Abstract: As the key metabolic enzyme in the glycolytic pathway, phosphoglycerate mutase 1 (PGAM1) participated in the synthesis of intracellular biological macromolecules and maintained redox homeostasis by catalyzing the conversion of 3-phosphoglycerate (3-PG) to 2-phosphoglycerate (2-PG). Increasing evidence has suggested that PGAM1 also conveys metabolism-independent function of protein-protein interaction to aggravate tumor growth and metastasis. PGAM1, which is generally over-expressed in a variety of malignancies and is closely related to the patient's poor prognosis, plays a vital role in tumor progression. As a novel potential antitumor target, PGAM1 together with the research and development of its inhibitors has attracted great attention. This article reviews the role of PGAM1 in tumors and recent advances in the research on PGAM1 inhibitors.