Internalization of the chemokine receptor CCR4 can be evoked by orthosteric and allosteric receptor antagonists

European Journal of Pharmacology

Volumn 729, Issue 1, 2014, Pages 75-85

  Ajram, Laura ^a   Begg, Malcolm ^a   Slack, Robert ^a   Cryan, Jenni ^a   Hall, David ^a   Hodgson, Simon ^a   Ford, Alison ^a   Barnes, Ashley ^a   Swieboda, Dawid ^b   Mousnier, Aurelie ^b   Solari, Roberto ^a,b  

^a GLAXOSMITHKLINE   (United Kingdom)

^b NATIONAL HEART AND LUNG INSTITUTE   (United Kingdom)

Author keywords

CCL17; CCL22; CCR4; Chemokine; MDC; TARC

Indexed keywords

ALLOSTERIC RECEPTOR ANTAGONIST; BETA ARRESTIN; CHEMOKINE RECEPTOR ANTAGONIST; CHEMOKINE RECEPTOR CCR4; F ACTIN; GUANINE NUCLEOTIDE BINDING PROTEIN; GUANOSINE 5' O (3 THIOTRIPHOSPHATE); MACROPHAGE DERIVED CHEMOKINE; ORTHOSTERIC RECEPTOR ANTAGONIST; PERTUSSIS TOXIN; THYMUS AND ACTIVATION REGULATED CHEMOKINE; UNCLASSIFIED DRUG; CCL17 PROTEIN, HUMAN; CCL22 PROTEIN, HUMAN; CCR4 PROTEIN, HUMAN;

ACTIN POLYMERIZATION; ALLOSTERISM; AMINO TERMINAL SEQUENCE; ARTICLE; BINDING SITE; CELL SURFACE; CHEMOTAXIS; CONCENTRATION RESPONSE; CONFOCAL MICROSCOPY; CONTROLLED STUDY; ENDOCYTOSIS; HUMAN; HUMAN CELL; INTERNALIZATION; INTRACELLULAR SIGNALING; LIGAND BINDING; MEMBRANE BINDING; PRIORITY JOURNAL; RECEPTOR BINDING; RECEPTOR BLOCKING; RECEPTOR INTERNALIZATION; ANIMAL; ANTAGONISTS AND INHIBITORS; BASOPHIL; CELL CULTURE; CHO CELL LINE; CRICETULUS; DOSE RESPONSE; DRUG EFFECTS; HAMSTER; METABOLISM; PHYSIOLOGY;

ALLOSTERIC REGULATION; ANIMALS; BASOPHILS; CELLS, CULTURED; CHEMOKINE CCL17; CHEMOKINE CCL22; CHEMOTAXIS; CHO CELLS; CRICETINAE; CRICETULUS; DOSE-RESPONSE RELATIONSHIP, DRUG; ENDOCYTOSIS; HUMANS; RECEPTORS, CCR4;

EID: 84894823040     PISSN: 00142999     EISSN: 18790712     Source Type: Journal    
DOI: 10.1016/j.ejphar.2014.02.007     Document Type: Article

References (28)

