DNMDP 是一种 PDE3A 抑制剂，是一种高效、选择性的肿瘤细胞毒药物。DNMDP 与 PDE3A 结合促进 PDE3A 与 Schlafen 12 (SLFN12) 之间的相互作用。DNMDP 具有明显的细胞选择性细胞毒性。
DNMDP, a phosphodiesterase 3A (PDE3A) inhibitor, is a potent and selective cancer cell cytotoxic agent. DNMDP binding to PDE3A promotes an interaction between PDE3A and Schlafen 12 (SLFN12). DNMDP shows clear cell-selective cytotoxicity[1].
DNMDP (0-1000 μM; 48 hours) shows clear cell-selective cytotoxicity[1]. HeLa cells undergo apoptosis upon DNMDP treatment, indicates by caspase activity detected by a caspase-sensitive luciferase assay and by poly ADP ribose polymerase (PARP) cleavage. At a concentration of 100 nM, DNMDP specifically inhibits both PDE3A and PDE3B, weakly inhibits PDE10, and had little or no detectable effect on other phosphodiesterases[1].
[1]. de Waal L, et al. Identification of cancer-cytotoxic modulators of PDE3A by predictive chemogenomics. Nat Chem Biol. 2016 Feb;12(2):102-8.
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