首页> 外国专利> COMPOUNDS AND METHODS OF STRENGTHENING THE DEGRADATION OF TARGET TARGETS AND OTHER POLYPEPTIDES USING E3 UUBIQUITINE LIGASES

COMPOUNDS AND METHODS OF STRENGTHENING THE DEGRADATION OF TARGET TARGETS AND OTHER POLYPEPTIDES USING E3 UUBIQUITINE LIGASES

机译:使用E3尿嘧啶连接酶加强降解目标靶标和其他多肽的化合物和方法

摘要

The present invention relates to bifunctional compounds, which find utility as modulators of targeted ubiquitination, especially of a variety of polypeptides and other proteins which are degraded and/or otherwise inhibited by bifunctional compounds according to the present invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand which binds to the ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of targeted polypeptides.
机译:本发明涉及双功能化合物,其可用作靶向泛素化的调节剂,尤其是被根据本发明的双功能化合物降解和/或抑制的多种多肽和其他蛋白质的调节剂。特别地,本发明涉及化合物,该化合物的一端含有与泛素连接酶结合的VHL配体,而另一端含有与靶蛋白结合的部分,从而使靶蛋白与泛素连接酶相邻。影响该蛋白质的降解(和抑制)。本发明表现出与根据本发明的化合物有关的广泛的药理活性,这与靶多肽的降解/抑制一致。

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