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1. 发明申请

WO1997011174A1 CYCLIN DEPENPENT KINASE BINDING COMPOUNDS 审中-公开
标题翻译：循环激素激酶结合化合物
公开(公告)号：WO1997011174A1
公开(公告)日：1997-03-27
申请号：PCT/GB1996002340
申请日：1996-09-23
申请人： UNIVERSITY OF DUNDEE , FAHRAEUS, Robin , LANE, David, Philip
发明人： UNIVERSITY OF DUNDEE
IPC分类号： C12N15/12
CPC分类号： C07K14/4703 , A61K38/00 , C07K14/4738 , C07K2319/02
摘要： The present invention identifies substances having the property of binding to cyclin dependent kinase (cdk) comprising: (i) a peptide including amino acid residues 84 to 103 of full length p16 protein, or an active portion or derivative thereof; or (ii) a functional mimetic of the fragment, active portion or derivative; the substance excludes full length p16, p15, p18 and p19 proteins. These substances are useful in tumour suppression by inhibiting the phosphorylation of Rb protein. Also described herein is the resolution of the amino acid motifs responsible for binding cdks, an FLD motif, corresponding to amino acid residues 90 to 92 of full length p16 protein, and an LVVL motif, corresponding to amino acid residues 94 to 97 of full length p16 protein. The substances disclosed herein can be used in the treatment of hyperproliferative disorders and to screen and design molecules having the similar properties.
摘要翻译：本发明鉴定具有与细胞周期蛋白依赖性激酶（cdk）结合的性质的物质，其包含：（i）包含全长p16蛋白的氨基酸残基84至103的肽或其活性部分或衍生物; 或（ii）片段，活性部分或衍生物的功能模拟物; 该物质不包括全长p16，p15，p18和p19蛋白。这些物质通过抑制Rb蛋白的磷酸化可用于肿瘤抑制。本文还描述了负责结合cdks的氨基酸基序的分辨率，对应于全长p16蛋白的90至92的氨基酸残基的FLD基序和对应于全长的氨基酸残基94至97的LVVL基序 p16蛋白。本文公开的物质可用于治疗过度增殖性疾病并筛选和设计具有相似性质的分子。

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