Table 3

Chemokine receptors: nomenclature, pharmacology and biology

NomenclatureAccession NumberPharmacologyBiology
NamePrevious NamesGene ChromosomeHumanMouseSelective ChemokinesSelective Nonpeptide Small Molecule Antagonists (Kd)Major Phenotypes of Genetically Deficient Mice/HumansHIV Coreceptor Activity?
CXC chemokine receptors
 CXCR1IL8RA, IL-8R-I, IL-8Rα IL8RA 2q34-q35 P25024 N.D.NoneNoneN.A.N.D.
 CXCR2IL8RB, IL-8R-II, IL-8Rβ IL8RB 2q34-q35 P25025 P35343 GROα, NAP-2, ENA-78SKB RS-145004-000 (35 nM)Mice:Defective neutrophil trafficking and distribution and B cell distribution; resistance to atherogenesisN.D.
 CXCR3IP10/Mig R, GPR9 GPR9 Xq13 P49682 AF045146 IP-10, I-TAC, MigNoneN.A.N.D.
 CXCR4HUMSTSR, LESTR, fusin, HM89, LCR1, NPYR, D2S201E CXCR4 2pter-qter P30991 P70658 SDF-1AMD3100Mice:Defective development of heart, cerebellum, stomach vasculature, B cell lymphopoiesis and bone marrow myelopoiesisEmbryonic lethal X4 strains
 CXCR5BLR-1, MDR15 BLR1 11 P32302 Q04683 BCA-1NoneMice:Defective B cell trafficking and development of inguinal nodes, Peyer's patches and germinal centersHIV-2
CC chemokine receptors
 CCR1CKR1, CC CKR1, MIP-1α/RANTES, CMKBR1 CCR1 3p21 P32246 P51675 HCC-1Berlex RS-162993-000 (6 nM)Mice: Susceptibility to A. fumigatus; resistance to pancreatitis-induced alveolitis; defective neutrophil chemotaxis, Th1/Th2 balance, hematopoiesis, and granuloma formation: susceptibility to nephrotoxic nephritis; resistance to acute and chronic cardiac allograft rejectionN.D.
 CCR2CKR2, CC CK2, CC CKR2, MCP-1, CMKBR2 CCR2 3p21 P41597 P51683 MCP-1Roche RS-511336-000 (33 nM)Mice: Susceptibility to Listeria;resistance to atherogenesis; defective monocyte trafficking, Th1/Th2 balance, and granuloma formationSome dual-tropic strains
 CCR3CKR3, CC CKR3, eotaxin receptor, CMKBR3 CCR3 3p21 P51677 P51678 Eotaxin, eotaxin-2Banyu RS-163883-230 (40 nM)N.A.Some X4, R5, and dual-tropic strains
 CCR4CKR4, CC CKR4, K5-5, CMKBR4, CHEMR1 CCR4 3p22 P51679 P51680 TARC, MDCNoneN.A.N.D.
 CCR5CKR5, CC CKR5, ChemR13, CMKBR5 CCR5 3p21 P51681 P51682 MIP-1βTakeda TAK-779 (1 nM)Mice: Susceptibility to Listeria, lps, and DTH reaction. Human: Resistance to HIVAll R5 and dual-tropic strains
 CCR6GPR-CY4, CKR-L3, STRL22, DRY-6, DCR2, BN-1, GPR29, CMKBR6 CCR6 6q27 P51684 AJ222714 LARCNoneN.A.N.D.
 CCR7EBI-1, BLR-2, CMKBR7 CCR7 17q12-q21.2 P32248 P47774 ELC, SLCNoneN.A.N.D.
 CCR8TER1, CKR-L1, GPR-CY6, ChemR1, CMKBR8 CCR8 3p22-p23 P51685 AF001277 I-309NoneN.A.Some X4, R5, and dual-tropic strains
 CCR9GPR 9-6Unnamed 3p21.3-22 P51686 AJ132336 TECKNoneN.A.N.D.
 CCR10GPR2 GPR2 17q21.1-q21.3 U13667 ESkineNoneN.A.
 CCR11PPR13p22 AF193507 N.A.TBA
C chemokine receptor
 XCR1GPR5 GPR5 3p21 P46094 N.A.LymphotactinNoneN.A.N.D.
CX3C chemokine receptor
 CX3CR1GPR13; V28; CMKBRL1 CX3CR1 3pter-p21 P49238 AF102269 FractalkineNoneN.A.Some X4, R5, and dual-tropic strains
Chemokine-binding proteins
 DuffyDARC; glycoprotein D Fy 1q21-q22 Q16570 AF016584 NoneYesHuman:Resistance to P. vivax malariaN.D.
 D6CCR9, CCR10 CMKBR9 3p21 Y12815 Y12879 NoneN.A.N.A.N.D.

N.D., not determined; N.A., not available. Two splice variants affecting the ORF have been identified for each of the following receptors: CXCR4, CXCR5, CCR2, and CCR9; however, biological or pharmacological significance has not been determined. Other HIV coreceptors include US28 (Pleskoff et al., 1997), the leukotriene B4 receptor (Owman et al., 1998), and the orphans Apj (Choe et al., 1998), BOB/GPR15 (Deng et al., 1997; Farzan et al., 1997), STRL33/Bonzo/TYMSTR (Deng et al., 1997; Liao et al., 1997; Loetscher et al., 1997), GPR1 (Farzan et al., 1997), ROC1 (Shimizu et al., 2000); and ChemR23 (Samson et al., 1998).