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Recent progress in the development of antagonists to the chemokine receptors CCR3 and CCR4

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  • Zhu Y, Yu T, Zhang XC, et al. Role of the chemokine SDF-1 as the meningeal attractant for embryonic cerebellar neurons. Nat Neurosci 2002;5:719-20
  • Gleissner CA, Shaked I, Little KM, Ley K. CXC chemokine ligand 4 induces a unique transcriptome in monocyte-derived macrophages. J Immunol 2010;184:4810-18
  • Bachelerie F, Ben-Baruch A, Burkhardt AM, et al. International Union of Pharmacology. LXXXIX. Update on the Extended Family of Chemokine Receptors and Introducing a New Nomenclature for Atypical Chemokine Receptors. Pharmacol Rev 2014;66:1-79
  • Horn F, Weare J, Beukers MW, et al. GPCRDB: an information system for G protein-coupled receptors. Nucleic Acids Res 1998;26:275-9
  • Kitaura M, Suzuki N, Imai T, et al. Molecular cloning of a novel human CC chemokine (Eotaxin-3) that is a functional ligand of CC chemokine receptor 3. J Biol Chem 1999;274:27975-80
  • Nakayama T, Watanabe Y, Oiso N, et al. Eotaxin-3/CC chemokine ligand 26 is a functional ligand for CX3CR1. J Immunol 2010;185:6472-9
  • Pease JE, Horuk R. Chemokine receptor antagonists:part 1. Exp Opin Ther Pat 2009;19:39-58
  • Pease J, Horuk R. Chemokine receptor antagonists. J Med Chem 2012;55:9363-92
  • Schall TJ, Proudfoot AE. Overcoming hurdles in developing successful drugs targeting chemokine receptors. Nat Rev Immunol 2011;11:355-63
  • Lebre MC, Vergunst CE, Choi IY, et al. Why CCR2 and CCR5 blockade failed and why CCR1 blockade might still be effective in the treatment of rheumatoid arthritis. PLoS One 2011;6:e21772
  • Pease JE, Horuk R. Small molecule antagonists of chemokine receptors – is promiscuity a virtue? Curr Top Med Chem 2010;10:1351-8
  • Disease TIUATaL. The Global Asthma Report. 2011. Available from: http://www.globalasthmareport.org/
  • Wenzel SE. Asthma phenotypes: the evolution from clinical to molecular approaches. Nat Med 2012;18:716-25
  • An Outcomes Strategy for COPD and Asthma: NHS Companion Document. 2012. Available from: https://www.gov.uk/government/uploads/system/.../dh_134001.pdf
  • Pease JE. Targeting chemokine receptors in allergic disease. Biochem J 2011;434:11-24
  • Collins PD, Marleau S, Griffiths-Johnson DA, et al. Cooperation between interleukin-5 and the chemokine eotaxin to induce eosinophil accumulation in vivo. J Exp Med 1995;182:1169-74
  • Palframan RT, Collins PD, Severs NJ, et al. Mechanisms of acute eosinophil mobilization from the bone marrow stimulated by interleukin 5: the role of specific adhesion molecules and phosphatidylinositol 3-kinase. J Exp Med 1998;188:1621-32
  • Palframan RT, Collins PD, Williams TJ, Rankin SM. Eotaxin induces a rapid release of eosinophils and their progenitors from the bone marrow. Blood 1998;91:2240-8
  • Matthews AN, Friend DS, Zimmermann N, et al. Eotaxin is required for the baseline level of tissue eosinophils. Proc Natl Acad Sci USA 1998;95:6273-8
  • Simons JE, Rothenberg ME, Lawrence RA. Eotaxin-1-regulated eosinophils have a critical role in innate immunity against experimental Brugia malayi infection. Eur J Immunol 2005;35:189-97
  • Culley FJ, Brown A, Conroy DM, et al. Eotaxin is specifically cleaved by hookworm metalloproteases preventing its action in vitro and in vivo. J Immunol 2000;165:6447-53
  • Beck LA, Tancowny B, Brummet ME, et al. Functional analysis of the chemokine receptor CCR3 on airway epithelial cells. J Immunol 2006;177:3344-54
