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Diabetic nephropathy, a dominating cause of end stage renal disease as well as a lethal microvascular complication of diabetes mellitus, is characterized by progressive albuminuria, excessive deposition of extracellular matrix, thickened glomerular basement membrane, podocyte abnormalities and loss.There is a growing body of evidence showing that G protein coupled receptors are closely related to the development and progression of diabetic nephropathy, mainly consisting of prostaglandin E receptors, adenosine receptors, endothelin receptors, angiotensin Ⅱ type receptors, etc, which can be used as attractive targets for developing innovative strategies to treat patients with diabetic nephropathy.Therefore, it is appreciated that exploring the mechanism of GPCRs and related therapeutic targets for novel diagnostic and treatment of DN.Collectively, the possibilities are endless, and needless to say more work is essential for shed some light on the selectivity of therapeutic drugs acting on GPCRs in treating DN due to its multiple types and complex roles.This review will give us a comprehensive overview of G protein coupled receptors and focus on their types and roles in diabetic nephropathy.