申请人:Hoffmann-La Roche Inc.
公开号:US10683329B2
公开(公告)日:2020-06-16
Provided herein are peptides having dual-site BACE1 inhibitory activity, useful for the treatment of, for example Alzheimer's disease and diabetes. One such peptide is a dual-site BACE1 inhibitor, or a pharmaceutically acceptable salt thereof, binding to both an enzymatic active site and an catalytic domain of the BACE enzyme, and an exosite inhibitory part is connected to an active-site inhibitory part of the dual site BACE1 inhibitor by a linker.
本文提供的多肽具有双位点 BACE1 抑制活性,可用于治疗阿尔茨海默病和糖尿病等疾病。其中一种多肽是双位点 BACE1 抑制剂或其药学上可接受的盐,可与 BACE 酶的酶活性位点和催化结构域结合,外抑制部分通过连接子与双位点 BACE1 抑制剂的活性位点抑制部分连接。