neocarzinostatin

Neocarzinostatin is a **macromolecular chromoprotein enediyne antitumor antibiotic** produced by Streptomyces macromomyceticus or Streptomyces carzinostaticus[1][3][5][7]. It consists of a **potent, labile enediyne chromophore** non-covalently bound to a 113-amino-acid protein, which stabilizes the chromophore and releases it at target DNA[1][3][7]. The chromophore acts by undergoing reductive activation in cells, triggering a Bergman cyclization and generating a benzenoid diradical; this leads to **sequence-selective single- and double-strand DNA breaks**, inhibiting DNA synthesis and inducing cell cycle arrest and apoptosis[1][3][5][6][7]. Neocarzinostatin has **antibiotic activity against Gram-positive bacteria** and **antitumor activity in liver cancer, leukemia, bladder cancer, and other solid tumors**, but clinical use is limited mainly to Japan due to its instability and toxicity[1][2][3][5][7].

Brand names

Zinostatin

Other names

holoneocarzinostatinmitomalcin