OBJECTIVE Recently, initial studies have been carried out in patients using monocyte chemoattractant protein-1 (MCP-1) inhibitors. This review summarizes the known function of MCP-1 in regulating monocytes during inflammation and its role in inflammatory disease of the kidney. RESULTS MCP-1 is one of the first chemokines described and plays an important role in renal inflammatory disease. The function of MCP-1 has been investigated and analyzed in both animal models of renal disease and renal patients. MCP-1 mediates firstly the release of monocytes from the bone marrow, and then generates a gradient in the endothelial glycocalyx to direct monocytes to sites of inflammation, thereby alleviating the migration of blood leukocytes into the inflamed tissue. In addition, MCP-1 has direct signaling effects in monocytes and influences migration, proliferation, and differentiation of leukocytes. Blockade of MCP-1 in several models of renal disease has ameliorated the disease, suggesting that inhibition of MCP-1 is a promising and valid strategy to treat patients with renal inflammatory disease. CONCLUSIONS Understanding the role of MCP-1 in monocyte homeostasis and the implications of MCP-1 inhibition in renal disease will help in designing better diagnostic and therapeutic strategies in patients with inflammatory renal disease.