Na⁺/K⁺-ATPase(NKA) is an anion channel protein with ATPase activity embedded in thecytoplasmic membrane.Generally,only 30% of NKAs is engaged in ion pumping,and most of NKAs mainly plays the role of signal transduction.NKA α1 subunit (ATP1A1) is mainly involved in Src-mediated signal transduction,initiating kinase cascade signal transduction,leading to the activation of downstream key signaling pathways (PI3K,Ras/Raf/ERK,PLC/PKC),playing an important role in regulating cell proliferation,differentiation and apoptosis.However,the expression of ATP1A1 gene is differentially in different tumor cells.Usually,over expression of ATP1A1 is found in lung cancer,liver cancer,breast cancer and glioblastoma,but is low in prostate cancer,renal cancer,colon cancer and other cancer cells.Over or low expression of ATP1A1 is closely related to tumor proliferation,disease progression and survival of patients.At present,a variety of NKA inhibitors have entered the clinical research stage of anti-tumor effects.In this paper,we will present an overview of the expression of ATP1A1 gene in different tumor cells,the molecular mechanism of ATP1A1 involved in signal transduction and the current therapeutic target of ATP1A1 in order to provide useful guidance for the follow-up research.