Phosphatide acid (PA) is a kind of multifunctional bioactive phospholipid. It has been proved that PA produced by lysophosphatide acid acyltransferase (LPAATbeta) was involved in several signalling pathways in tumor cells, leading to the proliferation, apoptosis, migration, invasion, respiratory burst, expression and release of cytokine form tumor cells. The fact that expression of LPAATbeta was higher in tumor tissues than in their homologous normal tissues, and that antitumor effect of inhibitng LPAATbeta on solid tumor and hematological malignancy suggested that the targeting LPAATbeta would be a promising method of antitumor treatment. In this paper, the relevant basic and preclinical researches of LPAATbeta on antitumor treatment were summarized.