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Curr Top Med Chem. 2010;10(13):1278-98.

CCR2 antagonists.

Author information

1
Departments of Cardiovascular Disease, Merck & Co. Inc.; P.O. Box 2000, Rahway, NJ 07065, USA. mary_struthers@merck.com

Abstract

Inhibition of CCR2 has been considered as a target for multiple therapeutic diseases including autoimmune disease, atherosclerosis, pain, and metabolic disease, based in part on the critical role this receptor plays on monocyte migration. Numerous companies have reported programs to identify CCR2 antagonists. Common challenges to the development of CCR2 agents have included poor activity at the rodent receptor and selectivity for both other chemokine receptors and ion channels. This review summarizes the rationale for targeting CCR2 in disease, the recent progress in the identification of potent and select CCR2 antagonists, and the current status of clinical trials for CCR2 agents.

PMID:
20536421
DOI:
10.2174/156802610791561255
[Indexed for MEDLINE]

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