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1.发明申请MONOAMINE OXIDASE INHIBITORS AND METHODS FOR TREATMENT AND DIAGNOSIS OF PROSTATE CANCER 有权单胺氧化酶抑制剂和前列腺癌治疗和诊断方法公开(公告)号：US20130039854A1
公开(公告)日：2013-02-14
申请号：US13559431
申请日：2012-07-26
IPC分类号： A61K31/405 , C07D319/18 , C07D311/36 , C07D311/54 , A61K31/381 , A61K31/357 , A61K31/352 , A61K31/366 , A61K31/7088 , A61K31/713 , A61K31/404 , C07D209/14 , C07D409/14 , C12N9/99 , C12Q1/26 , A61K49/00 , G01N33/574 , C12Q1/68 , A61P35/00 , C07D333/28
CPC分类号： A61K31/137 , A61K31/352 , A61K31/357 , A61K31/366 , A61K31/381 , A61K31/405 , A61K31/5375 , A61K31/713 , A61K47/545 , A61K47/55 , A61K47/6929 , A61K49/0032 , C12N15/1137 , C12N2310/14 , C12N2310/531 , C12Y104/03004
摘要： A mechanism of monoamine oxidases (MAOs) driven epithelium-to-mesenchymal transition (EMT) is disclosed. Also disclosed are methods for treating cancer by inhibiting or suppressing MAOs in cancer cells. Novel MAOs inhibitors, such as small molecules, siRNA, shRNA, antisense oligonucleotides, aptamers, decoys, and pharmaceutical compositions useful for treating cancer by disrupting the workings of MAOs are provided. In particular, a class of conjugates formed by covalently conjugating near infrared dye 783, IR-780, and MHI-148 to a MAO inhibitor, such as clorgyline, with and without encapsulation it in a nanoparticle is provided. Other aspects of the invention include methods for forming the nano-conjugates, method for monitoring treatment progress in a cancer patient by monitoring the changes in MAO activity, methods for screening patients who are at risk of cancer or differentiating different forms of cancer by assaying the level and location of MAO activity.
摘要翻译： 公开了单胺氧化酶（MAO）驱动上皮 - 间质转化（EMT）的机制。 还公开了通过抑制或抑制癌细胞中的MAO来治疗癌症的方法。 提供了新的MAO抑制剂，例如小分子，siRNA，shRNA，反义寡核苷酸，适体，诱饵和用于通过破坏MAO的运作来治疗癌症的药物组合物。 特别地，提供了通过将近红外染料783，IR-780和MHI-148共价结合到MAO抑制剂（例如clorgyline）上形成的一类缀合物，其具有和不将其包封在纳米颗粒中。 本发明的其它方面包括形成纳米缀合物的方法，通过监测MAO活性的变化来监测癌症患者的治疗进展的方法，用于筛选患有癌症风险的患者或通过测定不同形式的癌症来分化癌症的方法 水平和位置的MAO活动。
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