Furin-targeting activity-based probes with phosphonate and phosphinate esters as warheads

被引：2
|
作者：
Ji, Shanping [1 ]
Verhelst, Steven H. L. [1 ,2 ]
机构：
[1] Univ Leuven, Dept Cellular & Mol Med, Lab Chem Biol, KU Leuven, B-3000 Leuven, Belgium
[2] Leibniz Inst Analyt Sci ISAS, AG Chem Prote, D-44227 Dortmund, Germany
来源：
ORGANIC & BIOMOLECULAR CHEMISTRY | 2023年 / 21卷 / 32期
关键词：
PROPROTEIN CONVERTASE FURIN; INHIBITORS; PROTEASES; PROTEIN;
D O I：
10.1039/d3ob00948c
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
Activity-based probes (ABPs) are covalent chemical tools that are widely used to target proteases in chemical biology. Here, we report a series of novel ABPs for the serine protease furin with phosphonate and phosphinate esters as reactive electrophiles. We show that these probes covalently label furin and have nanomolar potencies, because of proposed interactions with the different recognition pockets around the active site of furin.
引用
收藏
页码：6498 / 6502
页数：5
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