Neocarzinostatin is an effective DNA-damaging, anti-tumor antibiotic. It recognizes double-stranded DNA bulge and induces DNAdoublestrand breaks (DSBs). Neocarzinostatin leads to apoptosis. Neocarzinostatin has potential for EpCAM-positive cancer treatment.
XSJ05,一种喜树碱 (CPT) 衍生物,能有效抑制拓扑异构酶 I (Topo I) 以发挥抗癌作用。该化合物能促使 DNA 双链断裂,进而引起 DNA 损伤。此外,XSJ05 对抑制结直肠癌 (CRC) 生长具有显著效果,能使细胞周期在 G2 M 期暂停,并能诱导细胞凋亡 (apoptosis)。
Etoposide phosphate is a phosphate salt of Etoposide, which binds to the enzyme topoisomerase II, then induces double-strandDNA breaks and inhibits DNA repair, leading to decreased DNA synthesis and tumor cell proliferation.
Afeletecan is a water-soluble camptothecin derivative. Afeletecan stabilizes the topoisomerase I-DNA covalent complex and forms an enzyme-drug-DNA ternary complex. Both the initial cleavage reaction and religation steps are inhibited and subsequent collis
Cylindrospermopsin, a tricyclic uracil derivative, is a cyanobacterial toxin that was first discovered in an algal bloom contaminating a local drinking supply on Palm Island in Queensland, Australia after an outbreak of a mysterious disease. Cylindrospermopsin targets protein and glutathione synthesis in hepatocytes (IC50s = 1.3 and 2.4 µM, respectively), leading to cell death. [1] It has been shown to inhibit the activity of the uridine monophosphate synthase complex with a Ki value of 10 µM.[2] Cylindrospermopsin is genotoxic, inducing DNA damage as evidenced by doublestrand breaks and reducing cell viability in HepG2 cells at 0.1-0.5 µg ml.[3]