Chemokines belong to a large family of chemoattractant molecules involved in the directed migration of immune cells. They achieve their cellular effects by direct interaction with cell surface receptors. Chemokines appear to be involved in a variety of proinflammatory and autoimmune diseases and this makes them and their receptors very attractive therapeutic targets. This review highlights current efforts toward obtaining highly specific chemokine receptor antogonists and discusses their chemistry and potential role as disease modifiers. ©2000 John Wiley & Sons, Inc. Med Res Rev, 20, No. 2, 155–168, 2000