hedrick, J. A.; Greene, J.; Bayne, M.; Monsma, F. J., Jr. Cloningand characterization of a novel human histamine receptor. J. Pharmacol. Exp. Ther. 2001, 296, 1058-1066.
16. Zhu, Y.; Michalovich, D.; Wu, H.; Tan, K.B.; Dytko, G. M.; Mannan, I.J.; Boyce, R.; Alston, J.; Tierney, L.A.; Li, X.; Herrity, N.C.; Vawter, L.; Sarau, H.M.; Ames, R.S.; Davenport, C.M.; Hieble, J.P.; Wilson, S.; Bergsma, D.J.; Fitzgerald, L.R. Cloning, expression, and pharmacological characterization of a novel human histaminereceptor. Mol. Pharmacol. 2001, 59, 434-441.
17. 4 receptor mediates chemotaxis and calcium mobilization ofmast cells. J. Pharmacol. Exp. Ther., 2003, 305, 1212-1221.
18. 4 receptor antagonism exhibitsanti-nociceptive effects in inflammatory and neuropathic painmodels in rats. Pharmacol. Biochem. Behav., 2010, 95, 41-50.
19. Morgan, R.K.; McAllister, B.; Cross, L.; Green, D.S.; Kornfeld, H.; Center, D.M.; Cruikshank, W.W. Histamine 4 receptor activationinduces recruitment of FoxP3+ T cells and inhibits allergic asthmain a murine model. J. Immunol., 2007, 178, 8081-8089.
20. 4 receptor in allergic conjunctivitis inmice. Eur. J. Pharmacol., 2009, 608, 71-75.
21. Parsons, M.E.; Ganellin, C.R. Histamine and its receptors, Br. J. Pharmacol., 2006, 147, S127-S135.
22. Jutel, M.; Blaser, K.; Akdis, C.A. The role of histamine in regulationof immune responses. Chem. Immunol. Allergy, 2006, 91, 174-187.
23. 4 receptors in allergic inflammation: the search fornew antihistamines, Nat. Rev. Drug Discov., 2008, 7, 41-53.
24. Huang, J.F.; Thurmond, R.L. The new biology of histamine receptors, Curr. Allergy Asthma Rep., 2008, 8, 21-27.
25. Raible, D.G.; Lenahan, T.; Fayvilevich, Y.; Kosinski, R.; Schulman, E.S. Pharmacologic characterization of a novel histamine receptoron human eosinophils. Am. J. Respir. Crit. Care Med., 1994, 149, 1506-1511.
26. 4R. Biochem. Biophys. Res. Commun., 2000, 279, 615-620.
27. 4 receptor onhuman eosinophils-role in eosinophilchemotaxis. J. Recept. Signal Transduct., 2002, 22, 431-448.
28. 4-receptor gene. Biochem. Biophys. Res. Commun., 2001, 284, 301-309.
29. Teller, D.C.; Okada, T.; Behnke, C. A.; Palczewski, K.; Stenkamp, R.E. Advances in determination of a high-resolution three dimensionalstructure of rhodopsin, a model of G-protein-coupled receptors(GPCRs). Biochemistry, 2001, 40, 7761-7772.
30. Cherezov, V.; Rosenbaum, D.M.; Hanson, M.A.; Rasmussen, S.G.; Thian, F.S.; Kobilka, T.S.; Choi, H.J.; Kuhn, P.; Weis, W.I.; Kobilka, B.K.; Stevens, R.C. High-resolution crystal structure of anengineered human beta2-adrenergic G protein coupled receptor. Science, 2007, 318, 1258-1265.
31. Warne, T.; Serrano-Vega, M.J.; Baker, J.G.; Moukhametzianov, R.; Edwards, P.C.; Henderson, R.; Leslie, A.G.; Tate, C.G.; Schertler, G.F. Structure of a beta1-adrenergic G-protein-coupled receptor. Nature, 2008, 454, 486-491.
32. Sibley, D.R.; Monsma, F.J. Jr. Molecular biology of dopaminereceptors. Trends Pharmacol. Sci., 1992, 13, 61-69.
33. Kroeze, W.K.; Roth, B.L. The molecular biology of serotoninreceptors: Therapeutic implications for the interface of mood andpsychosis. Biol. Psychiatry, 1988, 44, 1128-1142.