  • Joubert P, Lajoie-Kadoch S, Labonte I, et al. CCR3 expression and function in asthmatic airway smooth muscle cells. J Immunol 2005;175:2702-8
  • Halwani R, Al-Abri J, Beland M, et al. CC and CXC chemokines induce airway smooth muscle proliferation and survival. J Immunol 2011;186:4156-63
  • Markwick LJ, Clements D, Roberts ME, et al. CCR3 induced-p42/44 MAPK activation protects against staurosporine induced-DNA fragmentation but not apoptosis in airway smooth muscle cells. Clin Exp Allergy 2012;42:1040-50
  • Lilly CM, Woodruff PG, Camargo CA Jr, et al. Elevated plasma eotaxin levels in patients with acute asthma. J Allergy Clin Immunol 1999;104:786-90
  • Ying S, Robinson DS, Meng Q, et al. C-C chemokines in allergen-induced late-phase cutaneous responses in atopic subjects: association of eotaxin with early 6-hour eosinophils, and of eotaxin-2 and monocyte chemoattractant protein-4 with the later 24-hour tissue eosinophilia, and relationship to basophils and other C-C chemokines (monocyte chemoattractant protein-3 and RANTES). J Immunol 1999;163:3976-84
  • Ying S, Robinson DS, Meng Q, et al. Enhanced expression of eotaxin and CCR3 mRNA and protein in atopic asthma. Association with airway hyperresponsiveness and predominant co-localization of eotaxin mRNA to bronchial epithelial and endothelial cells. Eur J Immunol 1997;27:3507-16
  • Zeibecoglou K, Macfarlane AJ, Ying S, et al. Increases in eotaxin-positive cells in induced sputum from atopic asthmatic subjects after inhalational allergen challenge. Allergy 1999;54:730-5
  • Yamada H, Yamaguchi M, Yamamoto K, et al. Eotaxin in induced sputum of asthmatics: relationship with eosinophils and eosinophil cationic protein in sputum. Allergy 2000;55:392-7
  • Humbles AA, Lu B, Friend DS, et al. The murine CCR3 receptor regulates both the role of eosinophils and mast cells in allergen-induced airway inflammation and hyperresponsiveness. Proc Natl Acad Sci USA 2002;99:1479-84
  • Ma W, Bryce PJ, Humbles AA, et al. CCR3 is essential for skin eosinophilia and airway hyperresponsiveness in a murine model of allergic skin inflammation. J Clin Invest 2002;109:621-8
  • Pope SM, Zimmermann N, Stringer KF, et al. The eotaxin chemokines and CCR3 are fundamental regulators of allergen-induced pulmonary eosinophilia. J Immunol 2005;175:5341-50
  • Eum SY, Haile S, Lefort J, et al. Eosinophil recruitment into the respiratory epithelium following antigenic challenge in hyper-IgE mice is accompanied by interleukin 5-dependent bronchial hyperresponsiveness. Proc Natl Acad Sci USA 1995;92:12290-4
  • Foster PS, Hogan SP, Ramsay AJ, et al. Interleukin 5 deficiency abolishes eosinophilia, airways hyperreactivity, and lung damage in a mouse asthma model. J Exp Med 1996;183:195-201
  • Leckie MJ, ten Brinke A, Khan J, et al. Effects of an interleukin-5 blocking monoclonal antibody on eosinophils, airway hyper-responsiveness, and the late asthmatic response. Lancet 2000;356:2144-8
  • Kariyawasam HH, Robinson DS. The role of eosinophils in airway tissue remodelling in asthma. Curr Opin Immunol 2007;19:681-6
  • Venge P. The eosinophil and airway remodelling in asthma. Clin Respir J 2010;4(Suppl 1):15-19
  • Haldar P, Brightling CE, Hargadon B, et al. Mepolizumab and exacerbations of refractory eosinophilic asthma. N Engl J Med 2009;360:973-84
  • Nair P, Pizzichini MM, Kjarsgaard M, et al. Mepolizumab for prednisone-dependent asthma with sputum eosinophilia. N Engl J Med 2009;360:985-93
  • Blanchard C, Wang N, Stringer KF, et al. Eotaxin-3 and a uniquely conserved gene-expression profile in eosinophilic esophagitis. J Clin Invest 2006;116:536-47
