In recent years, there has been an observed increase in the proportion of solid tumours of the digestive system, with the incidence of oesophageal, gastric, liver and colorectal cancers being particularly high. Conventional treatments such as surgical intervention and radiotherapy have proven to be ineffective in addressing progressive tumours, which often result in a poor long-term prognosis. Consequently, there is an emerging focus on the development of novel targeted therapies for digestive system tumours, which hold great potential to significantly improve the lives of patients affected by these conditions. Enhancer of Zeste Homolog 2(EZH2), a pivotal epigenetic protein, is highly expressed in numerous tumours and predominantly catalyses the trimethylation of lysine at position 27 of histone H3 (H3K27me3). In this paper, we explored the mechanism of action of EZH2 and its relationship with digestive system tumourigenesis and prognosis. We revealed the key role of EZH2 in the immune microenvironment, cell cycle, apoptosis and migration of digestive system tumours. We also enumerated the EZH2 inhibitors that have already been applied in the clinic as well as some of them that are undergoing both clinical and basic research. In summary, utilising EZH2 as a target to elucidate its mechanism of action in digestive system tumours and developing corresponding EZH2 inhibitors can provide novel concepts for the diagnosis, treatment and prognosis of digestive system tumours. |