HTS005M - ChemiSCREEN™ CCR1 Chemokine Receptor Membrane Preparation

CCR1 is a GPCR that binds to a variety of CC ligands, including MIP-1a, RANTES, MCP-3, HCC-1, HCC-2, HCC-4, and MPIF-1 (Olson and Ley, 2002). Lymphocytes, macrophages, dendritic cells, and GM-CSF-activated neutrophils express CCR1 (Kaufmann et al., 2001; Cheng et al., 2001). Two selective, non-peptide small molecule antagonists of CCR1, BX-471 and CP-481,715 have been synthesized (Gladue et al., 2003; Liang et al., 2000). Pharmacological and genetic targeting of CCR1, either alone or in combination with cyclosporin A, reduces cardiac and renal allograft rejection (Gao et al., 2000; Horuk et al., 2001a; Horuk et al., 2001b), allergic encephalomyelitis (Liang et al., 2000), and renal fibrosis (Anders et al., 2002) in experimental models. CCR1 Membrane Preparations are ideal for screening molecules that disrupt interactions between CCR1 and its ligands. The CCR1 Membrane Preps bind to MIP-1a with a Kd of 1.8 nM, and yield greater than a 10-fold signal-to-background ratio with [125I]-MIP-1a at a concentration of 0.1 nM.

Additional Resource :  HTS005M090314 Datasheet