title: Selective binding of the truncated form of the chemokine CKbeta8 (25-99) to CC chemokine receptor 1(CCR1).
abstract: Human CC chemokine receptor 1 (CCR1) has been proposed as a receptor for CKbeta8. To obtain conclusive evidence, binding-displacement studies of 125I-CKbeta8 (25-99) were performed on membranes of Chinese hamster ovary cells expressing human CCR1. The Ic50 for displacement of 125I-CKbeta8 (25-99) with CKbeta8 (25-99) was 0.22 nM. The longer forms of CKbeta8 (24-99 and 1-99) also displaced 125I-CKbeta8, with Ic50 values of 6.5 and 16 nM, respectively. Displacement profiles of 125I-CKbeta8 (25-99) on freshly prepared human monocytes indicated that CCR1 was the major receptor for CKbeta8. We conclude that CCR1 is a receptor for different-length CKbeta8 and that CKbeta8 (25-99) has a similar affinity for CCR1 as macrophage inflammatory protein-1alpha (MIP-1alpha). The longer variants of CKbeta8 are significantly less potent than CKbeta8 (25-99) and MIP-1a on CCR1 and monocytes (P < 0.05).
authors.affiliation: Vascular Biology, SmithKline Beecham Pharmaceuticals, Harlow, UK. Theo_Berkhout-1@sbphrd.com
authors.forename: T A
authors.initials: TA
authors.lastname: Berkhout
authors.forename: J
authors.initials: J
authors.lastname: Gohil
authors.forename: P
authors.initials: P
authors.lastname: Gonzalez
authors.forename: C L
authors.initials: CL
authors.lastname: Nicols
authors.forename: K E
authors.initials: KE
authors.lastname: Moores
authors.forename: C H
authors.initials: CH
authors.lastname: Macphee
authors.forename: J R
authors.initials: JR
authors.lastname: White
authors.forename: P H
authors.initials: PH
authors.lastname: Groot
mesh_terms: D000818:Animals; D001667:Binding, Competitive; D016466:CHO Cells; D019742:Chemokines, CC / Q000378:metabolism*; D006224:Cricetinae; D006801:Humans; D007457:Iodine Radioisotopes; D009000:Monocytes / Q000378:metabolism; D010455:Peptides / Q000378:metabolism; D054389:Receptors, CCR1; D019707:Receptors, Chemokine / Q000378:metabolism*; D014162:Transfection
chemical_list: C105504:CCL23 protein, human; C515300:CCR1 protein, human; D019742:Chemokines, CC; D007457:Iodine Radioisotopes; D010455:Peptides; D054389:Receptors, CCR1; D019707:Receptors, Chemokine