1. G. Andrews, C. Jones, and K.A. Wreggett An intracellular allosteric site for a specific class of antagonists of the CC chemokine G protein-coupled receptors CCR4 and CCR5 Mol. Pharmacol. 73 2008 855 867 (Pubitemid 351397890)
2. R. Bonecchi, G. Bianchi, P.P. Bordignon, D. D'Ambrosio, R. Lang, A. Borsatti, S. Sozzani, P. Allavena, P.A. Gray, A. Mantovani, and F. Sinigaglia Differential expression of chemokine receptors and chemotactic responsiveness of type 1 T helper cells (Th1s) and Th2s J. Exp. Med. 187 1998 129 134 (Pubitemid 28044828)
3. A. Cahn, S. Hodgson, R. Wilson, J. Robertson., J. Watson, M. Beerahee, S.C. Hughes, G. Young, R. Graves, D. Hall, S. van Marle, and R. Solari 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. 14 2013 14
4. J.J. Campbell, G. Haraldsen, J. Pan, J. Rottman, S. Qin, P. Ponath, D.P. Andrew, R. Warnke, N. Ruffing, N. Kassam, L. Wu, and E.C. Butcher. The chemokine receptor CCR4 in vascular recognition by cutaneous but not intestinal memory T cells Nature 400 1999 776 780 (Pubitemid 29399540)
5. Y. Cheng, and W.H. Prusoff Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction Biochem. Pharmacol. 22 1973 3099 3108
6. A. Christopoulos, and T. Kenakin G protein-coupled receptor allosterism and complexing Pharmacol. Rev. 54 2002 323 374 (Pubitemid 34575719)
7. E.H. Demont, B.I. Andrews, R.A. Bit, C.A. Campbell, J.W.B. Cooke, N. Deeks, S. Desai, S.J. Dowell, P. Gaskin, J.R.J. Gray, A. Haynes, D.S. Holmes, U. Kumar, M.A. Morse, G.J. Osborne, T. Panchal, B. Patel, A. Perboni, S. Taylor, R. Watson, J. Witherington, and R. Willis Discovery of a selective S1P1 receptor agonist efficacious at low oral dose and devoid of effects on heart rate ACS Med. Chem. Lett. 2 2011 444 449
8. J.A. Gonzalo, Y. Pan, C.M. Lloyd, G.Q. Jia, G. Yu, B. Dussault, C.A. Powers, A.E. Proudfoot, A.J. Coyle, D. Gearing, and J.C. Gutierrez-Ramos Mouse monocyte-derived chemokine is involved in airway hyperreactivity and lung inflammation J. Immunol. 163 1999 403 411 (Pubitemid 29295867)
9. D.A. Hall Application of receptor theory to allosteric modulation of receptors Prog. Mol. Biol. Transl. Sci. 115 2013 217 290
10. A. Iellem, M. Mariani, R. Lang, H. Recalde, P. Panina-Bordignon, F. Sinigaglia, and D. D'Ambrosio Unique chemotactic response profile and specific expression of chemokine receptors CCR4 and CCR8 by CD4(+)CD25(+) regulatory T cells J. Exp. Med. 194 2001 847 853 (Pubitemid 32983019)
11. S. Kawasaki, H. Takizawa, H. Yoneyama, T. Nakayama, R. Fujisawa, M. Izumizaki, T. Imai, O. Yoshie, I. Homma, K. Yamamoto, and K. Matsushima Intervention of thymus and activation-regulated chemokine attenuates the development of allergic airway inflammation and hyperresponsiveness in mice J. Immunol. 166 2001 2055 2062 (Pubitemid 32114695)
12. M. Mariani, R. Lang, E. Binda, P. Panina-Bordignon, and D. D'Ambrosio Dominance of CCL22 over CCL17 in induction of chemokine receptor CCR4 desensitization and internalization on human Th2 cells Eur. J. Immunol. 34 2004 231 240 (Pubitemid 38111539)
13. K.T. Nouri-Aria, D. Wilson, J.N. Francis, L.A. Jopling, M.R. Jacobson, M.R. Hodge, D.P. Andrew, S.J. Till, E.M. Varga, T.,J. Williams, J.E. Pease, C.M. Lloyd, I. Sabroe, and S.R. Durham CCR4 in human allergen-induced late responses in the skin and lung Eur. J. Immunol. 32 2002 1933 1938 (Pubitemid 34814549)
