Dimeric IAP inhibitors
    4.
    发明申请
    Dimeric IAP inhibitors 有权
    二聚体IAP抑制剂

    公开(公告)号:US20060194741A1

    公开(公告)日:2006-08-31

    申请号:US11363387

    申请日:2006-02-27

    IPC分类号: A61K38/04 C07K5/04

    摘要: Molecular mimics of Smac are capable of modulating apoptosis through their interaction with cellular IAPs (inhibitor of apoptosis proteins). The mimetics are based on a monomer or dimer of the N-terminal tetrapeptide of IAP-binding proteins, such as Smac/DIABLO, Hid, Grim and Reaper, which interact with a specific surface groove of LAP. Also disclosed are methods of using these peptidomimetics for therapeutic purposes. In various embodiments of the invention the Smac mimetics of the invention are combined with chemotherapeutic agents, including, but not limited to topoisomerase inhibitors, kinase inbhibitors, NSAIDs, taxanes and platinum containing compounds use broader language

    摘要翻译: Smac的分子模拟物能够通过它们与细胞IAP(凋亡蛋白的抑制剂)的相互作用来调节凋亡。 模拟物基于IAP结合蛋白的N末端四肽的单体或二聚体,例如Smac / DIABLO,Hid,Grim和Reaper,其与LAP的特定表面凹槽相互作用。 还公开了将这些肽模拟物用于治疗目的的方法。 在本发明的各种实施方案中,本发明的Smac模拟物与化学治疗剂组合,包括但不限于拓扑异构酶抑制剂,激酶抑制剂,NSAID,紫杉烷和含铂化合物使用更广泛的语言