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. 2013 Dec 17;170(8):1459–1581. doi: 10.1111/bph.12445
Nomenclature CCR1 CCR2 CCR3 CCR4 CCR5
HGNC, UniProt CCR1, P32246 CCR2, P41597 CCR3, P51677 CCR4, P51679 CCR5, P51681
Principal transduction Gi/o Gi/o Gi/o Gi/o Gi/o
Endogenous agonists (pKi) CCL13, CCL8, CCL3 (7.8 – 10.2) 571,572,588,630, CCL23 (Selective) (8.9) 571, CCL7 (8.1) 571,583, CCL5 (6.8 – 8.2) 572,588, CCL14 (7.4) 571, CCL15 (Selective) (pIC50 7.9) 573 CCL16, CCL2 (pIC50 9.3 – 10.2) 573,595,598,605,615, CCL13 (pIC50 8.6 – 8.7) 595,615, CCL7 (pIC50 8.4 – 8.7) 573,595,615, CCL11 (Partial agonist) (pIC50 7.1 – 7.7) 595,605 CCL28, CCL8, CCL7 (8.6 – 9.2) 575, CCL13 (pIC50 8.7 – 10.3) 599,615, CCL11 (Selective) (pIC50 8.7 – 9.0) 577,591,599,610,615, CCL24 (Selective) (pIC50 8.0 – 9.4) 599,605, CCL15 (pIC50 8.6) 573, CCL26 (Selective) (pIC50 7.9 – 8.9) 591,599,605 CCL22 (Selective) (pIC50 9.2) 589, CCL17 (Selective) (pIC50 8.7) 589 CCL16, CCL4 (Selective) (9.4 – 9.6) 602,609, CCL5 (9.2 – 9.7) 566,602,609, CCL8 (9.3) 609, CCL3 (8.0 – 8.9) 602,609,630, CCL2 (7.5) 602, CCL14 (7.2) 602, CCL11 (pIC50 7.7) 570
Selective agonists (pKi) – – CCL11 {Sp: Mouse} (9.5 – 10.0) 575 – R5-HIV-1 gp120
Non-selective agonists (pKi) – – – vMIP-III –
Endogenous antagonists (pKi) CCL4 (Selective) (7.1 – 7.8) 571,572 CCL26 (Selective) (pIC50 8.5) 605 CXCL10 (Selective), CXCL11 (CXCL11, O14625) (Selective), CXCL9 (Selective) – CCL7 (Selective) (7.5) 602
Selective antagonists (pKi) CP-481,715 (pKd 8.0) 579, BX 471 (8.2 – 9.0) 593, 2b-1 (pIC50 8.7) 603, UCB35625 (pIC50 8.0) 610 GSK Compound 34 (7.6) banyu (I) (Inverse agonist) (8.5) 617, SB328437 (8.4), BMS compound 87b (8.1) 616 – MRK-1, vicriviroc (9.1) 613, aplaviroc (8.5) 596, ancriviroc (7.8 – 8.7) 596,604,613, TAK-779 (7.5) 596, E913 (pIC50 8.7) 597, maraviroc (pIC50 8.1) 602
Radioligands (Kd) [125I]CCL7 (human) (Agonist, Full agonist) (7x10-10 M) 568, [125I]CCL3 (human) (Agonist, Full agonist) (1.58x10-9 – 1x10-8 M) 568,580,611, [125I]CCL5 (human) (Agonist, Full agonist) (7x10-9 M) 611 [125I]CCL2 (Agonist, Full agonist), [125I]CCL7 (human) (Agonist) [125I]CCL5 (human) (Agonist), [125I]CCL7 (human) (Agonist), [125I]CCL11 (human) (Antagonist) (5.01x10-9 M) 617 [125I]CCL17 (Agonist, Full agonist), [125I]CCL27 (Agonist) [125I]CCL3 (human) (Agonist), [125I]CCL5 (human) (Agonist), [125I]CCL8 (human) (Agonist), [125I]CCL4 (human) (Agonist, Full agonist) (2.51x10-10 M) 602
Comment – – – Monoclonal antibody mogamulizumab selectively blocks CCR4 –