Furin-targeting activity-based probes with phosphonate and phosphinate esters as warheads.
Org Biomol Chem
; 21(32): 6498-6502, 2023 Aug 16.
Article
en En
| MEDLINE
| ID: mdl-37530461
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.
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Idioma:
En
Revista:
Org Biomol Chem
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2023
Tipo del documento:
Article
País de afiliación:
Bélgica