Fig. 2.

Mode of binding of 747 with CCR2.

(A) Sequence alignment of CCR2 and CCR5, the transmembrane regions, intracellular and extracellular loops are marked. From the docking results, 747 bonds with CCR2 residues are marked in red. (B) Schematic diagram of CCR2, CCR5, and the chimeric receptors CCR2-CCR5 (C-term), CCR5-CCR2 (C-term), and CCR5-CCR2 (Extracellular loops). (C) Inhibitory effect of 747 on binding of ¹²⁵I-MCP-1 for CCR2, CCR5, and chimeric receptors expressed in CHO-K1 cells. (D) Inhibitory effect of 747 on binding of ¹²⁵I-MIP-1α for CCR2, CCR5, and chimeric receptors expressed in CHO-K1 cells. (E) Induced-fit docking of 747 in a homology model of CCR2 based on the C-X-C chemokine receptor-4 crystal structure. (F) Inhibitory effect of 747 on binding of ¹²⁵I-MIP-1α for CCR2 wild type and mutant receptors expressed in CHO-K1 cells. (For interpretation of the references to colour in this figure legend, the reader is referred to the web version of this article.)