申请人:Moon Sung Hwan
公开号:US20100029630A1
公开(公告)日:2010-02-04
Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.
本文揭示了具有构象约束的化合物,其模拟生物活性肽和蛋白质的反转区域的二级结构。这种反转区域模拟结构在广泛的领域中具有实用性,包括用作诊断和治疗剂。本发明还揭示了包含这种反转区域模拟结构的文库,以及筛选这些文库以识别具有生物活性成员的方法。本发明还涉及使用这些化合物来抑制或治疗由Wnt信号通路调节的疾病,例如癌症,特别是结肠直肠癌,与血管成形术相关的再狭窄,多囊肾病,异常血管生成疾病,类风湿性关节炎疾病,结节性硬化症,阿尔茨海默病,过度生长或脱发,或溃疡性结肠炎。