DZ-1-artesunate

DZ-1-artesunate (DZ-1-ART) is an experimental small molecule drug conjugate consisting of the heptamethine cyanine dye DZ-1 and the antimalarial/anticancer agent artesunate. DZ-1 serves as a tumor-homing and mitochondria-targeting vector, utilizing the high mitochondrial membrane potential of cancer cells to achieve selective intracellular accumulation. Once localized within the mitochondria, the artesunate moiety induces the generation of reactive oxygen species (ROS), which leads to the disruption of mitochondrial membrane potential and the activation of mitochondria-mediated apoptotic pathways. The conjugate also possesses near-infrared (NIR) fluorescence properties, allowing for potential theranostic applications. Research has demonstrated its efficacy in inducing cytotoxicity in patient-derived colorectal cancer tumoroids, suggesting its potential as a precision therapy for malignant neoplasms.

Other names

heptamethine cyanine dye-conjugated artesunateDZ-1-artesunate conjugateDZ1-artesunate conjugateDZ 1-artesunate conjugate