Valosin-containing protein is a membrane-bound protein that is highly conserved and widely existed in cells. Valosin-containing protein and it’s cofactors jointly participate in various cell functions such as protein degradation, gene replication, and cell cycle regulation, which maintain cellular homeostasis. Valosin-containing protein also exists in tumor cells, and its expression is closely related to the occurrence and development of tumors, but the specific mechanism needs to be further clarified. The application of valosin-containing protein inhibitors in tumor treatment has been continuously and in-depth researched. This article will explore several aspects of the molecular basis of valosin-containing protein, valosin-containing protein and cell homeostasis, tumors, and targeted therapy with valosin-containing protein. It aims to provide a certain basis for the clinical application of valosin-containing protein inhibitors.