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Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).
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Chemokine receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on Chemokine Receptors [6,79-80]) comprise a large subfamily of 7TM proteins that bind one or more chemokines, a large family of small cytokines typically possessing chemotactic activity for leukocytes. Additional hematopoietic and non-hematopoietic roles have been identified for many chemokines in the areas of embryonic development, immune cell proliferation, activation and death, viral infection, and as antibacterials, among others. Chemokine receptors can be divided by function into two main groups: G protein-coupled chemokine receptors, which mediate leukocyte trafficking, and "Atypical chemokine receptors", which may signal through non-G protein-coupled mechanisms and act as chemokine scavengers to downregulate inflammation or shape chemokine gradients [6].
Chemokines in turn can be divided by structure into four subclasses by the number and arrangement of conserved cysteines. CC (also known as β-chemokines; n= 28), CXC (also known as α-chemokines; n= 17) and CX3C (n= 1) chemokines all have four conserved cysteines, with zero, one and three amino acids separating the first two cysteines respectively. C chemokines (n= 2) have only the second and fourth cysteines found in other chemokines. Chemokines can also be classified by function into homeostatic and inflammatory subgroups. Most chemokine receptors are able to bind multiple high-affinity chemokine ligands, but the ligands for a given receptor are almost always restricted to the same structural subclass. Most chemokines bind to more than one receptor subtype. Receptors for inflammatory chemokines are typically highly promiscuous with regard to ligand specificity, and may lack a selective endogenous ligand. G protein-coupled chemokine receptors are named acccording to the class of chemokines bound, whereas ACKR is the root acronym for atypical chemokine receptors [7]. There can be substantial cross-species differences in the sequences of both chemokines and chemokine receptors, and in the pharmacology and biology of chemokine receptors. Endogenous and microbial non-chemokine ligands have also been identified for chemokine receptors. Many chemokine receptors function as HIV co-receptors, but CCR5 is the only one demonstrated to play an essential role in HIV/AIDS pathogenesis. The tables include both standard chemokine receptor names [125] and aliases.
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* Key recommended reading is highlighted with an asterisk
* Bachelerie F, Ben-Baruch A, Burkhardt AM, Combadiere C, Farber JM, Graham GJ, Horuk R, Sparre-Ulrich AH, Locati M, Luster AD et al.. (2014) International Union of Pharmacology. LXXXIX. Update on the extended family of chemokine receptors and introducing a new nomenclature for atypical chemokine receptors. Pharmacol Rev, 66 (1): 1-79. [PMID:24218476]
* Bachelerie F, Graham GJ, Locati M, Mantovani A, Murphy PM, Nibbs R, Rot A, Sozzani S, Thelen M. (2015) An atypical addition to the chemokine receptor nomenclature: IUPHAR Review 15. Br J Pharmacol, 172 (16): 3945-9. [PMID:25958743]
* Koelink PJ, Overbeek SA, Braber S, de Kruijf P, Folkerts G, Smit MJ, Kraneveld AD. (2012) Targeting chemokine receptors in chronic inflammatory diseases: an extensive review. Pharmacol Ther, 133 (1): 1-18. [PMID:21839114]
* Murphy PM. (2002) International Union of Pharmacology. XXX. Update on chemokine receptor nomenclature. Pharmacol Rev, 54 (2): 227-9. [PMID:12037138]
* Murphy PM, Baggiolini M, Charo IF, Hébert CA, Horuk R, Matsushima K, Miller LH, Oppenheim JJ, Power CA. (2000) International union of pharmacology. XXII. Nomenclature for chemokine receptors. Pharmacol Rev, 52 (1): 145-76. [PMID:10699158]
Muñoz LM, Lucas P, Holgado BL, Barroso R, Vega B, Rodríguez-Frade JM, Mellado M. (2011) Receptor oligomerization: a pivotal mechanism for regulating chemokine function. Pharmacol Ther, 131 (3): 351-8. [PMID:21600920]
* Scholten DJ, Canals M, Maussang D, Roumen L, Smit MJ, Wijtmans M, de Graaf C, Vischer HF, Leurs R. (2012) Pharmacological modulation of chemokine receptor function. Br J Pharmacol, 165 (6): 1617-43. [PMID:21699506]
Szpakowska M, Fievez V, Arumugan K, van Nuland N, Schmit JC, Chevigné A. (2012) Function, diversity and therapeutic potential of the N-terminal domain of human chemokine receptors. Biochem Pharmacol, 84 (10): 1366-80. [PMID:22935450]
Wedemeyer MJ, Mahn SA, Getschman AE, Crawford KS, Peterson FC, Marchese A, McCorvy JD, Volkman BF. (2020) The chemokine X-factor: Structure-function analysis of the CXC motif at CXCR4 and ACKR3. J Biol Chem, 295 (40): 13927-13939. [PMID:32788219]
White GE, Iqbal AJ, Greaves DR. (2013) CC chemokine receptors and chronic inflammation--therapeutic opportunities and pharmacological challenges. Pharmacol Rev, 65 (1): 47-89. [PMID:23300131]