  • Stein ML, Collins MH, Villanueva JM, et al. Anti-IL-5 (mepolizumab) therapy for eosinophilic esophagitis. J Allergy Clin Immunol 2006;118:1312-19
  • Pease JE. Asthma, allergy and chemokines. Curr Drug Targets 2006;7:3-12
  • Pease JE, Williams TJ. The attraction of chemokines as a target for specific anti-inflammatory therapy. Br J Pharmacol 2006;147(Suppl 1):S212-21
  • Salib RJ, Kumar S, Wilson SJ, Howarth PH. Nasal mucosal immunoexpression of the mast cell chemoattractants TGF-beta, eotaxin, and stem cell factor and their receptors in allergic rhinitis. J Allergy Clin Immunol 2004;114:799-806
  • Francis JN, Lloyd CM, Sabroe I, et al. T lymphocytes expressing CCR3 are increased in allergic rhinitis compared with non-allergic controls and following allergen immunotherapy. Allergy 2007;62:59-65
  • Yawalkar N, Uguccioni M, Scharer J, et al. Enhanced expression of eotaxin and CCR3 in atopic dermatitis. J Invest Dermatol 1999;113:43-8
  • Petering H, Kluthe C, Dulkys Y, et al. Characterization of the CC chemokine receptor 3 on human keratinocytes. J Invest Dermatol 2001;116:549-55
  • Gaspar K, Kukova G, Bunemann E, et al. The chemokine receptor CCR3 participates in tissue remodeling during atopic skin inflammation. J Dermatol Sci 2013;71:12-21
  • Takeda A, Baffi JZ, Kleinman ME, et al. CCR3 is a target for age-related macular degeneration diagnosis and therapy. Nature 2009;460:225-30
  • Zhou WJ, Liu GQ, Li LB, et al. Inhibitory effect of CCR3 signal on alkali-induced corneal neovascularization. Int J Ophthalmol 2012;5:251-7
  • Mizutani T, Ashikari M, Tokoro M, et al. Suppression of laser-induced choroidal neovascularization by a CCR3 antagonist. Invest Ophthalmol Vis Sci 2013;54:1564-72
  • Li Y, Huang D, Xia X, et al. CCR3 and choroidal neovascularization. PLoS One 2011;6:e17106
  • Willems LI, Ijzerman AP. Small molecule antagonists for chemokine CCR3 receptors. Med Res Rev 2010;30:778-817
  • Gong L, Wilhelm RS. CCR3 antagonists: a survey of the patent literature. Expert Opin Ther Pat 2009;19:1109-32
  • Catley MC, Coote J, Bari M, Tomlinson KL. Monoclonal antibodies for the treatment of asthma. Pharmacol Ther 2011;132:333-51
  • Bhowmick B, Singh D. Novel anti-inflammatory treatments for asthma. Expert Rev Respir Med 2008;2:617-29
  • White JR, Lee JM, Dede K, et al. Identification of potent, selective non-peptide CC chemokine receptor-3 antagonist that inhibits eotaxin-, eotaxin-2-, and monocyte chemotactic protein-4-induced eosinophil migration. J Biol Chem 2000;275:36626-31
  • Takeda A, Baffi JZ, Kleinman ME, et al. CCR3 is a target for age-related macular degeneration diagnosis and therapy. Nature 2009;460:225-30
  • Ly TW, Forrester JA. Arylsulfonamide CCR3 antagonists. US20100273795; 2010
  • Wang H, Wittchen ES, Jiang Y, et al. Upregulation of CCR3 by age-related stresses promotes choroidal endothelial cell migration via VEGF-dependent and -independent signaling. Invest Ophthalmol Vis Sci 2011;52:8271-7
  • Adamson P, Shima D, Eric YS. Methods of treatment and prevention of eye diseases. WO2013079696A1; 2013
  • Li Y, Huang D, Xia X, et al. CCR3 and choroidal neovascularization. PLoS One 2011;6:1-8
  • De Lucca GV, Kim UT, Vargo BJ, et al. Discovery of CC chemokine receptor-3 (CCR3) antagonists with picomolar potency. J Med Chem 2005;48:2194-211
  • Pruitt JR, Batt DG, Wacker DA, et al. CC chemokine receptor-3 (CCR3) antagonists: improving the selectivity of DPC168 by reducing central ring lipophilicity. Bioorg Med Chem Lett 2007;17:2992-7
