Dysregulated production of adipokines from adipose tissue plays a critical role in the development of obesity‐associated cardiovascular abnormalities. A group of adipokines, including adipocyte fatty acid binding protein (A‐FABP) and lipocalin‐2, possess specific lipid‐binding activity and are up‐regulated in obese human subjects and animal models. They act as lipid chaperones to promote lipotoxicity in endothelial cells and cause endothelial dysfunction under obese conditions. However, different small lipid‐binding proteins modulate the development of vascular complications in distinctive manners, which are partly attributed to their specialized structural features and functionalities. By focusing on A‐FABP and lipocalin‐2, this review summarizes recent advances demonstrating the causative roles of these newly identified adipose tissue‐derived lipid chaperones in obesity‐related endothelial dysfunction and cardiovascular complications. The specific lipid‐signalling mechanisms mediated by these two proteins are highlighted to support their specialized functions. In summary, A‐FABP and lipocalin‐2 represent potential therapeutic targets to design drugs for preventing vascular diseases associated with obesity.

LINKED ARTICLES This article is part of a themed section on Fat and Vascular Responsiveness. To view the other articles in this section visit http://dx.doi.org/10.1111/bph.2012.165.issue‐3