Adipocyte/macrophage fatty acid binding protein (A-FABP) has been shown to be closely associated with metabolic syndrome, obesity and development of atherosclerosis. Moreover, A-FABP has been recently suggested as a potential therapeutic target of these abnormalities in animal models. The present review aims to summarize current knowledge on A-FABP functions and regulations both in animal models and humans, since the role of A-FABP in human physiology and disease has not been presently clarified.