Cytoplasmic glutathione S-transferase (GST) is a key enzyme in cellular detoxification, catalysing the nucleophilic attack of glutathione (GSH) with toxic electrophilic substrates to produce less harmful compounds, thus aiding cellular detoxification. Studies have shown that GST is closely associated with the development of resistance to chemotherapeutic drugs, pesticides, herbicides and antibiotics, and the development of drug resistance in organisms poses new challenges in areas such as environmental protection and tumour therapy. In order to clarify the mechanism of GST in the development of drug resistance and detect the content of GST more accurately, this paper summarized the mechanism of GST on the development of drug resistance in different organisms, the types and research progress of organic small molecule fluorescence probes for GST imaging detection are introduced.