Phosphinate Esters as Novel Warheads for Quenched Activity-Based Probes Targeting Serine Proteases.
ACS Chem Biol
; 19(7): 1409-1415, 2024 Jul 19.
Article
em En
| MEDLINE
| ID: mdl-38913607
ABSTRACT
Quenched activity-based probes (qABP) are invaluable tools to visualize aberrant protease activity. Unfortunately, most studies so far have only focused on cysteine proteases, and only a few studies describe the synthesis and use of serine protease qABPs. We recently used phosphinate ester electrophiles as a novel type of reactive group to construct ABPs for serine proteases. Here, we report on the construction of qABPs based on the phosphinate warhead, exemplified by probes for the neutrophil serine proteases. The most successful probes show sub-stoichiometric reaction with human neutrophil elastase, efficient fluorescence quenching, and rapid unquenching of fluorescence upon reaction with target proteases.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Elastase de Leucócito
/
Ésteres
/
Serina Proteases
Limite:
Humans
Idioma:
En
Revista:
ACS Chem Biol
Ano de publicação:
2024
Tipo de documento:
Article