[EN] AMPHIPHILIC THIOL COMPOUNDS AND USES THEREOF<br/>[FR] COMPOSÉS DE THIOL AMPHIPHILES ET LEURS UTILISATIONS
申请人:UNIV CALIFORNIA
公开号:WO2019178166A1
公开(公告)日:2019-09-19
Provided herein are, inter alia, amphiphilic thiol compounds and methods of using the same for the purpose of depalmitoylating proteins in cellular membranes (e.g., plasma membranes). The compounds provided herein include an amphiphilic tail, which enables them to associate with a cellular membrane and depalmitoylate (cleave native S-palmitoyl groups from) a protein in said membrane by native chemical ligation thereby triggering the protein's release from the plasma membrane. The compounds (amphiphilic thiol compounds of formula (I), (II), (III)) are, inter alia, useful for the treatment of diseases caused or associated with aberrant depalmitoylation of certain proteins (e.g., HRas, EGFR).
本文提供了一些两性硫醇化合物及其用于在细胞膜(例如,细胞膜)中去棕榈酰化蛋白质的方法。本文提供的化合物包括两性尾部,使它们能够与细胞膜结合,并通过本地化学连接去除(从)膜中的蛋白质上的天然S-棕榈酰基团,从而触发蛋白质从细胞膜中释放。这些化合物(公式(I)、(II)、(III)的两性硫醇化合物)等可用于治疗由于某些蛋白质(例如HRas、EGFR)异常去棕榈酰化而引起或相关的疾病。