14. R. Pal, A. Garzino-Demo, P.D. Markham, J. Burns, M. Brown, R.C. Gallo, and A.L. DeVico Inhibition of HIV-1 infection by the b-chemokine MDC Science 278 1997 695 698 (Pubitemid 27464969)
15. P. Panina-Bordignon, A. Papi, M. Mariani, P. Di Lucia, G. Casoni, C. Bellettato, C. Buonsanti, D. Miotto, C. Mapp, A. Villa, G. Arrigoni, L.M. Fabbri, and F. Sinigaglia The C-C chemokine receptors CCR4 and CCR8 identify airway T cells of allergen-challenged atopic asthmatics J. Clin. Invest. 107 2001 1357 1364 (Pubitemid 32522029)
16. C.A. Power, A. Meyer, K. Nemeth, K.B. Bacon, A.J. Hoogewerf, A.E. Proudfoot, and T.N. Wells Molecular cloning and functional expression of a novel CC chemokine receptor cDNA from a human basophilic cell line J. Biol. Chem. 270 1995 19495 19500
17. P.A. Procopiou, A.J. Ford, R.H. Graves, D.A. Hall, S.T. Hodgson, Y.M. Lacroix, D. Needham, and R.J. Slack 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. 22 2012 2730 2733
18. Purandare A.V., 2004. World patent WO2004020584. March 11.
19. A.V. Purandare, and J.E. Somerville Antagonists of CCR4 as immunomodulatory agents Curr. Top. Med. Chem. 6 2006 1335 1344 (Pubitemid 44144919)
20. Y. Reiss, A.E. Proudfoot, C.A. Power, J.J. Campbell, and G. Butcher CC chemokine receptor (CCR)4 and the CCR10 ligand cutaneous T cell-attracting chemokine (CTACK) in lymphocyte trafficking to inflamed skin J. Exp. Med. 194 2001 1541 1547 (Pubitemid 33081528)
21. T. Sato, M. Iwase, M. Miyama, M. Komai, E. Ohshima, A. Asai, H. Yano, and I. Miki Internalization of CCR4 and inhibition of chemotaxis by K777, a potent and selective CCR4 antagonist Pharmacology 91 2013 305 313
22. S. Sebastiani, G. Danelon, B. Gerber, and M. Uguccioni CCL22-induced responses are powerfully enhanced by synergy inducing chemokines via CCR4: evidence for the involvement of first beta-strand of chemokine Eur. J. Immunol. 35 2005 746 756 (Pubitemid 40425530)
23. R.J. Slack, L.J. Russell, D.A. Hall, M.A. Luttmann, A.J. Ford, K.A. Saunders, S.T. Hodgson, H.E. Connor, C. Browning, and K.L. Clark Pharmacological characterization of GSK1004723, a novel, long-acting antagonist at histamine H(1) and H(3) receptors Br. J. Pharmacol. 164 2011 1627 1641
24. R.J. Slack, and D.A. Hall Development of operational models of receptor activation including constitutive receptor activity and their use to determine the efficacy of the chemokine CCL17 at the CC chemokine receptor CCR4 Br. J. Pharmacol. 166 2012 1774 1792
25. S. Struyf, P. Proost., S. Sozzani, A. Mantovani, A. Wuyts, E. De Clercq, D. Schols, and J. Van Damme Enhanced anti-HIV-1 activity and altered chemotactic potency of NH2-terminally processed macrophage-derived chemokine (MDC) imply an additional MDC receptor J. Immunol. 161 1998 2672 2675 (Pubitemid 28425683)
26. A.J. Ulmer, W. Scholz, M. Ernst, E. Brandt, and H.-D. Flad Isolation and subfractionation of human peripheral blood mononuclear cells (PBMC) by density gradient centrifugation on Percoll Immunobiology 166 1983 238 250
27. C. Weston, and D. Hall Functional studies in primary human T cells indicate a second allosteric regulatory site on CCR4 Proc. Br. Pharm. Soc. 6 2008 066P
28. P.T. Yang, H. Kasai, L.J. Zhao, W.G. Xiao, F. Tanabe, and M. Ito Increased CCR4 expression on circulating CD4(+) T cells in ankylosing spondylitis, rheumatoid arthritis and systemic lupus erythematosus Clin. Exp. Immunol. 138 2004 342 347 (Pubitemid 39472454)