  • Santella JB III, Gardner DS, Yao W, et al. From rigid cyclic templates to conformationally stabilized acyclic scaffolds. Part I: the discovery of CCR3 antagonist development candidate BMS-639623 with picomolar inhibition potency against eosinophil chemotaxis. Bioorg Med Chem Lett 2008;18:576-85
  • Perks B. Synthetic chemists catch their breath. Chemistry World. 2004.1: Available from: http://www.rsc.org/chemistryworld/Issues/2004/August/chemists.asp
  • Dhar TG, Yang G, Davies P, et al. Urea based CCR3 antagonists employing a tetrahydro-1,3-oxazin-2-one spacer. Bioorg Med Chem Lett 2009;19:96-9
  • Sato I, Morihira K, Inami H, et al. Synthesis and structure-activity relationships of N-{1-[(6-fluoro-2-naphthyl)methyl]piperidin-4-yl}benzamide derivatives as novel CCR3 antagonists. Bioorg Med Chem 2008;16:144-56
  • Sato I, Morihira K, Inami H, et al. Design and synthesis of 6-fluoro-2-naphthyl derivatives as novel CCR3 antagonists with reduced CYP2D6 inhibition. Bioorg Med Chem 2008;16:8607-18
  • Takahashi T, Imaoka T, Tanida K, et al. Triazolo derivatives and chemokine inhibitors containing the same as the active ingredient patent. WO2000034278; 2000
  • Nitta A, Iura Y, Tomioka H, et al. Discovery and structure-activity relationships of urea derivatives as potent and novel CCR3 antagonists. Bioorg Med Chem Lett 2012;22:4951-4
  • Nitta A, Iura Y, Inoue H, et al. Pyrrolidinyl phenylurea derivatives as novel CCR3 antagonists. Bioorg Med Chem Lett 2012;22:6876-81
  • Suzuki K, Morokata T, Morihira K, et al. A dual antagonist for chemokine CCR3 receptor and histamine H1 receptor. Eur J Pharmacol 2007;563:224-32
  • Bahl A, Barton P, Bowers K, et al. The discovery of CCR3/H1 dual antagonists with reduced hERG risk. Bioorg Med Chem Lett 2012;22:6688-93
  • Bahl A, Barton P, Bowers K, et al. Scaffold-hopping with zwitterionic CCR3 antagonists: identification and optimisation of a series with good potency and pharmacokinetics leading to the discovery of AZ12436092. Bioorg Med Chem Lett 2012;22:6694-9
  • Furber M, Alcaraz L, Luckhurst C, et al. Discovery and evolution of phenoxypiperidine hydroxyamide dual CCR3/H(1) antagonists. Part I. Bioorg Med Chem Lett 2012;22:7702-6
  • Furber M, Alcaraz L, Luckhurst C, et al. Discovery and evolution of phenoxypiperidine hydroxyamide dual CCR3/H(1) antagonists. Part II: optimising in vivo clearance. Bioorg Med Chem Lett 2012;22:7707-10
  • Astra Zeneca Annual report. 2006. Available from: http://www.astrazeneca-annualreports.com/2006/astrazeneca-annual-report-20F-2006.pdf
  • Greiff L, Ahlstrom-Emanuelsson C, Bahl A, et al. Effects of a dual CCR3 and H1-antagonist on symptoms and eosinophilic inflammation in allergic rhinitis. Respir Res 2010;11:1-9
  • Gauvreau GM, Boulet LP, Cockcroft DW, et al. Antisense therapy against CCR3 and the common beta chain attenuates allergen-induced eosinophilic responses. Am J Respir Crit Care Med 2008;177:952-8
  • Imaoka H, Campbell H, Babirad I, et al. TPI ASM8 reduces eosinophil progenitors in sputum after allergen challenge. Clin Exp Allergy 2011;41:1740-6
  • Pharmaxis. Pharmaxis Completes Phase II Clinical Study With ASM8 in Asthma Patients. 2012. Available from: http://www.evaluategroup.com/Universal/View.aspx?type=Story&id=288742
  • Daily news on ASX-listed biotechnology companies. Biotech Daily. 2013. Available from: http://wwwbiotechdailycomau/media/backissues/2013/05%20May/BD%20Biotech%20Daily%20May%2028apdf
  • Horuk R. Chemokine receptor antagonists: overcoming developmental hurdles. Nat Rev Drug Discov 2009;8:23-33