1. Ahuja SK, Murphy PM. (1996) The CXC chemokines growth-regulated oncogene (GRO) alpha, GRObeta, GROgamma, neutrophil-activating peptide-2, and epithelial cell-derived neutrophil-activating peptide-78 are potent agonists for the type B, but not the type A, human interleukin-8 receptor. J Biol Chem, 271 (34): 20545-50. [PMID:8702798]
2. Ai LS, Liao F. (2002) Mutating the four extracellular cysteines in the chemokine receptor CCR6 reveals their differing roles in receptor trafficking, ligand binding, and signaling. Biochemistry, 41 (26): 8332-41. [PMID:12081481]
3. Antoniu SA. (2010) Mogamulizumab, a humanized mAb against C-C chemokine receptor 4 for the potential treatment of T-cell lymphomas and asthma. Curr Opin Mol Ther, 12 (6): 770-9. [PMID:21154168]
4. Baba M, Imai T, Nishimura M, Kakizaki M, Takagi S, Hieshima K, Nomiyama H, Yoshie O. (1997) Identification of CCR6, the specific receptor for a novel lymphocyte-directed CC chemokine LARC. J Biol Chem, 272 (23): 14893-8. [PMID:9169459]
5. Baba M, Nishimura O, Kanzaki N, Okamoto M, Sawada H, Iizawa Y, Shiraishi M, Aramaki Y, Okonogi K, Ogawa Y et al.. (1999) A small-molecule, nonpeptide CCR5 antagonist with highly potent and selective anti-HIV-1 activity. Proc Natl Acad Sci USA, 96 (10): 5698-703. [PMID:10318947]
6. Bachelerie F, Ben-Baruch A, Burkhardt AM, Combadiere C, Farber JM, Graham GJ, Horuk R, Sparre-Ulrich AH, Locati M, Luster AD et al.. (2014) International Union of Pharmacology. LXXXIX. Update on the extended family of chemokine receptors and introducing a new nomenclature for atypical chemokine receptors. Pharmacol Rev, 66 (1): 1-79. [PMID:24218476]
7. Bachelerie F, Graham GJ, Locati M, Mantovani A, Murphy PM, Nibbs R, Rot A, Sozzani S, Thelen M. (2015) An atypical addition to the chemokine receptor nomenclature: IUPHAR Review 15. Br J Pharmacol, 172 (16): 3945-9. [PMID:25958743]
8. Barella L, Loetscher M, Tobler A, Baggiolini M, Moser B. (1995) Sequence variation of a novel heptahelical leucocyte receptor through alternative transcript formation. Biochem J, 309 ( Pt 3): 773-9. [PMID:7639692]
9. Barnea G, Strapps W, Herrada G, Berman Y, Ong J, Kloss B, Axel R, Lee KJ. (2008) The genetic design of signaling cascades to record receptor activation. Proc Natl Acad Sci USA, 105 (1): 64-9. [PMID:18165312]
10. Barroso R, Martínez Muñoz L, Barrondo S, Vega B, Holgado BL, Lucas P, Baíllo A, Sallés J, Rodríguez-Frade JM, Mellado M. (2012) EBI2 regulates CXCL13-mediated responses by heterodimerization with CXCR5. FASEB J, 26 (12): 4841-54. [PMID:22913878]
11. Ben-Baruch A, Xu L, Young PR, Bengali K, Oppenheim JJ, Wang JM. (1995) Monocyte chemotactic protein-3 (MCP3) interacts with multiple leukocyte receptors. C-C CKR1, a receptor for macrophage inflammatory protein-1 alpha/Rantes, is also a functional receptor for MCP3. J Biol Chem, 270 (38): 22123-8. [PMID:7545673]
12. Berson JF, Long D, Doranz BJ, Rucker J, Jirik FR, Doms RW. (1996) A seven-transmembrane domain receptor involved in fusion and entry of T-cell-tropic human immunodeficiency virus type 1 strains. J Virol, 70 (9): 6288-95. [PMID:8709256]
13. Bertini R, Allegretti M, Bizzarri C, Moriconi A, Locati M, Zampella G, Cervellera MN, Di Cioccio V, Cesta MC, Galliera E et al.. (2004) Noncompetitive allosteric inhibitors of the inflammatory chemokine receptors CXCR1 and CXCR2: prevention of reperfusion injury. Proc Natl Acad Sci USA, 101 (32): 11791-6. [PMID:15282370]
14. Blanpain C, Migeotte I, Lee B, Vakili J, Doranz BJ, Govaerts C, Vassart G, Doms RW, Parmentier M. (1999) CCR5 binds multiple CC-chemokines: MCP-3 acts as a natural antagonist. Blood, 94 (6): 1899-905. [PMID:10477718]
15. Bozic CR, Gerard NP, von Uexkull-Guldenband C, Kolakowski Jr LF, Conklyn MJ, Breslow R, Showell HJ, Gerard C. (1994) The murine interleukin 8 type B receptor homologue and its ligands. Expression and biological characterization. J Biol Chem, 269 (47): 29355-8. [PMID:7961909]
16. Brodfuehrer J, Rankin A, Edmonds J, Keegan S, Andreyeva T, Lawrence-Henderson R, Ozer J, Gao H, Bloom L, Boisvert A et al.. (2014) Quantitative analysis of target coverage and germinal center response by a CXCL13 neutralizing antibody in a T-dependent mouse immunization model. Pharm Res, 31 (3): 635-48. [PMID:24190631]
17. Charo IF, Myers SJ, Herman A, Franci C, Connolly AJ, Coughlin SR. (1994) Molecular cloning and functional expression of two monocyte chemoattractant protein 1 receptors reveals alternative splicing of the carboxyl-terminal tails. Proc Natl Acad Sci USA, 91 (7): 2752-6. [PMID:8146186]
18. Chou CC, Fine JS, Pugliese-Sivo C, Gonsiorek W, Davies L, Deno G, Petro M, Schwarz M, Zavodny PJ, Hipkin RW. (2002) Pharmacological characterization of the chemokine receptor, hCCR1 in a stable transfectant and differentiated HL-60 cells: antagonism of hCCR1 activation by MIP-1beta. Br J Pharmacol, 137 (5): 663-75. [PMID:12381680]
19. Combadiere C, Ahuja SK, Murphy PM. (1995) Cloning and functional expression of a human eosinophil CC chemokine receptor. J Biol Chem, 270 (28): 16491-4. [PMID:7622448]
