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CC chemokine receptor (CCR) antagonists block G protein-coupled receptors that guide leukocyte migration. CCR2, a receptor for monocyte chemoattractant protein 1 (MCP-1), was cloned in 1994 as two splice variants. CCR5 was identified in 1996 as a fusion cofactor for macrophage-tropic human immunodeficiency virus type 1 (HIV-1). Maraviroc, described in 2005 as a selective small-molecule CCR5 inhibitor, blocks this route of viral entry. Other CCR5 antagonists include vicriviroc malate and aplaviroc, while INCB3344 and MK-0812 target CCR2. Cenicriviroc blocks both CCR2 and CCR5, and GSK2239633A is a CCR4 antagonist for studies of T cell trafficking.