  • Bonecchi R, Bianchi G, Bordignon PP, et al. Differential expression of chemokine receptors and chemotactic responsiveness of type 1 T helper cells (Th1s) and Th2s. J Exp Med 1998;187:129-34
  • Sallusto F, Lenig D, Mackay CR, Lanzavecchia A. Flexible programs of chemokine receptor expression on human polarized T helper 1 and 2 lymphocytes. J Exp Med 1998;187:875-83
  • Imai T, Nagira M, Takagi S, et al. Selective recruitment of CCR4-bearing Th2 cells toward antigen-presenting cells by the CC chemokines thymus and activation-regulated chemokine and macrophage-derived chemokine. Int Immunol 1999;11:81-8
  • Yamamoto J, Adachi Y, Onoue Y, et al. Differential expression of the chemokine receptors by the Th1- and Th2-type effector populations within circulating CD4+ T cells. J Leukoc Biol 2000;68:568-74
  • Annunziato F, Cosmi L, Galli G, et al. Assessment of chemokine receptor expression by human Th1 and Th2 cells in vitro and in vivo. J Leukoc Biol 1999;65:691-9
  • Chantry D, Romagnani P, Raport CJ, et al. Macrophage-derived chemokine is localized to thymic medullary epithelial cells and is a chemoattractant for CD3(+), CD4(+), CD8(low) thymocytes. Blood 1999;94:1890-8
  • Mikhak Z, Strassner JP, Luster AD. Lung dendritic cells imprint T cell lung homing and promote lung immunity through the chemokine receptor CCR4. J Exp Med 2013;210:1855-69
  • Chvatchko Y, Hoogewerf AJ, Meyer A, et al. A key role for CC chemokine receptor 4 in lipopolysaccharide-induced endotoxic shock. J Exp Med 2000;191:1755-64
  • Guabiraba R, Marques RE, Besnard AG, et al. Role of the chemokine receptors CCR1, CCR2 and CCR4 in the pathogenesis of experimental dengue infection in mice. PLoS One 2010;5:e15680
  • Panina-Bordignon P, Papi A, Mariani M, et al. The C-C chemokine receptors CCR4 and CCR8 identify airway T cells of allergen-challenged atopic asthmatics. J Clin Invest 2001;107:1357-64
  • Lezcano-Meza D, Negrete-Garcia MC, Dante-Escobedo M, Teran LM. The monocyte-derived chemokine is released in the bronchoalveolar lavage fluid of steady-state asthmatics. Allergy 2003;58:1125-30
  • Bochner BS, Hudson SA, Xiao HQ, Liu MC. Release of both CCR4-active and CXCR3-active chemokines during human allergic pulmonary late-phase reactions. J Allergy Clin Immunol 2003;112:930-4
  • Vijayanand P, Durkin K, Hartmann G, et al. Chemokine receptor 4 plays a key role in T cell recruitment into the airways of asthmatic patients. J Immunol 2010;184:4568-74
  • Campbell JJ, Haraldsen G, Pan J, et al. The chemokine receptor CCR4 in vascular recognition by cutaneous but not intestinal memory T cells. Nature 1999;400:776-80
  • Kakinuma T, Nakamura K, Wakugawa M, et al. Serum macrophage-derived chemokine (MDC) levels are closely related with the disease activity of atopic dermatitis. Clin Exp Immunol 2002;127:270-3
  • Fujisawa T, Fujisawa R, Kato Y, et al. Presence of high contents of thymus and activation-regulated chemokine in platelets and elevated plasma levels of thymus and activation-regulated chemokine and macrophage-derived chemokine in patients with atopic dermatitis. J Allergy Clin Immunol 2002;110:139-46
  • Horikawa T, Nakayama T, Hikita I, et al. IFN-gamma-inducible expression of thymus and activation-regulated chemokine/CCL17 and macrophage-derived chemokine/CCL22 in epidermal keratinocytes and their roles in atopic dermatitis. Int Immunol 2002;14:767-73
  • Vestergaard C, Bang K, Gesser B, et al. A Th2 chemokine, TARC, produced by keratinocytes may recruit CLA+CCR4+ lymphocytes into lesional atopic dermatitis skin. J Invest Dermatol 2000;115:640-6
