Abstract: Atherosclerosis is a chronic inflammatory pathologic change of blood vessels. The retention and accumulation of low density lipoprotein, oxidized low-density lipoprotein, and other modified forms of modified lipoproteins in the intima of the vessels is considered to be one of the initiating steps for atherosclerosis. Lectin-like oxidized low-density lipoprotein receptor 1 (LOX-1) has been proven to be significantly important in the development and progression of atherosclerosis. Accumulating evidence has emerged to support the diversity of extracellular legends for LOX-1 to induce intracellular effects. Current literature has revealed several drugs that could inhibit the progression of atherosclerosis through blocking or reducing LOX-1. The current review focuses on recent progress into the cell biological effects of LOX-1 in atherosclerosis and LOX-1 targeted medication.