公开(公告)号：US20050014206A1

公开(公告)日：2005-01-20

申请号：US10825688

申请日：2004-04-16

申请人： Hartmut Vodermaier ,  Christian Gieffers ,  Sebastian Maurer-Stroh ,  Frank Eisenhaber ,  Jan-Michael Peters ,  Michael Gmachl

发明人： Hartmut Vodermaier ,  Christian Gieffers ,  Sebastian Maurer-Stroh ,  Frank Eisenhaber ,  Jan-Michael Peters ,  Michael Gmachl

IPC分类号： C12Q1/37 ,  G01N33/567

CPC分类号： C12Q1/37 ,  G01N2500/02

摘要： A screening method for identifying specific APC inhibitors comprises a primary screen in which a compound is tested for its ability to interfere with binding of CDH1 or CDC20 to the APC and a secondary screen, in which the compound is tested for its ability to interfere with the activation of the APC by CDH1 or CDC20.

摘要翻译： 用于鉴定特异性APC抑制剂的筛选方法包括主筛选，其中化合物被测试其干扰CDH1或CDC20与APC结合的能力和次级筛，其中化合物被测试其干扰 通过CDH1或CDC20激活APC。

公开(公告)号：US07410774B1

公开(公告)日：2008-08-12

申请号：US09500991

申请日：2000-02-15

申请人： Frank Uhlmann ,  Kim Nasmyth ,  Jan-Michael Peters ,  Irene Waizenegger ,  Sara Buonomo ,  Rosemary Clyne

发明人： Frank Uhlmann ,  Kim Nasmyth ,  Jan-Michael Peters ,  Irene Waizenegger ,  Sara Buonomo ,  Rosemary Clyne

IPC分类号： C12Q1/00 ,  C12Q1/37 ,  C12N9/00 ,  C12N9/50 ,  C12N9/64 ,  C07K1/00

CPC分类号： G01N33/5011 ,  G01N2800/7023

摘要： Method for identifying compounds that interfere with or modulate sister chromatid separation in animal or plant cells by modulating a protease with separin-like cysteine endopeptidase activity. Inhibitors of separin activity are useful in cancer therapy, to prevent birth defects and to increase ploidy in plants.

摘要翻译： 通过调节具有分离样半胱氨酸内肽酶活性的蛋白酶鉴定在动物或植物细胞中干扰或调节姐妹染色单体分离的化合物的方法。 分离活性抑制剂可用于癌症治疗，以预防出生缺陷并增加植物中的倍性。

公开(公告)号：US5726025A

公开(公告)日：1998-03-10

申请号：US425299

申请日：1995-04-20

申请人： Marc W. Kirschner ,  Randall W. King ,  Jan-Michael Peters

发明人： Marc W. Kirschner ,  Randall W. King ,  Jan-Michael Peters

IPC分类号： C12Q1/25 ,  G01N33/68 ,  C12Q1/48 ,  G01N33/567

CPC分类号： G01N33/6842 ,  C12Q1/25 ,  G01N33/68

摘要： The present invention provides a systematic and practical approach for the identification of candidate agents able to inhibit ubiquitin-mediated degradation of a cell-cycle regulatory protein, such as cyclins. One aspect of the present invention relates to a method for identifying an inhibitor of ubiquitin-mediated proteolysis of a cell-cycle regulatory protein by (i) providing a ubiquitin-conjugating system that includes the regulatory protein and ubiquitin under conditions which promote the ubiquitination of the target protein, and (ii) measuring the level of ubiquitination of the subject protein brought about by the system in the presence and absence of a candidate agent. A decrease in the level of ubiquitin conjugation is indicative of an inhibitory activity for the candidate agent. The level of ubiquitination of the regulatory protein can be measured by determining the actual concentration of protein:ubiquitin conjugates formed; or inferred by detecting some other quality of the subject protein affected by ubiquitination, including the proteolytic degradation of the protein.

摘要翻译： 本发明提供了一种用于鉴定能够抑制泛素介导的细胞周期调节蛋白如细胞周期蛋白降解的候选试剂的系统和实用的方法。 本发明的一个方面涉及通过（i）在促进泛素化的条件下提供包含调节蛋白和泛素的泛素缀合系统来鉴定泛素介导的细胞周期调节蛋白的蛋白水解抑制剂的方法 目标蛋白质，以及（ii）测量在存在和不存在候选药剂的情况下由系统产生的受试蛋白质的泛素化水平。 泛素缀合水平的降低表明候选试剂的抑制活性。 调节蛋白的泛素化水平可以通过测定蛋白质的实际浓度来测量：泛素缀合物的形成; 或通过检测受泛素化影响的受试蛋白的一些其他质量，包括蛋白质的蛋白水解降解来推断。