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 α,α-disubstituted amino acid, or may comprise a crosslinker linking the α-positions of at least two amino acids or at least one of said two amino acids may be an α,α-disubstituted amino acid. Further included is the targeting of components of the Wnt signaling pathway such as the Tcf4-/3-catenin complex.
本发明公开了包含螺旋(如α螺旋)的拟肽大环以及使用这种大环治疗疾病(如癌症)的方法。在其他方面,拟肽大环包括α,α-二取代
氨基酸,或可包括连接至少两个
氨基酸的α-位的
交联剂,或所述两个
氨基酸中的至少一个可以是α,α-二取代
氨基酸。还包括靶向 Wnt 信号通路的成分,如 Tcf4-/3-catenin 复合物。