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公开(公告)号:US20130072439A1
公开(公告)日:2013-03-21
申请号:US13497522
申请日:2010-09-22
申请人: Huw M. Nash , Rosana Kapeller-Libermann , Jia-wen Han , Tomi K. Sawyer , Justin Noehre , Noriyuki Kawahata
发明人: Huw M. Nash , Rosana Kapeller-Libermann , Jia-wen Han , Tomi K. Sawyer , Justin Noehre , Noriyuki Kawahata
摘要: Disclosed are peptidomimetic macrocycles comprising a helix, such as an alpha helix, and methods of using such macrocycles for the treatment of disease such as cancer. In other aspects, the peptidomimetic macrocycle comprises an a,a-disubstituted amino acid, or may comprise a crosslinker linking the a-positions of at least two amino acids or at least one of said two amino acids may be an a,a-disubstituted amino acid. Further included is the targeting of components of the Wnt signaling pathway such as the Tcf4-/3-catenin complex.
摘要翻译: 公开了包含螺旋的拟肽大环化合物,例如α螺旋,以及使用这种大环化合物治疗诸如癌症的疾病的方法。 在其它方面,拟肽大环化合物包含a,α-二取代的氨基酸,或可以包含连接至少两个氨基酸的a-位的交联剂或所述两个氨基酸中的至少一个可以是a, 氨基酸。 进一步包括靶向Wnt信号通路的组分,例如Tcf4- / 3-连环蛋白复合物。