Dehydroaltenusin

Dehydroaltenusin 脱氢阿霉素是真核DNA 聚合酶 α (DNA polymerase α) 的小分子选择性抑制剂，一种由真菌产生的抗生素，其 IC50值为 0.68 μM。 Dehydroaltenusin 对哺乳动物 polα 活性的抑制作用模式对 DNA 模板引物 (Ki=0.23 μM) 是竞争性的，对 2'-脱氧核糖核苷 5'-三磷酸底物是非竞争性的 (Ki=0.18 μM)。Dehydroaltenusin 在 S 期阻止癌细胞周期并触发凋亡 apoptosis。Dehydroa

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Background

Dehydroaltenusin is a small molecule selective inhibitor of eukaryotic DNA polymerase α, a type of antibiotic produced by a fungus with an IC50 value of 0.68 μM. The inhibitory mode of action of dehydroaltenusin against mammalian pol α activity is competitive with respect to the DNA template primer (Ki=0.23 µM) and non-competitive with respect to the 2'-deoxyribonucleoside 5'-triphosphate substrate (Ki=0.18 µM)[1].Dehydroaltenusin arrests the cancer cell cycle at the S-phase and triggers apoptosis[1].Dehydroaltenusin possesses anti-tumor activity against human adenocarcinoma tumor in vivo[1]. IC50: 0.68 μM (DNA polymerase α)[1]

Dehydroaltenusin (38.0-44.4 μM; 24 hours) inhibits cell growth in a dose-dependent manner and the LD50 values varies from 38.0 to 44.4 μM[1].Dehydroaltenusin (38.0 μM; 6 hours) inhibits cell growth by blocking the S-phase of DNA replication[1].Dehydroaltenusin (75.0 μM; 24 hours) has a strong apoptotic effect on human cancer cells, DNA ladders can be detected after 12 h of incubation with dehydroaltenusin[1]. Cell Proliferation Assay[1] Cell Line: Human cancer cell line: A549, BALL-1, HeLa and NUGC-3 cells

Dehydroaltenusin (injection; 20 mg/kg; 2-day intervals; 12-39 days) shows suppressed tumor growth from 21 days[1]. Animal Model: Nude mice bearing HeLa solid tumors[1]

[1]. Mizushina Y, et al. Dehydroaltenusin is a specific inhibitor of mammalian DNA polymerase α. Expert Opin Investig Drugs. 2011 Nov;20(11):1523-34.