Chemically diverse activity-based probes with unexpected inhibitory mechanisms targeting trypsin-like serine proteases.
activity-based probe
inhibitors
irreversible inhibition
mast cells (MCs)
serine protease
Journal
Frontiers in chemistry
ISSN: 2296-2646
Titre abrégé: Front Chem
Pays: Switzerland
ID NLM: 101627988
Informations de publication
Date de publication:
2022
2022
Historique:
received:
04
11
2022
accepted:
19
12
2022
entrez:
23
1
2023
pubmed:
24
1
2023
medline:
24
1
2023
Statut:
epublish
Résumé
Activity-based probes (ABP) are molecules that bind covalently to the active form of an enzyme family, making them an attractive tool for target and biomarker identification and drug discovery. The present study describes the synthesis and biochemical characterization of novel activity-based probes targeting trypsin-like serine proteases. We developed an extensive library of activity-based probes with "clickable" affinity tags and a diaryl phosphonate warhead. A wide diversity was achieved by including natural amino acid analogs as well as basic polar residues as side chains. A detailed enzymatic characterization was performed in a panel of trypsin-like serine proteases. Their inhibitory potencies and kinetic profile were examined, and their IC
Identifiants
pubmed: 36688031
doi: 10.3389/fchem.2022.1089959
pii: 1089959
pmc: PMC9849758
doi:
Types de publication
Journal Article
Langues
eng
Pagination
1089959Informations de copyright
Copyright © 2023 Ramos-Llorca, Decraecker, Cacheux, Zeiburlina, De bruyn, Battut, Moreno-Cinos, Ceradini, Espinosa, Dietrich, Berg, De Meester, Van Der Veken, Boeckxstaens, Lambeir, Denadai-Souza and Augustyns.
Déclaration de conflit d'intérêts
The authors declare that the research was conducted in the absence of any commercial or financial relationships that could be construed as a potential conflict of interest.
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