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Optimization and Anti-Cancer Properties of Fluoromethylketones as Covalent Inhibitors for Ubiquitin C-Terminal Hydrolase L1

Molecules. 2021-02; 
Aaron D Krabill, Hao Chen, Sajjad Hussain, Chad S Hewitt, Ryan D Imhoff, Christine S Muli, Chittaranjan Das, Paul J Galardy, Michael K Wendt, Daniel P Flaherty
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Gene Synthesis UCHL1, UCHL1C90A, and UCHL3 (Expressed in pET15b by GenScript) for biochemical assays were grown in LB growth medium at 37 °C to an optical density of 0.6–0.8. Get A Quote

摘要

The deubiquitinating enzyme (DUB) UCHL1 is implicated in various disease states including neurodegenerative disease and cancer. However, there is a lack of quality probe molecules to gain a better understanding on UCHL1 biology. To this end a study was carried out to fully characterize and optimize the irreversible covalent UCHL1 inhibitor VAEFMK. Structure-activity relationship studies identified modifications to improve activity versus the target and a full cellular characterization was carried out for the first time with this scaffold. The studies produced a new inhibitor, , with an IC value of 7.7 µM against UCHL1 and no observable activity versus the closest related DUB UCHL3. The molecule was also capabl... More

关键词

UCHL1 inhibitors, covalent inhibitors, deubiquitinases, fluoromethylketones