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Current Topics in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

CCR2 Antagonists

Author(s): Mary Struthers and Alexander Pasternak

Volume 10, Issue 13, 2010

Page: [1278 - 1298] Pages: 21

DOI: 10.2174/156802610791561255

Price: $65

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.

Keywords: CCR2, autoimmune disease, atherosclerosis, metabolic disease, receptors, CCR2 antagonists


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