Abstract: Phosphoglycerate kinase 1 (PGK1) is a key metabolic enzyme in the glycolysis pathway, which catalyzes the transfer of 1,3-bisphosphoglycerate (1,3-BPG) to 3-phosphoglycerate (3-PG) with ATP production. Over-expression of PGK1 has been observed in many types of malignance. Besides as a metabolic enzyme, PGK1 can also act as a protein kinase, which promotes the development and progression of tumors and correlates with chemoradiotherapy resistance and poor survival of cancer patients by regulating tumor cell metabolism. Functions of PGK1 were summarized in this article to provide theoretical basis for PGK1-targeting drug development.