  • Sekiya T, Miyamasu M, Imanishi M, et al. Inducible expression of a Th2-type CC chemokine thymus- and activation-regulated chemokine by human bronchial epithelial cells. J Immunol 2000;165:2205-13
  • Berin MC, Eckmann L, Broide DH, Kagnoff MF. Regulated production of the T helper 2-type T-cell chemoattractant TARC by human bronchial epithelial cells in vitro and in human lung xenografts. Am J Respir Cell Mol Biol 2001;24:382-9
  • Bonner K, Pease JE, Corrigan CJ, et al. CCL17/thymus and activation-regulated chemokine induces calcitonin gene-related peptide in human airway epithelial cells through CCR4. J Allergy Clin Immunol 2013;132:942-50; e1-3
  • Kay AB, Ali FR, Heaney LG, et al. Airway expression of calcitonin gene-related peptide in T-cell peptide-induced late asthmatic reactions in atopics. Allergy 2007;62:495-503
  • Brain SD, Williams TJ. Inflammatory oedema induced by synergism between calcitonin gene-related peptide (CGRP) and mediators of increased vascular permeability. Br J Pharmacol 1985;86:855-60
  • Gonzalo JA, Pan Y, Lloyd CM, et al. Mouse monocyte-derived chemokine is involved in airway hyperreactivity and lung inflammation. J Immunol 1999;163:403-11
  • Lloyd CM, Delaney T, Nguyen T, et al. CC chemokine receptor (CCR)3/eotaxin is followed by CCR4/monocyte-derived chemokine in mediating pulmonary T helper lymphocyte type 2 recruitment after serial antigen challenge in vivo. J Exp Med 2000;191:265-74
  • Kawasaki S, Takizawa H, Yoneyama H, et al. Intervention of thymus and activation-regulated chemokine attenuates the development of allergic airway inflammation and hyperresponsiveness in mice. J Immunol 2001;166:2055-62
  • Iellem A, Mariani M, Lang R, et al. Unique chemotactic response profile and specific expression of chemokine receptors CCR4 and CCR8 by CD4(+)CD25(+) regulatory T cells. J Exp Med 2001;194:847-53
  • Afshar R, Strassner JP, Seung E, et al. Compartmentalized chemokine-dependent regulatory T-cell inhibition of allergic pulmonary inflammation. J Allergy Clin Immunol 2013;131:1644-52
  • Viney JM, Andrew DP, Phillips RM, et al. Distinct conformations of the chemokine receptor CCR4 with implications for its targeting in allergy. J Immunol 2014. [Epub ahead of print]
  • Yoshie O, Fujisawa R, Nakayama T, et al. Frequent expression of CCR4 in adult T-cell leukemia and human T-cell leukemia virus type 1-transformed T cells. Blood 2002;99:1505-11
  • Ferenczi K, Fuhlbrigge RC, Pinkus J, et al. Increased CCR4 expression in cutaneous T cell lymphoma. J Invest Dermatol 2002;119:1405-10
  • Pere H, Montier Y, Bayry J, et al. A CCR4 antagonist combined with vaccines induces antigen-specific CD8+ T cells and tumor immunity against self antigens. Blood 2011;118:4853-62
  • Kuhn CF, Bazin M, Philippe L, et al. Bipiperidinyl carboxylic acid amides as potent, selective, and functionally active CCR4 antagonists. Chem Biol Drug Des 2007;70:268-72
  • Purandare AV, Wan H, Somerville JE, et al. Core exploration in optimization of chemokine receptor CCR4 antagonists. Bioorg Med Chem Lett 2007;17:679-82
  • Yokoyama K, Ishikawa N, Igarashi S, et al. Discovery of potent CCR4 antagonists: synthesis and structure-activity relationship study of 2,4-diaminoquinazolines. Bioorg Med Chem 2008;16:7021-32
  • Baxter A, Johnson T, Kindon N, et al. N-pyrazinyl-phenylsulphonamides and their use in the treatment of chemokine mediated diseases. US7662825B2; 2003
