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    Ubiquitin ligase inhibitors
    7.
    发明申请
    Ubiquitin ligase inhibitors 审中-公开
    泛素连接酶抑制剂

    公开(公告)号：US20060160869A1

    公开(公告)日：2006-07-20

    申请号：US11325845

    申请日：2006-01-05

    申请人： Rajinder Singh ,  Usha Ramesh ,  Sarkiz Issakani ,  Jianing Huang ,  Taisei Kinoshita ,  Tarikere Gururaja

    发明人： Rajinder Singh ,  Usha Ramesh ,  Sarkiz Issakani ,  Jianing Huang ,  Taisei Kinoshita ,  Tarikere Gururaja

    IPC分类号： A61K31/427 ,  A61K31/426 ,  C07D277/38 ,  C07D417/02

    CPC分类号： C07D277/38 ,  C07D277/42

    摘要： This invention describes compounds and pharmaceutical compositions useful as ubiquitin agent inhibitors, particularly ubiquitin ligase inhibitors. The compounds and pharmaceutical compositions of the invention are useful as inhibitors of the biochemical pathways of organisms in which ubiquitination is involved, such as signal transduction pathways. The invention also comprises the use of the compounds and pharmaceutical compositions of the invention for the treatment of conditions that require inhibition of ubiquitination. Furthermore, the invention comprises methods of inhibiting ubiquitination in a cell comprising contacting a cell in which inhibition of ubiquitination is desired with a compound or pharmaceutical composition according to the invention. Particularly, the compounds and pharmaceutical compositions are useful to inhibit the ubiquitin ligase activity of MDM2.

    摘要翻译： 本发明描述了可用作泛素抑制剂，特别是泛素连接酶抑制剂的化合物和药物组合物。 本发明的化合物和药物组合物可用作其中涉及泛素化的生物体的生物化学途径的抑制剂，例如信号转导途径。 本发明还包括使用本发明的化合物和药物组合物来治疗需要抑制泛素化的病症。 此外，本发明包括在细胞中抑制泛素化的方法，包括使需要泛素化抑制的细胞与根据本发明的化合物或药物组合物接触。 特别地，化合物和药物组合物可用于抑制MDM2的泛素连接酶活性。

    Peptides causing formation of compact structures
    9.
    发明授权
    Peptides causing formation of compact structures 有权
    引起紧密结构形成的肽

    公开(公告)号：US06709814B1

    公开(公告)日：2004-03-23

    申请号：US09285912

    申请日：1999-04-02

    申请人： David Anderson ,  Tarikere Gururaja

    发明人： David Anderson ,  Tarikere Gururaja

    IPC分类号： C12N1563

    CPC分类号： C07K7/06 ,  C07K1/047 ,  C07K14/47

    摘要： The present invention is directed to compositions and methods including peptides which have a high affinity for each other and, when linked to a protein, are used to help fold the protein into a compact structure. By virtue of its stability and constraints, this scaffold can prolong the activity of any embedded protein sequences in the presence of cellular and other proteases. The compact structure can have other functional sequences embedded, and is preferable to linear and less constrained peptides for library screening, for creating structurally-biased peptide libraries and for targeting to specific intracellular and extracellular compartments. Compositions of the present invention can be displayed on the surface of viruses, archaebacteria, prokaryotic and eukaryotic cells for library screening, drug screening and display. Methods of the present invention are useful for screening in vivo for intracellular effector proteins modulating signaling pathways and to identify interacting proteins in vitro. Thus, the present invention is useful as a scaffold for gene therapy, for the isolation of new therapeutic drug leads and for potential use as a therapeutic in physiological fluids.

    摘要翻译： 本发明涉及组合物和方法，包括彼此具有高亲和力的肽，当与蛋白质连接时，用于帮助将蛋白质折叠成紧密结构。 由于其稳定性和约束，该支架可以延长任何嵌入的蛋白质序列在细胞和其它蛋白酶存在下的活性。 紧密结构可以具有嵌入的其它功能序列，并且优选用于文库筛选的线性和较不受约束的肽，用于产生结构偏向肽文库并靶向特定的细胞内和细胞外区室。 本发明的组合物可以显示在病毒，古细菌，原核和真核细胞的表面上，用于文库筛选，药物筛选和显示。 本发明的方法可用于体内筛选调节信号传导途径的细胞内效应蛋白，并在体外鉴定相互作用蛋白。 因此，本发明可用作基因治疗的支架，用于分离新的治疗药物引线和潜在用作生理液体中的治疗剂。