34. Oliviera, L., Paiva, A. C. M., Sander, C., Vriend, G. A. commonstep for signal transduction in G protein-coupled receptors. TrendsPharmacol. Sci., 1994, 15, 170-172.
35. Huang, E.S. Construction of a sequence motif characteristic ofaminergic G protein-coupled receptors. Protein Sci., 2003, 12, 1360-1367.
36. Ananthan, S.; Zhang, W.; Hobrath, J.V. Recent advances in structure-based virtual screening of G-protein coupled receptors. AAPSJ., 2009, 2, 178-185.
37. 4 agonism in antigen-specifichuman T-cell responses. Immunology, 2007, 121, 266-275.
38. 4 receptor. Biochem. J., 2008, 414, 121-131.
39. 4 receptor. Mol. Pharmacol., 2002, 62, 38-47.
40. 4receptor using mutational analysis, homology modeling, and ab initiocalculations. J. Chem. Inf. Model., 2008, 48, 1455-1463.
41. 4 receptor. Eur. J. Med. Chem., 2008, 43, 1059-1070.
42. 4receptor ligands, J. Pharmacol. Exp. Ther., 2010, 334, 513-521.
43. 4 receptor antagonists. J. Mol. Model., DOI 10.1007/s00894-010-0779-4 (article in press).
44. 4 receptor - an explicit membranemolecular dynamics simulation study. J. Chem. Inf. Model., 2008, 48, 1199-1210.
45. 4 receptor. ChemMedChem, 2009, 4, 820-827.
46. 4 receptor. J. Pharmacol. Sci., 2005, 98, 319-322.
47. 4 receptor. Eur. J. Pharmacol., 2008, 592, 26-32.
48. 4 receptors revealssubstantial pharmacological species variation. J. Pharmacol. Exp. Ther., 2001, 299, 121-130.
49. 4 receptor. Biochim. Biophys. Acta, 2002, 1575, 135-1358.
50. 4 receptors. J. Pharmacol. Exp. Ther., 2008, 327, 88-96.
51. 4 histamine receptor in humannatural killer cells, monocytes, and dendritic Cells. J. Immunol., 2007, 179, 7907-7915.
52. 4 receptor inmouse splenic dendritic cells. Inflamm. Res., 2010, 59, S201-203.
53. 4receptors in the central nervous system of human and rat. BrainRes., 2009, 1250, 41-48.
54. 4R antibody. Inflamm. Res., 2010, 59, S197-S198.
55. 4 receptor expression in human synovialcells obtained from patients suffering from rheumatoid arthritis. Biol. Pharm. Bull., 2005, 28, 2016-2018.
56. 4 receptor in humansynovial tissue from patients with rheumatoid arthritis. Inflamm. Res., 2007, 56, S59-S60.
57. 4 receptor in humanosteoarthritic synovial tissue. Inflamm. Res., 2008, 57, S63-S64.
58. Maruotti, N.; Crivellato, E.; Cantatore, F.P.; Vacca, A.; Ribatti, D. Mast cells in rheumatic arthritis. Clin. Rheumatol., 2007, 26, 1-4.
59. 4 receptor antagonist with anti-inflammatory properties. J. Pharmacol. Exp. Ther., 2004, 309, 404-413.
60. 4 receptor in leukotriene B4 production and mast celldependentneutrophil recruitment induced by zymosan in vivo. J. Pharmacol. Exp. Ther., 2003, 307, 1072-1078.
61. 4 receptor is functionally expressedon TH2 cells. J. Allergy Clin. Immunol., 2009;123, 619-625.
62. 4 receptor mediates allergicairway inflammation by regulating the activation of CD4+Tcells. J. Immunol., 2006, 176, 7062-7070.
63. 4 receptor. J. Invest. Dermatol., 2008, 128, 1696-1703.
64. 4 receptor expressionis elevated in human nasal polyp tissue. Cell Biol. Int., 2007, 31, 1367-1370.
65. 4 receptors: structure-activity relationships of histamine derivatives. Br. J. Pharmacol., 2006, 147, 744-754.
66. 4receptor ligands. Bioorg. Med. Chem., 2010, 18, 1076-1082.
