Issue 32, 2023
From the journal:

Organic & Biomolecular Chemistry

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

Shanping Jia  and  Steven H. L. Verhelst ORCID logo *ab  

* Corresponding authors

a Laboratory of Chemical Biology, Department of Cellular and Molecular Medicine, KU Leuven – University of Leuven, 3000 Leuven, Belgium
E-mail: steven.verhelst@kuleuven.be

b AG Chemical Proteomics, Leibniz Institute for Analytical Sciences – ISAS, 44227 Dortmund, Germany

Abstract

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.

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

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Article information

DOI
https://doi.org/10.1039/D3OB00948C
Article type
Communication
Submitted
15 Jun 2023
Accepted
10 Jul 2023
First published
28 Jul 2023
This article is Open Access
Creative Commons BY-NC license

Org. Biomol. Chem., 2023,21, 6498-6502

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

S. Ji and S. H. L. Verhelst, Org. Biomol. Chem., 2023, 21, 6498 DOI: 10.1039/D3OB00948C

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