Title

Identifying bias in CCR1 antagonists using radiolabelled binding, receptor internalization, β-arrestin translocation and chemotaxis assays

Authors

A. Gilchrist, College of Pharmacy
T. D. Gauntner, Chicago College of Osteopathic Medicine
A. Fazzini, Università di Pisa
K. M. Alley, Chicago College of Osteopathic Medicine
D. S. Pyen, College of Pharmacy
J. Ahn, College of Pharmacy
S. J. Ha, Chicago College of Osteopathic Medicine
A. Willett, College of Pharmacy
S. E. Sansom, Chicago College of Osteopathic Medicine
J. L. Yarfi, Kean University
K. A. Bachovchin, Kean University
M. R. Mazzoni, Università di Pisa
J. R. Merritt, Kean University

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