Selective binding of the truncated form of the chemokine CKβ8 (25-99) to CC chemokine receptor 1 (CCR1)
Nicols, Charlotte L.
Moores, Kitty E.
MacPhee, Colin H.
White, John R.
Groot, Pieter H. E.
Human CC chemokine receptor 1 (CCR1) has been proposed as a receptor for CKβ8. To obtain conclusive evidence, binding-displacement studies of 125I-CKβ8 (25-99) were performed on membranes of Chinese hamster ovary cells expressing human CCR1. The IC50 for displacement of 125I-CKβ8 (25-99) with CKβ8 (25-99) was 0.22 nM. The longer forms of CKβ8 (24-99 and 1-99) also displaced 125I-CKβ8, with IC50 values of 6.5 and 16 nM, respectively. Displacement profiles of 125I-CKβ8 (25-99) on freshly prepared human monocytes indicated that CCR1 was the major receptor for CKβ8. We conclude that CCR1 is a receptor for different-length CKβ8 and that CKβ8 (25-99) has a similar affinity for CCR1 as macrophage inflammatory protein-1α (MIP-1α). The longer variants of CKβ8 are significantly less potent than CKβ8 (25-99) and MIP-1α on CCR1 and monocytes (P < 0.05). Copyright (C) 2000 Elsevier Science Inc.
Published inBiochemical Pharmacology
RelationsSchool of Life and Medical Sciences
MetadataShow full item record
Showing items related by title, author, creator and subject.
Fractalkine is expressed by smooth muscle cells in response to IFN-gamma and TNF-alpha and is modulated by metalloproteinase activity Ludwig, A.; Berkhout, Theo; Moores, K.; Groot, P.; Chapman, G. (2002-01-15)Fractalkine/CX3C-chemokine ligand 1 is expressed as a membrane-spanning adhesion molecule that can be cleaved from the cell surface to produce a soluble chemoattractant. Within the vasculature, fractalkine is known to be ...
School of Life and Medical Sciences; Department of Pharmacy; Health & Human Sciences Research Institute; Medicinal and Analytical Chemistry; Berkhout, Theo; Moores, Kitty E.; MacPhee, Colin H. (1999)The ligand PF-4 has been identified as a ligand for the 7TM receptor HBMBU14, also known as TYMSTR, STRL-33 and BONZO.
CCR2: Characterization of the antagonist binding site from a combined receptor modeling/mutagenesis approach Berkhout, Theo; Blaney, F.E.; Bridges, A.M.; Cooper, D.G.; Forbes, I.T.; Gribble, A.D.; Groot, P.H.E.; Hardy, A.; Ife, R.J.; Kaur, R.; Moores, K.E.; Shillito, H.; Willetts, J.; Witherington, J. (2003-09-11)We describe here a classical molecular modeling exercise that was carried out to provide a basis for the design of novel antagonist ligands of the CCR2 receptor. Using a theoretical model of the CCR2 receptor, docking ...