- 专利标题： BINDING INHIBITORS OF THE BETA. TRANSDUCIN REPEAT-CONTAINING PROTEIN
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申请号： US16129700申请日： 2018-09-12
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公开(公告)号： US20190106460A1公开(公告)日： 2019-04-11
- 发明人: Mark Bradley , Jeffrey George Andrew Walton , Sunay Vijaykumar Chankeshwara , Mazen Sleiman , George S. Baillie , Lucien Gibson
- 申请人： Mark Bradley , Jeffrey George Andrew Walton , Sunay Vijaykumar Chankeshwara , Mazen Sleiman , George S. Baillie , Lucien Gibson
- 优先权： GB1110938.6 20110627
- 主分类号： C07K14/00
- IPC分类号： C07K14/00 ; C07K7/08 ; C07K7/06 ; C07K7/64 ; A61K38/08 ; C12N9/00
摘要：
The present invention relates to compounds which bind to Beta Trans-ducin repeat-containing protein (βTrCP), and modulate the activity of βTrCP. In particular, the invention relates to compounds which demonstrate optimised binding to PTrCP. The invention also relates to pharmaceutical compositions comprising such compounds and the use of such compounds as medicaments, specifically for the treatment of disorders associated with aberrant protein degradation, such as cancer. The preferred binding inhibitors are peptides derived from the motive DSGXXS, e.g. DEGFWE, DDGFWD and Succinyl-EGFWE.
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