Recent developments in CCR2 antagonists

Expert Opin Ther Pat. 2009 Mar;19(3):295-303. doi: 10.1517/13543770902755129.


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.

Publication types

  • Review

MeSH terms

  • Animals
  • Anti-Inflammatory Agents / pharmacology
  • Chemokine CCL2 / metabolism*
  • Chemotaxis / physiology
  • Disease Models, Animal
  • Drug Design
  • Humans
  • Inflammation / drug therapy*
  • Inflammation / physiopathology
  • Monocytes / metabolism
  • Patents as Topic
  • Receptors, CCR2 / antagonists & inhibitors*


  • Anti-Inflammatory Agents
  • CCL2 protein, human
  • CCR2 protein, human
  • Chemokine CCL2
  • Receptors, CCR2