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Inhibitors of GSK-3 and crystal structures of GSK-3β protein and protein complexes

机译:GSK-3抑制剂和GSK-3β蛋白及蛋白复合物的晶体结构

摘要

The present invention relates to inhibitors of GSK-3 and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors and methods of utilizing those compositions in the treatment and prevention of various disorders, such as diabetes and Alzheimer's disease. In addition, the invention relates to molecules or molecular complexes which comprise binding pockets of GSK-3β or its homologues. The invention relates to a computer comprising a data storage medium encoded with the structure coordinates of such binding pockets. The invention also relates to methods of using the structure coordinates to solve the structure of homologous proteins or protein complexes. The invention relates to methods of using the structure coordinates to screen for and design compounds that bind to GSK-3β protein or homologues thereof. The invention also relates to crystallizable compositions and crystals comprising GSK-3β protein or GSK-3β protein complexes.
机译:本发明涉及GSK-3抑制剂和制备这些抑制剂的方法。本发明还提供了包含抑制剂的药物组合物,以及利用这些组合物治疗和预防各种疾病,例如糖尿病和阿尔茨海默氏病的方法。另外,本发明涉及包含GSK-3β或其同源物的结合口袋的分子或分子复合物。本发明涉及一种包括数据存储介质的计算机,该数据存储介质被编码有这种装订袋的结构坐标。本发明还涉及使用结构坐标来解析同源蛋白质或蛋白质复合物的结构的方法。本发明涉及使用结构坐标来筛选和设计与GSK-3β蛋白或其同源物结合的化合物的方法。本发明还涉及包含GSK-3β蛋白或GSK-3β蛋白复合物的可结晶组合物和晶体。

著录项

  • 公开/公告号US8318467B2

    专利类型

  • 公开/公告日2012-11-27

    原文格式PDF

  • 申请/专利权人 ERNST TER HAAR;LOVORKA SWENSON;

    申请/专利号US20100944909

  • 发明设计人 ERNST TER HAAR;LOVORKA SWENSON;

    申请日2010-11-12

  • 分类号C12N9;C12N9/10;

  • 国家 US

  • 入库时间 2022-08-21 16:43:19

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