20. Combadiere C, Ahuja SK, Murphy PM. (1995) Cloning, chromosomal localization, and RNA expression of a human beta chemokine receptor-like gene. DNA Cell Biol, 14: 673-680. [PMID:7646814]
21. Combadiere C, Ahuja SK, Van Damme J, Tiffany HL, Gao JL, Murphy PM. (1995) Monocyte chemoattractant protein-3 is a functional ligand for CC chemokine receptors 1 and 2B. J Biol Chem, 270: 29671-29675. [PMID:8530354]
22. Combadiere C, Salzwedel K, Smith ED, Tiffany HL, Berger EA, Murphy PM. (1998) Identification of CX3CR1. A chemotactic receptor for the human CX3C chemokine fractalkine and a fusion coreceptor for HIV-1. J Biol Chem, 273: 23799-23804. [PMID:9726990]
23. Coulin F, Power CA, Alouani S, Peitsch MC, Schroeder JM, Moshizuki M, Clark-Lewis I, Wells TN. (1997) Characterisation of macrophage inflammatory protein-5/human CC cytokine-2, a member of the macrophage-inflammatory-protein family of chemokines. Eur J Biochem, 248 (2): 507-15. [PMID:9346309]
24. Dairaghi DJ, Fan RA, McMaster BE, Hanley MR, Schall TJ. (1999) HHV8-encoded vMIP-I selectively engages chemokine receptor CCR8. Agonist and antagonist profiles of viral chemokines. J Biol Chem, 274 (31): 21569-74. [PMID:10419462]
25. Daugherty BL, Siciliano SJ, DeMartino JA, Malkowitz L, Sirotina A, Springer MS. (1996) Cloning, expression, and characterization of the human eosinophil eotaxin receptor. J Exp Med, 183 (5): 2349-54. [PMID:8642344]
26. Di Salvo J, Koch GE, Johnson KE, Blake AD, Daugherty BL, DeMartino JA, Sirotina-Meisher A, Liu Y, Springer MS, Cascieri MA et al.. (2000) The CXCR4 agonist ligand stromal derived factor-1 maintains high affinity for receptors in both Galpha(i)-coupled and uncoupled states. Eur J Pharmacol, 409 (2): 143-54. [PMID:11104827]
27. Duggal P, An P, Beaty TH, Strathdee SA, Farzadegan H, Markham RB, Johnson L, O'Brien SJ, Vlahov D, Winkler CA. (2003) Genetic influence of CXCR6 chemokine receptor alleles on PCP-mediated AIDS progression among African Americans. Genes Immun, 4 (4): 245-50. [PMID:12761559]
28. Dunstan CA, Salafranca MN, Adhikari S, Xia Y, Feng L, Harrison JK. (1996) Identification of two rat genes orthologous to the human interleukin-8 receptors. J Biol Chem, 271: 32770-32776. [PMID:8955112]
29. Dwyer MP, Yu Y, Chao J, Aki C, Chao J, Biju P, Girijavallabhan V, Rindgen D, Bond R, Mayer-Ezel R et al.. (2006) Discovery of 2-hydroxy-N,N-dimethyl-3-{2-[[(R)-1-(5- methylfuran-2-yl)propyl]amino]-3,4-dioxocyclobut-1-enylamino}benzamide (SCH 527123): a potent, orally bioavailable CXCR2/CXCR1 receptor antagonist. J Med Chem, 49 (26): 7603-6. [PMID:17181143]
30. Feng Y, Broder CC, Kennedy PE, Berger EA. (1996) HIV-1 entry cofactor: functional cDNA cloning of a seven-transmembrane, G protein-coupled receptor. Science, 272 (5263): 872-7. [PMID:8629022]
31. Fox JC, Nakayama T, Tyler RC, Sander TL, Yoshie O, Volkman BF. (2015) Structural and agonist properties of XCL2, the other member of the C-chemokine subfamily. Cytokine, 71 (2): 302-11. [PMID:25497737]
32. Förster R, Mattis AE, Kremmer E, Wolf E, Brem G, Lipp M. (1996) A putative chemokine receptor, BLR1, directs B cell migration to defined lymphoid organs and specific anatomic compartments of the spleen. Cell, 87 (6): 1037-47. [PMID:8978608]
33. Gao JL, Murphy PM. (1995) Cloning and differential tissue-specific expression of three mouse beta chemokine receptor-like genes, including the gene for a functional macrophage inflammatory protein-1 alpha receptor. J Biol Chem, 270: 17494-17501. [PMID:7542241]
34. Garin A, Tarantino N, Faure S, Daoudi M, Lécureuil C, Bourdais A, Debré P, Deterre P, Combadiere C. (2003) Two novel fully functional isoforms of CX3CR1 are potent HIV coreceptors. J Immunol, 171 (10): 5305-12. [PMID:14607932]
35. Giagulli C, Magiera AK, Bugatti A, Caccuri F, Marsico S, Rusnati M, Vermi W, Fiorentini S, Caruso A. (2012) HIV-1 matrix protein p17 binds to the IL-8 receptor CXCR1 and shows IL-8-like chemokine activity on monocytes through Rho/ROCK activation. Blood, 119 (10): 2274-83. [PMID:22262769]
36. Gladue RP, Tylaska LA, Brissette WH, Lira PD, Kath JC, Poss CS, Brown MF, Paradis TJ, Conklyn MJ, Ogborne KT et al.. (2003) CP-481,715, a potent and selective CCR1 antagonist with potential therapeutic implications for inflammatory diseases. J Biol Chem, 278 (42): 40473-80. [PMID:12909630]
37. Gong X, Gong W, Kuhns DB, Ben-Baruch A, Howard OM, Wang JM. (1997) Monocyte chemotactic protein-2 (MCP-2) uses CCR1 and CCR2B as its functional receptors. J Biol Chem, 272 (18): 11682-5. [PMID:9115216]
38. Gravel S, Malouf C, Boulais PE, Berchiche YA, Oishi S, Fujii N, Leduc R, Sinnett D, Heveker N. (2010) The peptidomimetic CXCR4 antagonist TC14012 recruits beta-arrestin to CXCR7: roles of receptor domains. J Biol Chem, 285 (49): 37939-43. [PMID:20956518]
39. Greaves DR, Wang W, Dairaghi DJ, Dieu MC, Saint-Vis B, Franz-Bacon K, Rossi D, Caux C, McClanahan T, Gordon S et al.. (1997) CCR6, a CC chemokine receptor that interacts with macrophage inflammatory protein 3alpha and is highly expressed in human dendritic cells. J Exp Med, 186 (6): 837-44. [PMID:9294138]
