Identifying bias in CCR1 antagonists using radiolabelled binding, receptor internalization, β-arrestin translocation and chemotaxis assays
Document Type
Article
Publication Date
1-1-2014
Abstract
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.
Publication Title
British Journal of Pharmacology
First Page Number
5127
Last Page Number
5138
DOI
10.1111/bph.12835
Recommended Citation
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.
https://digitalcommons.kean.edu/keanpublications/2004