DNA Methylase Inhibitors

我们对表观遗传药物zebularine的研究，zebularine是一种DNA抑制剂， 甲基化继续进行。去年发表的文章（Cancer Prevention Res.2008，1， 233 - 240）提供了支持癌症预防中的表观遗传疗法的有力数据。 因此，为了探索zebularine在长期给药后的作用， 一项新的使用两种人类异种移植物（NSCLC和膀胱癌）的小鼠体内研究的资金 已经被批准了。这将使用口服zebularine和平行的药代动力学 (PK)study.由于在雌性动物中，通过醛氧化酶（AO）代谢的zebularine很少 本研究仅使用雌性小鼠。AO抑制剂（雷洛昔芬）与 也考虑了泽布拉林。一项新的研究揭示了zebularine的作用机制 已经发表（Biochemical Pharmacology 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.