  • Procopiou PA, Ford AJ, Graves RH, et al. Lead optimisation of the N1 substituent of a novel series of indazole arylsulfonamides as CCR4 antagonists and identification of a candidate for clinical investigation. Bioorg Med Chem Lett 2012;22:2730-3
  • Procopiou PA, Barrett JW, Barton NP, et al. Synthesis and structure-activity relationships of indazole arylsulfonamides as allosteric CC-chemokine receptor 4 (CCR4) antagonists. J Med Chem 2013;56:1946-60
  • Cahn A, Hodgson S, Wilson R, et al. Safety, tolerability, pharmacokinetics and pharmacodynamics of GSK2239633, a CC-chemokine receptor 4 antagonist, in healthy male subjects: results from an open-label and from a randomised study. BMC Pharmacol Toxicol 2013;14:14
  • Andrews G, Jones C, Wreggett KA. An intracellular allosteric site for a specific class of antagonists of the CC chemokine G protein-coupled receptors CCR4 and CCR5. Mol Pharmacol 2008;73:855-67
  • Banfield G, Watanabe H, Scadding G, et al. CC chemokine receptor 4 (CCR4) in human allergen-induced late nasal responses. Allergy 2010;65:1126-33
  • Yokoyama K, Ishikawa N, Igarashi S, et al. Potent and orally bioavailable CCR4 antagonists: synthesis and structure-activity relationship study of 2-aminoquinazolines. Bioorg Med Chem 2009;17:64-73
  • Yokoyama K, Ishikawa N, Igarashi S, et al. Potent CCR4 antagonists: synthesis, evaluation, and docking study of 2,4-diaminoquinazolines. Bioorg Med Chem 2008;16:7968-74
  • Nakagami Y, Kawase Y, Yonekubo K, et al. RS-1748, a novel CC chemokine receptor 4 antagonist, inhibits ovalbumin-induced airway inflammation in guinea pigs. Biol Pharm Bull 2010;33:1067-9
  • Nakagami Y, Kawashima K, Etori M, et al. A novel CC chemokine receptor 4 antagonist RS-1269 inhibits ovalbumin-induced ear swelling and lipopolysaccharide-induced endotoxic shock in mice. Basic Clin Pharmacol Toxicol 2010;107:793-7
  • Nakagami Y, Kawashima K, Yonekubo K, et al. Novel CC chemokine receptor 4 antagonist RS-1154 inhibits ovalbumin-induced ear swelling in mice. Eur J Pharmacol 2009;624:38-44
  • Purandare AV, Gao A, Wan H, et al. Identification of chemokine receptor CCR4 antagonist. Bioorg Med Chem Lett 2005;15:2669-72
  • Kaminuma O, Ohtomo T, Mori A, et al. Selective down-regulation of Th2 cell-mediated airway inflammation in mice by pharmacological intervention of CCR4. Clin Exp Allergy 2012;42:315-25
  • Qi H, Zheng Y, Xu E, et al. An antagonist for CCR4 alleviates murine allergic rhinitis by intranasal administration. Int Arch Allergy Immunol 2012;159:297-305
  • Sato T, Komai M, Iwase M, et al. Inhibitory effect of the new orally active CCR4 antagonist K327 on CCR4+CD4+ T cell migration into the lung of mice with ovalbumin-induced lung allergic inflammation. Pharmacology 2009;84:171-82
  • Ishida T, Utsunomiya A, Iida S, et al. Clinical significance of CCR4 expression in adult T-cell leukemia/lymphoma: its close association with skin involvement and unfavorable outcome. Clin Cancer Res 2003;9:3625-34
  • Beck A, Reichert JM. Marketing approval of mogamulizumab: a triumph for glyco-engineering. MAbs 2012;4:419-25
  • Subramaniam JM, Whiteside G, McKeage K, Croxtall JC. Mogamulizumab: first global approval. Drugs 2012;72:1293-8
  • Ishida T, Ito A, Sato F, et al. Stevens-Johnson Syndrome associated with mogamulizumab treatment of adult T-cell leukemia/ lymphoma. Cancer Sci 2013;104:647-50
  • Noel RJ, Putnam PE, Rothenberg ME. Eosinophilic esophagitis. N Engl J Med 2004;351:940-1
  • Owen CG, Jarrar Z, Wormald R, et al. The estimated prevalence and incidence of late stage age related macular degeneration in the UK. Br J Ophthalmol 2012;96:752-6

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