[EN] COMPOUNDS USEFUL FOR PROMOTING PROTEIN DEGRADATION AND METHODS USING SAME<br/>[FR] COMPOSÉS UTILES POUR STIMULER LA DÉGRADATION DES PROTÉINES ET PROCÉDÉS UTILISANT CEUX-CI
申请人:UNIV YALE
公开号:WO2013170147A1
公开(公告)日:2013-11-14
The present invention includes compounds that act as degraders of a target protein, wherein degradation is independent of the class of the target protein or its localization. In one embodiment, the invention comprises a compound comprising a protein degradation moiety covalently bound to a linker, wherein the ClogP of the compound is equal to or higher than 1.5. The target protein contemplated within the invention comprises a posttranslational modified protein or intracellular protein. Compounds of the present invention may be used to treat disease states wherein protein degradation is a viable therapeutic approach, such as cancer or any sort of oxidative stress disease state.
本发明包括作为目标蛋白质降解剂的化合物,其中降解与目标蛋白质的类别或其定位无关。在一种实施方式中,该发明包括一种化合物,其中蛋白质降解基团与连接剂共价结合,该化合物的ClogP等于或高于1.5。本发明中考虑的目标蛋白质包括后转录修饰蛋白质或细胞内蛋白质。本发明的化合物可用于治疗蛋白质降解是一种可行的治疗方法的疾病状态,如癌症或任何一种氧化应激疾病状态。