Myeloperoxidase（MPO）is an important member of the haemoglobin peroxidase-cyclooxygenase superfamily. It is expressed in a variety of inflammatory cells，including neutrophils，activated microglia，monocytes/macrophages，as well as astrocytes and neurons，and plays an important role in immune surveillance and host defense mechanisms. However，studies have found that the increased expression and activity of MPO is associated with the development and progression of several major diseases，including Parkinson’s disease，Alzheimer’s disease，stroke，and cardiovascular disease. Over the years，several pharmaceutical companies and research institutes have made a lot of progress in the development of MPO inhibitors. This review mainly summrizes the structure of MPO protein，its catalytic mechanism and the progress of inhibitor development，aiming to provide a reference for the development of this enzyme inhibitors.