Efrapeptin J, a new down-regulator of the molecular chaperone GRP78 from a marine Tolypocladium sp.
J Antibiot (Tokyo)
; 61(6): 365-71, 2008 Jun.
Article
em En
| MEDLINE
| ID: mdl-18667784
ABSTRACT
A new down-regulator of the molecular chaperone GRP78, efrapeptin J, was isolated from a marine fungus, Tolypocladium sp. AMB18. The molecular formula of efrapeptin J was established as C(81)H(139)N(18)O(16)(+) by high-resolution FAB-MS. The structure was elucidated to be a linear pentadecapeptide containing a hexahydropyrrolo[1,2-a]pyrimidinium moiety by NMR and MS analyses. Efrapeptins F, G and J dose-dependently inhibited 2-deoxyglucose-induced luciferase expression in HT1080 human fibrosarcoma cells transfected with a luciferase reporter plasmid containing the GRP78 promoter. Efrapeptin J also inhibited the protein expression of GRP78 in HT1080 cells and MKN-74 human gastric cancer cells. Efrapeptin J induced cell death in HT1080 cells under endoplasmic reticulum stress.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Peptídeos
/
Proteínas Fúngicas
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Chaperonas Moleculares
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Proteínas de Choque Térmico
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Hypocreales
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Antineoplásicos
Limite:
Humans
Idioma:
En
Ano de publicação:
2008
Tipo de documento:
Article