Fatty acid-binding proteins (FABPs) are abundant 14-15-kDa cytoplasmic proteins expressed in almost all mammalian tissues. They coordinate lipid responses in cells and related with metabolic and inflammatory pathways. FABPs bind to hydrophobic ligands, such as saturated and unsaturated long-chain fatty acids and eicosanoids with high affinity. They play a role in lipid transport to the specific compartments in the cell. Since the initial discovery of FABPs in 1972, at least nine members have been identified. Adipocyte FABP (A-FABP) is highly expressed in the adipose tissue and macrophages. A-FABP deficient mice exhibited reduced hyperinsulinaemia and insulin resistance in the context of both dietary and genetic obesity. Recent studies have shown that, inhibition of A-FABP has potential therapeutic effects against insulin resistance, diabetes, fatty liver and atherosclerosis. In this review, we focused on the structure and functions of FABPs, and the role of A-FABP on the metabolic processes and possible therapeutic approaches.