首页> 外国专利> BIFUNCTIONAL MOLECULES CONTAINING AN E3 UBIQUITINE LIGASE BINDING MOIETY LINKED TO A BCL6 TARGETING MOIETY

BIFUNCTIONAL MOLECULES CONTAINING AN E3 UBIQUITINE LIGASE BINDING MOIETY LINKED TO A BCL6 TARGETING MOIETY

机译:含有与BCl6靶向部分连接的E3泛素连接酶结合部分的双官能分子

摘要

Bifunctional compounds, which find utility as modulators of B-cell lymphoma 6 protein (BCL6; target protein), are described herein. In particular, the bifunctional compounds of the present disclosure contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand that binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The bifunctional compounds of the present disclosure exhibit a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
机译:本文描述了双官能化合物,其作为B细胞淋巴瘤6蛋白(BCL6;靶蛋白)的调节剂。特别地,本公开的双官能化合物含有von hippel-lindau,遗传蛋白或小鼠抑制剂或小鼠双重同源物2配体,其与相应的E3泛素连接酶结合,另一端是部分结合靶蛋白,使得靶蛋白邻近泛素连接酶,以实现靶蛋白的降解(和抑制)。本公开的双官能化合物表现出与靶蛋白的降解/抑制相关的广泛的药理学活性。用本公开的化合物和组合物处理或预防由靶蛋白的聚集或积聚产生的疾病或病症。

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