Recent developments in CCR2 antagonists

被引:155
作者
Xia, Mingde [1 ]
Sui, Zhihua [1 ]
机构
[1] Johnson & Johnson Pharmaceut Res & Dev LLC, Cranbury, NJ 08512 USA
关键词
asthma; CCR2; antagonist; MCP-1; multiple sclerosis; rheumatoid arthritis; MONOCYTE CHEMOATTRACTANT PROTEIN-1; CHEMOKINE RECEPTOR-2 ANTAGONISTS; DISEASE; DISCOVERY; RECRUITMENT; MACROPHAGES;
D O I
10.1517/13543770902755129
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Monocyte chemoattractant protein-1 (MCP-1) is a major chemoattractant for monocytes and memory T cells by means of their binding to its specific cell-surface receptor, CC-chemokine receptor-2 (CCR2). CCR2 belongs to the G-protein-coupled seven-transmembrane receptor superfamily. The evidence in favor of CCR2 and MCP-1 having dominant roles in monocyte chemotaxis and chronic inflammation was provided by CCR2 and MCP-1 knockout mice. It has been recognized that CCR2 antagonists are potential therapeutic agents in preventing, treating, or ameliorating a CCR2-mediated inflammatory syndrome or disease such as psoriasis, uveitis, rheumatoid arthritis, multiple sclerosis, asthma, obesity, and chronic obstructive pulmonary disease. This review summarizes recent developments in small-molecule CCR2 antagonists disclosed by patent applications published between 2005 and 2008 and related publications.
引用
收藏
页码:295 / 303
页数:9
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