Streptozocin

Streptozocin is a nitrosourea antineoplastic antibiotic (nitrosourea antineoplastic antibiotic) and also an alkylating molecule with selective toxicity toward pancreatic beta cells. Structurally similar to glucose, streptozocin is efficiently taken up by the glucose transporter GLUT2. Because GLUT2 is highly expressed in pancreatic beta cells, streptozocin shows marked beta-cell selective toxicity. After entering cells, the nitrosourea moiety of streptozocin alkylates DNA, particularly causing DNA strand breaks and base damage. DNA damage activates PARP (poly ADP-ribose polymerase), resulting in massive consumption of NAD+ and ATP, rapid cellular energy depletion, and eventually necrosis or apoptosis. Streptozocin also promotes the generation of reactive oxygen species (ROS), further aggravating DNA and mitochondrion damage.