Discovery of a Plant 14-3-3 Inhibitor Possessing Isoform Selectivity and In Planta Activity.
Angew Chem Int Ed Engl
; 63(27): e202400218, 2024 07 01.
Article
em En
| MEDLINE
| ID: mdl-38658314
ABSTRACT
Synthetic modulators of plant 14-3-3s are promising chemical tools both for understanding the 14-3-3-related signaling pathways and controlling plant physiology. Herein, we describe a novel small-molecule inhibitor for 14-3-3 proteins of Arabidopsis thaliana. The inhibitor was identified from unexpected products in a stock solution in dimethyl sulfoxide (DMSO) of an in-house chemical library. Mass spectroscopy, mutant-based analyses, fluorescence polarization assays, and thermal shift assays revealed that the inhibitor covalently binds to an allosteric site of 14-3-3 with isoform selectivity. Moreover, infiltration of the inhibitor to Arabidopsis leaves suppressed the stomatal aperture. The inhibitor should provide new insight into the design of potent and isoform-selective 14-3-3 modulators.
Palavras-chave
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Arabidopsis
/
Isoformas de Proteínas
/
Proteínas 14-3-3
Idioma:
En
Revista:
Angew Chem Int Ed Engl
Ano de publicação:
2024
Tipo de documento:
Article
País de afiliação:
Japão