公开(公告)号：EP2810655A1

公开(公告)日：2014-12-10

申请号：EP13740969.4

申请日：2013-01-28

申请人： Osaka University

发明人： ISHII, Masaru ,  KAGAWA, Yoshinori ,  MORI, Masaki ,  ISHII, Hideshi

IPC分类号： A61K45/00 ,  A61K31/7088 ,  A61K31/711 ,  A61K48/00 ,  A61P35/00 ,  C12N15/113 ,  C12Q1/68 ,  G01N33/15 ,  G01N33/50 ,  G01N33/574

CPC分类号： C12N15/113 ,  A61K31/7115 ,  C12N2310/11 ,  C12N2310/3231 ,  C12N2310/3341 ,  C12Q1/6886 ,  C12Q2600/112 ,  C12Q2600/136 ,  C12Q2600/158 ,  C12Q2600/178 ,  G01N33/5011 ,  G01N2333/726 ,  G01N2500/04 ,  G01N2800/7028

摘要： The present invention provides a novel antitumor agent that acts through a novel mechanism. The novel antitumor agent contains as an active ingredient a substance capable of inhibiting a cell cycle-dependent Rho GTPase activating protein (RhoGAP). The RhoGAP is cell cycle-dependent and plays an important role in a process through which cancer cells acquire invasive capacity and/or metastatic capacity. The invasion and/or metastasis of cancer cells can be controlled by targeting the RhoGAP. Examples of the substance capable of inhibiting a cell cycle-dependent RhoGAP include an antisense oligonucleotide against a gene encoding the RhoGAP and an oligonucleotide that induces RNA interference of the gene. As the oligonucleotide, one containing an artificial nucleic acid such as BNA is preferred because of its excellent stability. The present invention also provides a screening method including selecting an antitumor agent capable of suppressing cancer cell invasion and/or metastasis through a novel mechanism. The screening method is a screening method for a novel antitumor agent, including selecting a substance capable of inhibiting a cell cycle-dependent Rho GTPase activating protein.

摘要翻译： 本发明提供了一种通过新型机制起作用的新型抗肿瘤剂。 新型抗肿瘤剂含有作为活性成分的能够抑制细胞周期依赖性Rho GTPase激活蛋白（RhoGAP）的物质。 RhoGAP是细胞周期依赖性的，并且在癌细胞获得侵袭能力和/或转移能力的过程中起重要作用。 可以通过靶向RhoGAP来控制癌细胞的侵袭和/或转移。 能够抑制细胞周期依赖性RhoGAP的物质的实例包括针对编码RhoGAP的基因的反义寡核苷酸和诱导该基因的RNA干扰的寡核苷酸。 作为寡核苷酸，由于其优异的稳定性，因此优选含有人造核酸如BNA的寡核苷酸。 本发明还提供一种筛选方法，其包括通过新的机制选择能够抑制癌细胞侵袭和/或转移的抗肿瘤剂。 筛选方法是新型​​抗肿瘤剂的筛选方法，包括选择能够抑制细胞周期依赖性Rho GTPase激活蛋白的物质。