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CC Chemokine Receptor-1 (CCR1) Antagonist

No.190(August 2022)
B6060
BX 471 (1)

CC Chemokine Receptor-1 (CCR1) Antagonist

BX 471 (1) is a non-peptide CC chemokine receptor-1 (CCR1) antagonist.1) 1 is able to displace the CCR1 ligands as shown in Table 1. 1 has also greatly higher selectivity for CCR1 than 28 other G-protein-coupled receptors on Ki basis (>10000 fold).1)
He et al. showed that 1 attenuates systemic inflammatory response during sepsis.2) Blocking CCR1 by 1 downregulated ICAM-1, P-selectin, and E-selectin expression at mRNA and protein levels. On the other hand, Lebre et al. reported that 1 blocked CCL5/RANTES-induced migration of rheumatoid arthritis monocytes isolated from the patients.3) Furthermore, Anders et al. showed that 1 blocks macrophage and T-cell recruitment to the renal interstitium of autoimmune mice (MRLlpr/lpr).4)

Competition of 1 with CCR1 ligands

References

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