40. Habasque C, Aubry F, Jégou B, Samson M. (2002) Study of the HIV-1 receptors CD4, CXCR4, CCR5 and CCR3 in the human and rat testis. Mol Hum Reprod, 8 (5): 419-25. [PMID:11994538]
41. Hall DA, Beresford IJ, Browning C, Giles H. (1999) Signalling by CXC-chemokine receptors 1 and 2 expressed in CHO cells: a comparison of calcium mobilization, inhibition of adenylyl cyclase and stimulation of GTPgammaS binding induced by IL-8 and GROalpha. Br J Pharmacol, 126 (3): 810-8. [PMID:10188995]
42. Haskell CA, Horuk R, Liang M, Rosser M, Dunning L, Islam I, Kremer L, Gutiérrez J, Marquez G, Martinez-A C et al.. (2006) Identification and characterization of a potent, selective nonpeptide agonist of the CC chemokine receptor CCR8. Mol Pharmacol, 69 (1): 309-16. [PMID:16221874]
43. Hayes IM, Jordan NJ, Towers S, Smith G, Paterson JR, Earnshaw JJ, Roach AG, Westwick J, Williams RJ. (1998) Human vascular smooth muscle cells express receptors for CC chemokines. Arterioscler Thromb Vasc Biol, 18 (3): 397-403. [PMID:9514408]
44. Heesen M, Berman MA, Benson JD, Gerard C, Dorf ME. (1996) Cloning of the mouse fusin gene, homologue to a human HIV-1 co-factor. J Immunol, 157 (12): 5455-60. [PMID:8955194]
45. Heiber M, Docherty JM, Shah G, Nguyen T, Cheng R, Heng HH, Marchese A, Tsui LC, Shi X, George SR et al.. (1995) Isolation of three novel human genes encoding G protein-coupled receptors. DNA Cell Biol, 14 (1): 25-35. [PMID:7832990]
46. Heise CE, Pahuja A, Hudson SC, Mistry MS, Putnam AL, Gross MM, Gottlieb PA, Wade WS, Kiankarimi M, Schwarz D et al.. (2005) Pharmacological characterization of CXC chemokine receptor 3 ligands and a small molecule antagonist. J Pharmacol Exp Ther, 313 (3): 1263-71. [PMID:15761110]
47. Hesselgesser J, Liang M, Hoxie J, Greenberg M, Brass LF, Orsini MJ, Taub D, Horuk R. (1998) Identification and characterization of the CXCR4 chemokine receptor in human T cell lines: ligand binding, biological activity, and HIV-1 infectivity. J Immunol, 160 (2): 877-83. [PMID:9551924]
48. Hesselgesser J, Ng HP, Liang M, Zheng W, May K, Bauman JG, Monahan S, Islam I, Wei GP, Ghannam A et al.. (1998) Identification and characterization of small molecule functional antagonists of the CCR1 chemokine receptor. J Biol Chem, 273 (25): 15687-92. [PMID:9624164]
49. Homey B, Alenius H, Müller A, Soto H, Bowman EP, Yuan W, McEvoy L, Lauerma AI, Assmann T, Bünemann E et al.. (2002) CCL27-CCR10 interactions regulate T cell-mediated skin inflammation. Nat Med, 8 (2): 157-65. [PMID:11821900]
50. Homey B, Wang W, Soto H, Buchanan ME, Wiesenborn A, Catron D, Muller A, McClanahan TK, Dieu-Nosjean MC, Orozco R, Ruzicka T, Lehmann P, Oldham E, Zlotnik A. (2000) Cutting edge: the orphan chemokine receptor G protein-coupled receptor-2 (GPR-2, CCR10) binds the skin-associated chemokine CCL27 (CTACK/ALP/ILC). J Immunol, 164: 3465-3470. [PMID:10725697]
51. Imai T, Chantry D, Raport CJ, Wood CL, Nishimura M, Godiska R, Yoshie O, Gray PW. (1998) Macrophage-derived chemokine is a functional ligand for the CC chemokine receptor 4. J Biol Chem, 273 (3): 1764-8. [PMID:9430724]
52. Imai T, Hieshima K, Haskell C, Baba M, Nagira M, Nishimura M, Kakizaki M, Takagi S, Nomiyama H, Schall TJ et al.. (1997) Identification and molecular characterization of fractalkine receptor CX3CR1, which mediates both leukocyte migration and adhesion. Cell, 91 (4): 521-30. [PMID:9390561]
53. Inngjerdingen M, Damaj B, Maghazachi AA. (2001) Expression and regulation of chemokine receptors in human natural killer cells. Blood, 97 (2): 367-75. [PMID:11154210]
54. Jenh CH, Cox MA, Kaminski H, Zhang M, Byrnes H, Fine J, Lundell D, Chou CC, Narula SK, Zavodny PJ. (1999) Cutting edge: species specificity of the CC chemokine 6Ckine signaling through the CXC chemokine receptor CXCR3: human 6Ckine is not a ligand for the human or mouse CXCR3 receptors. J Immunol, 162 (7): 3765-9. [PMID:10201891]
55. Jinno A, Shimizu N, Soda Y, Haraguchi Y, Kitamura T, Hoshino H. (1998) Identification of the chemokine receptor TER1/CCR8 expressed in brain-derived cells and T cells as a new coreceptor for HIV-1 infection. Biochem Biophys Res Commun, 243 (2): 497-502. [PMID:9480837]
56. Kitaura M, Suzuki N, Imai T, Takagi S, Suzuki R, Nakajima T, Hirai K, Nomiyama H, Yoshie O. (1999) Molecular cloning of a novel human CC chemokine (Eotaxin-3) that is a functional ligand of CC chemokine receptor 3. J Biol Chem, 274 (39): 27975-80. [PMID:10488147]
57. Kledal TN, Rosenkilde MM, Coulin F, Simmons G, Johnsen AH, Alouani S, Power CA, Lüttichau HR, Gerstoft J, Clapham PR et al.. (1997) A broad-spectrum chemokine antagonist encoded by Kaposi's sarcoma-associated herpesvirus. Science, 277 (5332): 1656-9. [PMID:9287217]
58. Kouba M, Vanetti M, Wang X, Schäfer M, Höllt V. (1993) Cloning of a novel putative G-protein-coupled receptor (NLR) which is expressed in neuronal and lymphatic tissue. FEBS Lett, 321 (2-3): 173-8. [PMID:8386678]
