There is much interest in the role of oxidant stress in an ever-increasing list of disease states. However, the precise mediator of oxidant stress and the stressor molecule/s have not been identified. Accordingly, trials of inhibitors of oxidant stress in animal models of disease states have met only limited success. The trials of traditional anti-oxidant vitamins have been largely unsuccessful in the treatment of a wide array of disease states in humans. Recent identification of LOX-1 in vascular endothelial cells and its activation by oxidant species have led to a marked improvement in our understanding of the pathology of several cardiovascular disease states. Here, we review the disease states where therapy targeted at LOX-1 inhibition might be helpful.