Autophagy is a catabolic process responsible for the degradation and recycling of misfolded proteins and damaged organelles for cellular homeostasis. This degradative pathway,closely related to many diseases including cancer,has become a focus of cancer research. lt can serve as a tumor suppressor,also functions as a protective cell-survival mechanism against chemotherapies. Of the autophagy-related proteins,vacuolar protein sorting 34(VPS34)has attracted major attention over the past decade because of its role in autophagic procedure. Recently,three specific inhibitors of VPS34,PlK-Ⅲ,VPSlN1 and SlR405,have been invented,showing unique implications for autophagy reduction and therapeutic benefit in tumor treatment. This paper summarizes the different roles of autophagy in clinical settings and the functional regulation of VPS34 upon post-translational modification and also discusses the application prospects of inhibitors targeting VPS34 or autophagy in cancer prevention and treatment.