59. Kumar S, Kwei GY, Poon GK, Iliff SA, Wang Y, Chen Q, Franklin RB, Didolkar V, Wang RW, Yamazaki M et al.. (2003) Pharmacokinetics and interactions of a novel antagonist of chemokine receptor 5 (CCR5) with ritonavir in rats and monkeys: role of CYP3A and P-glycoprotein. J Pharmacol Exp Ther, 304 (3): 1161-71. [PMID:12604693]
60. Lee J, Horuk R, Rice GC, Bennett GL, Camerato T, Wood WI. (1992) Characterization of two high affinity human interleukin-8 receptors. J Biol Chem, 267 (23): 16283-7. [PMID:1379593]
61. Legler DF, Loetscher M, Roos RS, Clark-Lewis I, Baggiolini M, Moser B. (1998) B cell-attracting chemokine 1, a human CXC chemokine expressed in lymphoid tissues, selectively attracts B lymphocytes via BLR1/CXCR5. J Exp Med, 187 (4): 655-60. [PMID:9463416]
62. Liang M, Mallari C, Rosser M, Ng HP, May K, Monahan S, Bauman JG, Islam I, Ghannam A, Buckman B et al.. (2000) Identification and characterization of a potent, selective, and orally active antagonist of the CC chemokine receptor-1. J Biol Chem, 275 (25): 19000-8. [PMID:10748002]
63. Liao F, Alkhatib G, Peden KW, Sharma G, Berger EA, Farber JM. (1997) STRL33, A novel chemokine receptor-like protein, functions as a fusion cofactor for both macrophage-tropic and T cell line-tropic HIV-1. J Exp Med, 185 (11): 2015-23. [PMID:9166430]
64. Liao F, Lee HH, Farber JM. (1997) Cloning of STRL22, a new human gene encoding a G-protein-coupled receptor related to chemokine receptors and located on chromosome 6q27. Genomics, 40 (1): 175-80. [PMID:9070937]
65. Loetscher M, Amara A, Oberlin E, Brass N, Legler D, Loetscher P, D'Apuzzo M, Meese E, Rousset D, Virelizier JL et al.. (1997) TYMSTR, a putative chemokine receptor selectively expressed in activated T cells, exhibits HIV-1 coreceptor function. Curr Biol, 7 (9): 652-60. [PMID:9285716]
66. Loetscher M, Geiser T, O'Reilly T, Zwahlen R, Baggiolini M, Moser B. (1994) Cloning of a human seven-transmembrane domain receptor, LESTR, that is highly expressed in leukocytes. J Biol Chem, 269 (1): 232-7. [PMID:8276799]
67. Loetscher P, Gong JH, Dewald B, Baggiolini M, Clark-Lewis I. (1998) N-terminal peptides of stromal cell-derived factor-1 with CXC chemokine receptor 4 agonist and antagonist activities. J Biol Chem, 273 (35): 22279-83. [PMID:9712844]
68. Lüttichau HR. (2010) The cytomegalovirus UL146 gene product vCXCL1 targets both CXCR1 and CXCR2 as an agonist. J Biol Chem, 285 (12): 9137-46. [PMID:20044480]
69. Lüttichau HR, Clark-Lewis I, Jensen PØ, Moser C, Gerstoft J, Schwartz TW. (2003) A highly selective CCR2 chemokine agonist encoded by human herpesvirus 6. J Biol Chem, 278 (13): 10928-33. [PMID:12554737]
70. Maeda DY, Peck AM, Schuler AD, Quinn MT, Kirpotina LN, Wicomb WN, Fan GH, Zebala JA. (2014) Discovery of 2-[5-(4-Fluorophenylcarbamoyl)pyridin-2-ylsulfanylmethyl]phenylboronic Acid (SX-517): Noncompetitive Boronic Acid Antagonist of CXCR1 and CXCR2. J Med Chem, 57 (20): 8378-97. [PMID:25254640]
71. Maeda K, Das D, Ogata-Aoki H, Nakata H, Miyakawa T, Tojo Y, Norman R, Takaoka Y, Ding J, Arnold GF, Arnold E, Mitsuya H. (2006) Structural and molecular interactions of CCR5 inhibitors with CCR5. J Biol Chem, 281: 12688-12698. [PMID:16476734]
72. Maeda K, Yoshimura K, Shibayama S, Habashita H, Tada H, Sagawa K, Miyakawa T, Aoki M, Fukushima D, Mitsuya H. (2001) Novel low molecular weight spirodiketopiperazine derivatives potently inhibit R5 HIV-1 infection through their antagonistic effects on CCR5. J Biol Chem, 276 (37): 35194-200. [PMID:11454872]
73. Matloubian M, David A, Engel S, Ryan JE, Cyster JG. (2000) A transmembrane CXC chemokine is a ligand for HIV-coreceptor Bonzo. Nat Immunol, 1 (4): 298-304. [PMID:11017100]
74. Meyrath M, Szpakowska M, Zeiner J, Massotte L, Merz MP, Benkel T, Simon K, Ohnmacht J, Turner JD, Krüger R et al.. (2020) The atypical chemokine receptor ACKR3/CXCR7 is a broad-spectrum scavenger for opioid peptides. Nat Commun, 11 (1): 3033. [PMID:32561830]
75. Miller BE, Mistry S, Smart K, Connolly P, Carpenter DC, Cooray H, Bloomer JC, Tal-Singer R, Lazaar AL. (2015) The pharmacokinetics and pharmacodynamics of danirixin (GSK1325756) - a selective CXCR2 antagonist - in healthy adult subjects. BMC Pharmacol Toxicol, 16 (1): 18. [PMID:26092545]
76. Mirzadegan T, Diehl F, Ebi B, Bhakta S, Polsky I, McCarley D, Mulkins M, Weatherhead GS, Lapierre JM, Dankwardt J et al.. (2000) Identification of the binding site for a novel class of CCR2b chemokine receptor antagonists: binding to a common chemokine receptor motif within the helical bundle. J Biol Chem, 275 (33): 25562-71. [PMID:10770925]
77. Moepps B, Frodl R, Rodewald HR, Baggiolini M, Gierschik P. (1997) Two murine homologues of the human chemokine receptor CXCR4 mediating stromal cell-derived factor 1alpha activation of Gi2 are differentially expressed in vivo. Eur J Immunol, 27 (8): 2102-12. [PMID:9295051]
78. Morokata T, Suzuki K, Masunaga Y, Taguchi K, Morihira K, Sato I, Fujii M, Takizawa S, Torii Y, Yamamoto N et al.. (2006) A novel, selective, and orally available antagonist for CC chemokine receptor 3. J Pharmacol Exp Ther, 317 (1): 244-50. [PMID:16339911]
