Abstract: Breast cancer cells are largely different in terms of energy metabolism, which refers to energy transformation from mi-tochondrial oxidative phosphorylation to glycolysis. However, energy supply of breast cancer cells is practically the same as that of nor -mal breast cells. The metabolic pathway is used to generate ATP as a main source of energy supply. This phenomenon is one of the most fundamental metabolic alterations during malignant transformation. This phenomenon mainly contributes to the over-activity of the key enzymes and some regulatory factors involved in the process, the targeting treatment of which provides a potential way to inhibit glycol -ysis and leads to cell death consequently. This review mainly summarizes the reported modulators and the key enzymes of glycolysis in breast cancer treatment over the past few years.