Chemoproteomic fishing identifies arzanol as a positive modulator of brain glycogen phosphorylase.
Chem Commun (Camb)
; 54(91): 12863-12866, 2018 Nov 13.
Article
em En
| MEDLINE
| ID: mdl-30375590
ABSTRACT
The interactome of arzanol was investigated by MS-based chemical proteomics, a pioneering technology for small molecule target discovery. Brain glycogen phosphorylase (bGP), a key regulator of glucose metabolism so far refractory to small molecule modulation, was identified as the main high-affinity target of arzanol. Competitive affinity-based proteomics, DARTS, molecular docking, surface plasmon resonance and in vitro biological assays provided molecular mechanistic insights into the arzanol-enzyme interaction, qualifying this positive modulator of bGP for further studies in the realm of neurodegeneration and cancer.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Floroglucinol
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Pironas
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Encéfalo
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Glicogênio Fosforilase
Limite:
Humans
Idioma:
En
Revista:
Chem Commun (Camb)
Ano de publicação:
2018
Tipo de documento:
Article