79. Murphy PM. (2002) International Union of Pharmacology. XXX. Update on chemokine receptor nomenclature. Pharmacol Rev, 54 (2): 227-9. [PMID:12037138]
80. Murphy PM, Baggiolini M, Charo IF, Hébert CA, Horuk R, Matsushima K, Miller LH, Oppenheim JJ, Power CA. (2000) International union of pharmacology. XXII. Nomenclature for chemokine receptors. Pharmacol Rev, 52 (1): 145-76. [PMID:10699158]
81. Napier C, Sale H, Mosley M, Rickett G, Dorr P, Mansfield R, Holbrook M. (2005) Molecular cloning and radioligand binding characterization of the chemokine receptor CCR5 from rhesus macaque and human. Biochem Pharmacol, 71 (1-2): 163-72. [PMID:16298345]
82. Napolitano M, Zingoni A, Bernardini G, Spinetti G, Nista A, Storlazzi CT, Rocchi M, Santoni A. (1996) Molecular cloning of TER1, a chemokine receptor-like gene expressed by lymphoid tissues. J Immunol, 157: 2759-2763. [PMID:8816377]
83. Naya A, Ishikawa M, Matsuda K, Ohwaki K, Saeki T, Noguchi K, Ohtake N. (2003) Structure-activity relationships of xanthene carboxamides, novel CCR1 receptor antagonists. Bioorg Med Chem, 11 (6): 875-84. [PMID:12614873]
84. Olson WC, Maddon PJ, Tsurushita N, Hinton PR, Vasquez M. (2006) Anti-CCR5 antibody. Patent number: US7122185B2. Assignee: CytoDyn Inc; AbbVie Biotherapeutics Inc. Priority date: 22/02/2002. Publication date: 17/10/2006.
85. Ott TR, Lio FM, Olshefski D, Liu XJ, Ling N, Struthers RS. (2006) The N-terminal domain of CCL21 reconstitutes high affinity binding, G protein activation, and chemotactic activity, to the C-terminal domain of CCL19. Biochem Biophys Res Commun, 348 (3): 1089-93. [PMID:16904643]
86. Palani A, Shapiro S, Clader JW, Greenlee WJ, Cox K, Strizki J, Endres M, Baroudy BM. (2001) Discovery of 4-[(Z)-(4-bromophenyl)- (ethoxyimino)methyl]-1'-[(2,4-dimethyl-3- pyridinyl)carbonyl]-4'-methyl-1,4'- bipiperidine N-oxide (SCH 351125): an orally bioavailable human CCR5 antagonist for the treatment of HIV infection. J Med Chem, 44 (21): 3339-42. [PMID:11585437]
87. Parody TR, Stone MJ. (2004) High level expression, activation, and antagonism of CC chemokine receptors CCR2 and CCR3 in Chinese hamster ovary cells. Cytokine, 27 (1): 38-46. [PMID:15207250]
88. Power CA, Church DJ, Meyer A, Alouani S, Proudfoot AE, Clark-Lewis I, Sozzani S, Mantovani A, Wells TN. (1997) Cloning and characterization of a specific receptor for the novel CC chemokine MIP-3alpha from lung dendritic cells. J Exp Med, 186 (6): 825-35. [PMID:9294137]
89. Raport CJ, Schweickart VL, Eddy RL, Shows TB, Gray PW. (1995) The orphan G-protein-coupled receptor-encoding gene V28 is closely related to genes for chemokine receptors and is expressed in lymphoid and neural tissues. Gene, 163: 295-299. [PMID:7590284]
90. Richardson RM, Marjoram RJ, Barak LS, Snyderman R. (2003) Role of the cytoplasmic tails of CXCR1 and CXCR2 in mediating leukocyte migration, activation, and regulation. J Immunol, 170: 2904-2911. [PMID:12626541]
91. Roos RS, Loetscher M, Legler DF, Clark-Lewis I, Baggiolini M, Moser B. (1997) Identification of CCR8, the receptor for the human CC chemokine I-309. J Biol Chem, 272 (28): 17251-4. [PMID:9211859]
92. Ruffing N, Sullivan N, Sharmeen L, Sodroski J, Wu L. (1998) CCR5 has an expanded ligand-binding repertoire and is the primary receptor used by MCP-2 on activated T cells. Cell Immunol, 189 (2): 160-8. [PMID:9790730]
93. Sabroe I, Peck MJ, Van Keulen BJ, Jorritsma A, Simmons G, Clapham PR, Williams TJ, Pease JE. (2000) A small molecule antagonist of chemokine receptors CCR1 and CCR3. Potent inhibition of eosinophil function and CCR3-mediated HIV-1 entry. J Biol Chem, 275 (34): 25985-92. [PMID:10854442]
94. Samson M, Labbe O, Mollereau C, Vassart G, Parmentier M. (1996) Molecular cloning and functional expression of a new human CC-chemokine receptor gene. Biochemistry, 35 (11): 3362-7. [PMID:8639485]
95. Samson M, Stordeur P, Labbé O, Soularue P, Vassart G, Parmentier M. (1996) Molecular cloning and chromosomal mapping of a novel human gene, ChemR1, expressed in T lymphocytes and polymorphonuclear cells and encoding a putative chemokine receptor. Eur J Immunol, 26 (12): 3021-8. [PMID:8977299]
96. Sarau HM, Rush JA, Foley JJ, Brawner ME, Schmidt DB, White JR, Barnette MS. (1997) Characterization of functional chemokine receptors (CCR1 and CCR2) on EoL-3 cells: a model system to examine the role of chemokines in cell function. J Pharmacol Exp Ther, 283 (1): 411-8. [PMID:9336350]
97. Schweickart VL, Raport CJ, Godiska R, Byers MG, Eddy Jr RL, Shows TB, Gray PW. (1994) Cloning of human and mouse EBI1, a lymphoid-specific G-protein-coupled receptor encoded on human chromosome 17q12-q21.2. Genomics, 23 (3): 643-50. [PMID:7851893]
98. Shitara K, Nakamura K, Hosaka E, Tanaka A, Koike M. (2009) Monoclonal antibodies which preferentially bind to chemokine receptors, used for immunotherapy, as antiinflammatory, aniticarcinogenic agents and for prophylaxis of respiratory system disorders or antiallergens. Patent number: US7504104. Assignee: Kyowa Hakko Kogyo Co., Ltd. Priority date: 31/08/2001. Publication date: 17/01/2010.
