Identifying bias in CCR1 antagonists using radiolabelled binding, receptor internalization, β-arrestin translocation and chemotaxis assays
Background and purpose: Investigators have suggested that the chemokine receptor CCR1 plays a role in multiple myeloma. Studies using antisense and neutralizing antibodies to CCR1 showed that down-regulation of the receptor altered disease progression in a mouse model. More recently, experiments utilizing scid mice injected with human myeloma cells demonstrated that the CCR1 antagonist BX471 reduced osteolytic lesions, while the CCR1 antagonist MLN-3897 prevented myeloma cell adhesion to osteoclasts. However, information is limited regarding the pharmacology of CCR1 antagonists in myeloma cells.
British Journal of Pharmacology
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Gilchrist, A.; Gauntner, T. D.; Fazzini, A.; Alley, K. M.; Pyen, D. S.; Ahn, J.; Ha, S. J.; Willett, A.; Sansom, S. E.; Yarfi, J. L.; Bachovchin, K. A.; Mazzoni, M. R.; and Merritt, J. R., "Identifying bias in CCR1 antagonists using radiolabelled binding, receptor internalization, β-arrestin translocation and chemotaxis assays" (2014). Kean Publications. 2004.