Calicheamicin is a highly potent enediyne antibiotic known for its exceptional cytotoxicity and precise DNA-cleaving activity. Isolated from Micromonospora echinospora, it binds to the minor groove of DNA and induces double-strand breaks, making it one of the most powerful antitumor agents ever discovered. Due to its extreme potency, calicheamicin is widely used as a payload in antibody–drug conjugates (ADCs), enabling targeted delivery in cancer therapy.
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