Pathophysiological roles of chemokines, and their cognate receptors have helped elucidating the detailed molecular mechanisms of leukocyte trafficking and activation in inflammatory diseases. Chemokine / chemokine receptor systems might be essential for the pathogenesis of phase-specific renal disorders and the measurement of urinary levels of chemokines might be clinically useful for monitoring different disease phases and activities. In addition, chemokine receptors expressed in renal resident cells may be involved in proliferation, proteinuria, and fibrogenesis as well as chemotaxis. Importantly, the selective intervention of chemokine / chemokine receptor systems (anti-chemokine therapy) may have potential as therapeutic strategies for renal diseases. Despite the apparent redundancy in the chemokine systems, accumulating evidence supports this concept. Small molecule inhibitors of the chemokine / chemokine receptor systems are now being developed. We anticipate that active, orally bio-available inhibitors of chemokines / chemokine receptors for progressive renal diseases as well as other inflammatory disorders will be developed.