Neocarzinostatin

Neocarzinostatin from Streptomyces carzinostaticus has been used:

• as a DNA damaging agent to treat human fibroblast GM0637 cells
• as a radiomimetic antibiotic to induce DNA damage
• in combination with Vγ2Vδ2 T cells to determine the cytotoxicity in ovarian cancer cells

Neocarzinostatin is a protein-small molecule complex composed of an enediyne chromophore tightly bound to a 113 amino acid single chain protein. The complex possesses antiproliferative and antitumor activity. The chromophore is the active compound, which is responsible for DNA cleavage; while the apoprotein stabilizes and regulates the availability of the labile chromophore. NCS chromophore is bound non-covalently in a cleft of the binding protein and is dissociable. Upon addition of a thiol, the chromophore forms a highly reactive biradical species that can induce sequence-specific single and double strand breaks in DNA. Neocarzinostatin inhibits DNA synthesis and possesses antitumor activity in various human and animal tumors. NCS inhibits cellular proliferation by inducing G₂ cell cycle arrest and apoptosis in both human papillomavirus (HPV) positive and negative cell lines.

Neocarzinostatin is a radiomimetic antibiotic substance.

Protein-small molecule complex composed of an enediyne chromophore tightly bound to a 113-amino acid single chain protein. Chemotherapeutic agent, which inhibits DNA synthesis, possesses antitumor activity, and induces apoptosis.

Supplied as 100 μg (~9 nmoles) in a solution containing 20 mM MES buffer, pH 5.5.