First, owing to the classic mechanosensitive role of GPCRs and the regulation of GPCRs by GRK2, as well as the important role of AP‐1 in inflammatory responses, targeting GRK2/AP‐1 signaling pathway could be a potential therapeutic strategy for preventing or mitigating atherosclerosis, particularly in regions exposed to disturbed flow. This evidence concerns the gene GRK2 and atherosclerosis.