Choline kinase α (CHOKα), a member of the choline kinase family, is a key enzyme in the CDP-pathway. CHOKα has been reported overexpressed in a wide variety of human tumors including breast cancer, colorectal cancer, prostate cancer, and lung cancer. The interaction between CHOKα and cancer related pathways has been revealed. Due to its overexpression and aberrant activation in cancers, CHOKα is expected to be a potential biomarker and has been demonstrated to be a promising cancer therapeutic target. In this paper we reviewed the role of CHOKα in the tumorigenesis process, biological function, diagnosis and prognosis evaluation and tumor targeting therapy.