DNA Methylase Inhibitors

我们的研究与表观遗传药物，泽布拉林，DNA甲基化抑制剂继续。去年发表的这篇文章（《癌症预防》2008,1,233 -240）为表观遗传疗法在癌症预防中的应用提供了强有力的数据支持。因此，为了探索西布拉林在慢性给药后的作用，一项新的小鼠体内研究的资金已经被批准，该研究使用两种人类异种移植物：非小细胞肺癌和膀胱癌。这将使用口服西布拉林和平行药代动力学（PK）研究来完成。由于雌性小鼠对乙醛氧化酶（AO）的代谢很少，因此本研究将只使用雌性小鼠。还考虑将AO抑制剂（雷洛昔芬）与西布拉林联合使用。一项新的研究揭示了zebularine的作用机制（生化药理学2009,78,633641）。甲基化抑制剂。

Our investigations with the epigenetic drug, zebularine, an inhibitor of DNA methylation continue. The article published last year (Cancer Prevention Res. 2008, 1, 233-240) provided strong data in support of epigenetic therapy in cancer prevention. Therefore, in order to explore the effects of zebularine following chronic administration, funds for a new in vivo study in mice using two human xenografts: NSCLC and Bladder carcinoma have been approved. This will be done using oral zebularine and a parallel pharmacokinetic (PK) study. Because the metabolism of zebularine by aldehyde oxidase (AO) is minimal in female mice, this study will use only female mice. Combined used of an AO inhibitor (Raloxifene) with zebularine is also contemplated. A new study that sheds light on the mechanism of zebularine has been published (Biochemical Pharmacology 2009, 78, 633641). the methylation inhibitor.