99. Skerlj RT, Bridger GJ, Kaller A, McEachern EJ, Crawford JB, Zhou Y, Atsma B, Langille J, Nan S, Veale D et al.. (2010) Discovery of novel small molecule orally bioavailable C-X-C chemokine receptor 4 antagonists that are potent inhibitors of T-tropic (X4) HIV-1 replication. J Med Chem, 53 (8): 3376-88. [PMID:20297846]
100. Southern C, Cook JM, Neetoo-Isseljee Z, Taylor DL, Kettleborough CA, Merritt A, Bassoni DL, Raab WJ, Quinn E, Wehrman TS et al.. (2013) Screening β-Arrestin Recruitment for the Identification of Natural Ligands for Orphan G-Protein-Coupled Receptors. J Biomol Screen, 18 (5): 599-609. [PMID:23396314]
101. Strizki JM, Tremblay C, Xu S, Wojcik L, Wagner N, Gonsiorek W, Hipkin RW, Chou CC, Pugliese-Sivo C, Xiao Y et al.. (2005) Discovery and characterization of vicriviroc (SCH 417690), a CCR5 antagonist with potent activity against human immunodeficiency virus type 1. Antimicrob Agents Chemother, 49 (12): 4911-9. [PMID:16304152]
102. Szpakowska M, Meyrath M, Reynders N, Counson M, Hanson J, Steyaert J, Chevigné A. (2018) Mutational analysis of the extracellular disulphide bridges of the atypical chemokine receptor ACKR3/CXCR7 uncovers multiple binding and activation modes for its chemokine and endogenous non-chemokine agonists. Biochem Pharmacol, 153: 299-309. [PMID:29530506]
103. Tamamura H, Xu Y, Hattori T, Zhang X, Arakaki R, Kanbara K, Omagari A, Otaka A, Ibuka T, Yamamoto N et al.. (1998) A low-molecular-weight inhibitor against the chemokine receptor CXCR4: a strong anti-HIV peptide T140. Biochem Biophys Res Commun, 253 (3): 877-82. [PMID:9918823]
104. Uguccioni M, Mackay CR, Ochensberger B, Loetscher P, Rhis S, LaRosa GJ, Rao P, Ponath PD, Baggiolini M, Dahinden CA. (1997) High expression of the chemokine receptor CCR3 in human blood basophils. Role in activation by eotaxin, MCP-4, and other chemokines. J Clin Invest, 100 (5): 1137-43. [PMID:9276730]
105. Wacker DA, Santella 3rd JB, Gardner DS, Varnes JG, Estrella M, DeLucca GV, Ko SS, Tanabe K, Watson PS, Welch PK et al.. (2002) CCR3 antagonists: a potential new therapy for the treatment of asthma. Discovery and structure-activity relationships. Bioorg Med Chem Lett, 12 (13): 1785-9. [PMID:12067561]
106. Walters MJ, Wang Y, Lai N, Baumgart T, Zhao BN, Dairaghi DJ, Bekker P, Ertl LS, Penfold ME, Jaen JC et al.. (2010) Characterization of CCX282-B, an orally bioavailable antagonist of the CCR9 chemokine receptor, for treatment of inflammatory bowel disease. J Pharmacol Exp Ther, 335 (1): 61-9. [PMID:20660125]
107. Wan Y, Jakway JP, Qiu H, Shah H, Garlisi CG, Tian F, Ting P, Hesk D, Egan RW, Billah MM et al.. (2002) Identification of full, partial and inverse CC chemokine receptor 3 agonists using [35S]GTPgammaS binding. Eur J Pharmacol, 456 (1-3): 1-10. [PMID:12450563]
108. Wang W, Soto H, Oldham ER, Buchanan ME, Homey B, Catron D, Jenkins N, Copeland NG, Gilbert DJ, Nguyen N et al.. (2000) Identification of a novel chemokine (CCL28), which binds CCR10 (GPR2). J Biol Chem, 275 (29): 22313-23. [PMID:10781587]
109. Watts AO, Verkaar F, van der Lee MM, Timmerman CA, Kuijer M, van Offenbeek J, van Lith LH, Smit MJ, Leurs R, Zaman GJ et al.. (2013) β-Arrestin recruitment and G protein signaling by the atypical human chemokine decoy receptor CCX-CKR. J Biol Chem, 288 (10): 7169-81. [PMID:23341447]
110. Weng Y, Siciliano SJ, Waldburger KE, Sirotina-Meisher A, Staruch MJ, Daugherty BL, Gould SL, Springer MS, DeMartino JA. (1998) Binding and functional properties of recombinant and endogenous CXCR3 chemokine receptors. J Biol Chem, 273 (29): 18288-91. [PMID:9660793]
111. White JR, Lee JM, Young PR, Hertzberg RP, Jurewicz AJ, Chaikin MA, Widdowson K, Foley JJ, Martin LD, Griswold DE et al.. (1998) Identification of a potent, selective non-peptide CXCR2 antagonist that inhibits interleukin-8-induced neutrophil migration. J Biol Chem, 273 (17): 10095-8. [PMID:9553055]
112. Wilbanks A, Zondlo SC, Murphy K, Mak S, Soler D, Langdon P, Andrew DP, Wu L, Briskin M. (2001) Expression cloning of the STRL33/BONZO/TYMSTRligand reveals elements of CC, CXC, and CX3C chemokines. J Immunol, 166 (8): 5145-54. [PMID:11290797]
113. Wilson S, Wilkinson G, Milligan G. (2005) The CXCR1 and CXCR2 receptors form constitutive homo- and heterodimers selectively and with equal apparent affinities. J Biol Chem, 280 (31): 28663-74. [PMID:15946947]
114. Wong ML, Xin WW, Duman RS. (1996) Rat LCR1: cloning and cellular distribution of a putative chemokine receptor in brain. Mol Psychiatry, 1 (2): 133-40. [PMID:9118323]
115. Wu L, Ruffing N, Shi X, Newman W, Soler D, Mackay CR, Qin S. (1996) Discrete steps in binding and signaling of interleukin-8 with its receptor. J Biol Chem, 271 (49): 31202-9. [PMID:8940121]
