Recent Advances in the Development of Optical Imaging Probes for γ‐Glutamyltranspeptidase

Abstract γ‐Glutamyltranspeptidase (GGT) is a cell‐membrane‐bound protease that participates in cellular glutathione and cysteine homeostasis, which are closely related to many physiological and pathological processes. The accurate measurement of GGT activity is useful for the early diagnosis of diseases. In the past few years, many efforts have been made to build optical imaging probes for the detection of GGT activity both in vitro and in vivo. In this Minireview, recent advances in the development of various optical imaging probes for GGT, including activatable fluorescence probes, ratiometric fluorescence probes, and activatable bioluminescence probes, are summarized. This review starts from the instruction of the GGT enzyme and its biological functions, followed by a discussion of activatable fluorescence probes that show off–on fluorescence in response to GGT. GGT‐activatable two‐photon fluorescence imaging probes with improved imaging depth and spatial resolution are also discussed. Ratiometric fluorescence probes capable of accurately reporting on GGT levels through a self‐calibration mechanism are discussed, followed by describing GGT‐activatable bioluminescence probes that can offer a high signal‐to‐background ratio to detect GGT in living mice. Finally, current challenges and further perspectives for the development of molecular imaging probes for GGT are addressed.