Supplemental Material can be found at: /content/suppl/2014/09/18/66.1.1.DC1.html 1521-0081/66/1/1–79$25.00 http://dx.doi.org/10.1124/pr.113.007724 PHARMACOLOGICAL REVIEWS Pharmacol Rev 66:1–79, January 2014 U.S. Government work not protected by U.S. copyright ASSOCIATE EDITOR: ELLIOT H. OHLSTEIN International Union of Basic and Clinical Pharmacology. LXXXIX. Update on the Extended Family of Chemokine Receptors and Introducing a New Nomenclature for Atypical Chemokine Receptors Francoise Bachelerie,1 Adit Ben-Baruch, Amanda M. Burkhardt, Christophe Combadiere, Joshua M. Farber, Gerard J. Graham,1 Richard Horuk, Alexander Hovard Sparre-Ulrich, Massimo Locati,1 Andrew D. Luster, Alberto Mantovani,1 Kouji Matsushima, Philip M. Murphy,1 Robert Nibbs,1 Hisayuki Nomiyama, Christine A. Power, Amanda E. I. Proudfoot, Mette M. Rosenkilde, Antal Rot,1 Silvano Sozzani,1 Marcus Thelen,1 Osamu Yoshie, and Albert Zlotnik INSERM UMR_S996, Laboratory of Excellence in Research on Medication and Innovative Therapeutics (LERMIT), Université Paris-Sud, Clamart, France (F.B.); Department of Cell Research and Immunology, George S. Wise Faculty of Life Sciences, Tel Aviv University, Tel Aviv, Israel (A.B.-B.); Department of Physiology and Biophysics, University of California Irvine, Irvine, California (A.M.B., A.Z.); INSERM UMR-S 945, Laboratoire d’Immunologie Cellulaire, Faculte de Medicine Pitie-Salpetriere, Paris, France (C.C.); Laboratory of Molecular Immunology, National Institute of Allergy and Infectious Diseases, National Institutes of Health, Bethesda, Maryland (J.M.F., P.M.M.); Institute of Infection, Immunity and Inflammation, College of Medical, Veterinary and Life Sciences, University of Glasgow, Glasgow Biomedical Research Centre, Glasgow, United Kingdom (G.J.G., R.N.); Department of Pharmacology, University of California at Downloaded from Davis, Davis, California (R.H.); Laboratory for Molecular Pharmacology, Department of Neuroscience and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, Copenhagen, Denmark (A.H.S.-U., M.M.R.); University of Milan, Milan, Italy, and Humanitas Clinical and Research Institute, Rozzano, Italy (M.L., A.M.); Center for Immunology and Inflammatory Diseases, Division of Rheumatology, Allergy and Immunology, Massachusetts General Hospital, Harvard Medical School, Boston, Massachusetts (A.D.L.); Department of Molecular Preventive Medicine, School of Medicine, University of Tokyo, Tokyo, Japan (K.M.); Department of Molecular Enzymology, Kumamoto University Graduate School of Medical Sciences, Kumamoto, Japan (H.N.); Geneva Research Centre, Merck Serono S. A., Geneva, Switzerland (C.A.P.); NovImmune SA, Geneva, Switzerland (A.E.I.P.); Medical Research Council Centre for Immune by guest on September 29, 2021 Regulation, Institute of Biomedical Research, School of Infection and Immunity, University of Birmingham, Birmingham, United Kingdom (A.R.); Department of Molecular and Translational Medicine, University of Brescia, Brescia, and Humanitas Clinical and Research Center, Rozzano, Italy (S.S.); Institute for Research in Biomedicine, Bellinzona, Switzerland (M.T.); and Department of Microbiology, Kinki University Faculty of Medicine, Osaka, Japan (O.Y.) Abstract. ..................................................................................... 3 I. Introduction. ............................................................................... 3 II. Host G Protein-Coupled Chemokine Receptors ................................................ 4 A. CXC Chemokine Receptors. ............................................................. 4 1. CXCR1 and CXCR2 .................................................................. 4 Drug development ...................................................................10 2. CXCR3 ..............................................................................12 Drug development ...................................................................15 3. CXCR4 ..............................................................................15 Drug development. ...................................................................20 4. CXCR5 ..............................................................................21 Drug development. ...................................................................21 5. CXCR6 ..............................................................................22 Drug development. ...................................................................23 6. CXCR7 (now ACKR3, see Section III.A.3) . ...........................................23 B. CC Chemokine Receptors .................................................................23 1. CCR1................................................................................23 Drug development ...................................................................24 This work was supported by the Intramural Research Program of the National Institutes of Health [National Institute of Allergy and Infectious Diseases]. Address correspondence to: Dr. Philip M. Murphy, Chair, Subcommittee on Chemokine Receptors, Nomenclature Committee- International Union of Pharmacology, Bldg. 10, Room 11N113, NIH, Bethesda, MD 20892. E-mail: [email protected] 1Members of the Subcommittee on Atypical Chemokine Receptor Nomenclature. Authors are listed alphabetically. dx.doi.org/10.1124/pr.113.007724 1 An erratum has been published: /content/66/2/467.full.pdf 2 Bachelerie et al. 2. CCR2................................................................................24 Drug development ...................................................................27 3. CCR3................................................................................29 Drug development ...................................................................30 4. CCR4................................................................................31 Drug development. ...................................................................32 5. CCR5................................................................................32 Drug development ...................................................................34 6. CCR6................................................................................36 Drug development. ...................................................................37 7. CCR7................................................................................37 Drug development. ...................................................................38 8. CCR8................................................................................38 Drug development. ...................................................................39 9. CCR9................................................................................40 Drug development. ...................................................................41 10. CCR10...............................................................................41 Drug development. ...................................................................42 C. CX3C Chemokine Receptors . .............................................................42 1. CX3CR1.............................................................................42 Drug development. ...................................................................44 D. XC Chemokine Receptors .................................................................44 1. XCR1 . ...............................................................................44 Drug development. ...................................................................46 III. Host Atypical Chemokine Receptors . .......................................................46 A. ACKR1 (Previously Duffy Antigen Receptor for Chemokines) ..............................46 Drug Development .......................................................................47 B. ACKR2 (Formerly D6 or CCBP2). .......................................................47 Drug Development .......................................................................49 C. ACKR3 (Alias CXCR7). ...................................................................49 Drug Development .......................................................................51 D. ACKR4 (Formerly CCRL1 and CCX CKR).................................................51 Drug Development .......................................................................51 E. CCRL2 (ACKR5, Reserved) . .............................................................51 Drug Development .......................................................................52 F. PITPNM3 (Also Known as the CCL18/PARC Receptor; New Name: ACKR6, Reserved) . 52 Drug Development .......................................................................52 G. C5L2 .....................................................................................52 Drug Development .......................................................................53 IV. Microbial Chemokine Receptors and Chemokine-Binding Proteins . ..........................53 A. Virus-Encoded Chemokine Receptors and Chemokine-Binding Proteins ....................53 1. US28 from Human Cytomegalovirus . .................................................53 2. U12 and U51 from HHV6 ............................................................54 ABBREVIATIONS: 7TM, 7-transmembrane; aa, amino acid; ACKR, atypical chemokine receptor; AMD, age-related macular degeneration; APCs, antigen presenting cells; ATL, adult T-cell leukemia/lymphoma; BM, bone marrow; BMS, Bristol-Myers