116. Wuyts A, Proost P, Lenaerts JP, Ben-Baruch A, Van Damme J, Wang JM. (1998) Differential usage of the CXC chemokine receptors 1 and 2 by interleukin-8, granulocyte chemotactic protein-2 and epithelial-cell-derived neutrophil attractant-78. Eur J Biochem, 255 (1): 67-73. [PMID:9692902]
117. Yang D, Chertov O, Bykovskaia SN, Chen Q, Buffo MJ, Shogan J, Anderson M, Schröder JM, Wang JM, Howard OM et al.. (1999) Beta-defensins: linking innate and adaptive immunity through dendritic and T cell CCR6. Science, 286 (5439): 525-8. [PMID:10521347]
118. Yokoyama K, Ishikawa N, Igarashi S, Kawano N, Masuda N, Hamaguchi W, Yamasaki S, Koganemaru Y, Hattori K, Miyazaki T et al.. (2009) Potent and orally bioavailable CCR4 antagonists: Synthesis and structure-activity relationship study of 2-aminoquinazolines. Bioorg Med Chem, 17 (1): 64-73. [PMID:19081254]
119. Yoshida R, Imai T, Hieshima K, Kusuda J, Baba M, Kitaura M, Nishimura M, Kakizaki M, Nomiyama H, Yoshie O. (1997) Molecular cloning of a novel human CC chemokine EBI1-ligand chemokine that is a specific functional ligand for EBI1, CCR7. J Biol Chem, 272 (21): 13803-9. [PMID:9153236]
120. Yoshida R, Nagira M, Kitaura M, Imagawa N, Imai T, Yoshie O. (1998) Secondary lymphoid-tissue chemokine is a functional ligand for the CC chemokine receptor CCR7. J Biol Chem, 273: 7118-7122. [PMID:9507024]
121. Yoshida T, Imai T, Kakizaki M, Nishimura M, Takagi S, Yoshie O. (1998) Identification of single C motif-1/lymphotactin receptor XCR1. J Biol Chem, 273 (26): 16551-4. [PMID:9632725]
122. Zaballos A, Gutiérrez J, Varona R, Ardavín C, Márquez G. (1999) Cutting edge: identification of the orphan chemokine receptor GPR-9-6 as CCR9, the receptor for the chemokine TECK. J Immunol, 162 (10): 5671-5. [PMID:10229797]
123. Zaballos A, Varona R, Gutierrez J, Lind P, Marquez G. (1996) Molecular cloning and RNA expression of two new human chemokine receptor-like genes. Biochem Biophys Res Commun, 227: 846-853. [PMID:8886020]
124. Zhang WB, Navenot JM, Haribabu B, Tamamura H, Hiramatu K, Omagari A, Pei G, Manfredi JP, Fujii N, Broach JR, Peiper SC. (2002) A point mutation that confers constitutive activity to CXCR4 reveals that T140 is an inverse agonist and that AMD3100 and ALX40-4C are weak partial agonists. J Biol Chem, 277: 24515-24521. [PMID:11923301]
125. Zlotnik A, Yoshie O. (2000) Chemokines: a new classification system and their role in immunity. Immunity, 12 (2): 121-7. [PMID:10714678]
126. Zoffmann S, Turcatti G, Galzi J, Dahl M, Chollet A. (2001) Synthesis and characterization of fluorescent and photoactivatable MIP-1alpha ligands and interactions with chemokine receptors CCR1 and CCR5. J Med Chem, 44 (2): 215-22. [PMID:11170631]
Subcommittee members:
Francoise Bachelerie
Adit Ben-Baruch
Christophe Combadiere
Joshua M. Farber
Gerard J. Graham
Richard Horuk
Massimo Locati
Andrew D. Luster
Alberto Mantovani
Philip M. Murphy (Chairperson)
Robert J. B. Nibbs
Hisayuki Nomiyama
Christine A. Power
Amanda E. I. Proudfoot
Mette M. Rosenkilde
Antal Rot
Silvano Sozzani
Marcus Thelen
Osamu Yoshie
Albert Zlotnik
Amanda M. Burkhardt
Alexander H. Sparre-Ulrich |
Other contributors:
Israel F. Charo
Reinhold Förster
Rebecca Hills
Kouji Matsushima
Amy E. Monaghan
Georgios L. Moschovakis
Joost J. Oppenheim
Mohib Uddin |
Database page citation (select format):
Concise Guide to PHARMACOLOGY citation:
Alexander SPH, Christopoulos A, Davenport AP, Kelly E, Mathie AA, Peters JA, Veale EL, Armstrong JF, Faccenda E, Harding SD, Davies JA et al. (2023) The Concise Guide to PHARMACOLOGY 2023/24: G protein-coupled receptors. Br J Pharmacol. 180 Suppl 2:S23-S144.
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Specific chemokine receptors facilitate cell entry by microbes, such as ACKR1 for Plasmodium vivax, and CCR5 and CXCR4 for HIV-1. Virally encoded chemokine receptors are known (e.g. US28, a homologue of CCR1 from human cytomegalovirus and ORF74, which encodes a homolog of CXCR2 in Herpesvirus saimiri and gamma-Herpesvirus-68), but their role in viral life cycles is not established. Viruses can exploit or subvert the chemokine system by producing chemokine antagonists and scavengers. Three chemokine receptor antagonists have now been approved by the FDA: 1) the CCR5 antagonist maraviroc (Pfizer) for treatment of HIV/AIDS in patients with CCR5-using strains; and 2) the CXCR4 antagonist plerixafor (Sanofi) for hematopoietic stem cell mobilization with G-CSF (CSF3, P09919) in patients undergoing transplantation in the context of chemotherapy for Hodgkins' Disease and multiple myeloma; and 3) the CCR4 blocking antibody Poteligeo (mogamulizumab-kpkc, Kyowa Kirin, Inc.) for mycosis fungoides or Sezary syndrome.