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
Current Topics in Medicinal Chemistry
Title: CCR2 Antagonists
Volume: 10 Issue: 13
Author(s): Mary Struthers and Alexander Pasternak
Affiliation:
Keywords: CCR2, autoimmune disease, atherosclerosis, metabolic disease, receptors, CCR2 antagonists
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.
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Cite this article as:
Struthers Mary and Pasternak Alexander, CCR2 Antagonists, Current Topics in Medicinal Chemistry 2010; 10 (13) . https://dx.doi.org/10.2174/156802610791561255
DOI https://dx.doi.org/10.2174/156802610791561255 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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