Abstract Activating protein 1 (AP-1) is a transcription factor composed of several protein families, Jun proteins and Fos proteins are the components of AP-1. AP-1 is involved in various cellular processes, such as proliferation, differentiation, apoptosis and inflammation. For tumor cells, AP-1 is considered to be a driver whose activity is associated with dysfunction and the onset, development, invasion, and migration of cancer. In addition, AP-1 has been reported to be involved in the drug resistance and radiation resistance of tumor cells during the treatment process. Therefore, AP-1 is a potential target for cancer therapy. At present, a number of inhibitors targeting AP-1 have been developed and have shown certain anti-cancer effects. However, due to the complex structure and function of AP-1, different structures of AP-1 show different effects in different tumor cells, and more studies are needed to reveal its mechanism of action. This article introduces the relationship between AP-1 and tumor development, summarize the current studies and developments of AP-1 related drugs, and provide the future development values of AP-1.