67. 4receptor agonists: selectivity by variation of the NG-Substituent. J. Med. Chem., 2009, 52, 2623-2627.
68. 4 receptor agonists. J. Med. Chem., 2009, 52, 6297-6313.
69. 4 receptors: Synthesis, pharmacologicalevaluation, and cross-target QSAR studies. Bioorg. Med. Chem., 2009, 17, 3987-3994.
70. 4 receptor agonist. J. Med. Chem., 2006, 49, 6650-6651.
71. 4 receptor bindingsite. Part 1. synthesis and pharmacological evaluation of dibenzodiazepinederivatives. J. Med. Chem., 2006, 49, 4512-4516.
72. 4 receptor ligands. J. Med. Chem., 2008, 51, 6571-6580.
73. 4 receptor ligands-Scaffoldoptimization and pharmacological characterization. Bioorg. Med. Chem., 2009, 17, 7186-7196.
74. 4 receptorligands. Inflamm. Res., 2010, 59(Suppl 2), S249-S51.
75. 4 receptor antagonists: Effects of substitution about the rigidifyingring. Bioorg. Med. Chem. Lett., 2010, 20, 1900-1904.
76. 4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia. J. Med. Chem., 2008, 51, 7094-7098.
77. 4 receptor antagonists. J. Med. Chem., 2003, 46, 3957-3960.
78. 4 receptor antagonists. Bioorg. Med. Chem. Lett., 2004, 14, 5251-5256.
79. 4 antagonists. J. Med. Chem., 2005, 48, 8289-8298.
80. 4 receptor ligands. Bioorg. Med. Chem. Lett., 2006, 16, 6043-6048.
81. 4 receptor-ligands with anti-inflammatory propertiesin vivo. J. Med. Chem., 2008, 51, 2457-2467.
82. 4 receptor inverse agonistsusing a scaffold hopping approach. J. Med. Chem., 2008, 51, 7855-7865.
83. 4 receptorantagonists with an Imidazolylcyclopropane Structure. J. Med. Chem., 2006, 49, 5587-5596.
84. 4 receptor. Br.J. Pharmacol., 2003, 140, 1117-1127.
85. 4 receptorantagonist, thioperamide on regional haemodynamics in ratswith trinitrobenzene sulfonic acid-induced colitis. Inflamm. Res., 2007, 56, S21-22.
86. 4 receptor antagonistson experimental colitis in the rat. Eur. J. Pharmacol., 2005, 522, 130-138.
87. 4-receptor antagonists JNJ7777120 and VUF6002 in a rat modelof carrageenan-induced acute inflammation. Eur. J. Pharmacol., 2007, 563, 240-244.
88. 4 receptors in mechanical hyperalgesiafollowing peripheral nerve injury. Neuroimmunomodulation, 2007, 14, 317-325.
89. 4 receptor antagonists are superiorto traditional antihistamines in the attenuation of experimental pruritus. J. Allergy Clin. Immunol., 2007, 119, 176-183.
90. 4 receptor antagonist on allergic rhinitis inmice. Int. Immunopharmacol., 2009, 9, 734-738.
91. 4 receptor-inverse agonist thatshows good efficacy in a rat asthma model. Inflamm. Res., 2010, 59, S199-200.
92. 4): a comparative antagonists study. AsianPac. J. Trop. Med., 2010, 3, 465-470.
93. 4R)-antagonist in rabbit experimental model: A short term study. Exp. Toxicol. Pathol., 2010, doi:10.1016/j.etp.2010.08.018 (articlein press).
94. 4 receptor inverse agonists. Bioorg. Med. Chem. Lett., 2010, 20, 2016-2019.
95. 4 receptor ligands by large-scale structure-based virtualscreening. J. Med. Chem., 2008, 51, 3145-3153.
96. Keiser, M.J.; Setola, V.; Irwin, J.J.; Laggner, C.; Abbas, A.I.; Hufeisen S.J.;, Jensen, N.H.; Kuijer, M.B.; Matos, R.C.; Tran, T.B.; Whaley, R.; Glennon, R.A.; Hert, J.; Thomas, K.L.H.; Edwards, D.D.; Shoichet, B.K.; Roth, B.L. Predicting new molecular targetsfor known drugs. Nature, 2009, 462, 175-181.