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 C81H139N18O16+ 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.
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Hayakawa, Y., Hattori, Y., Kawasaki, T. et al. Efrapeptin J, a New Down-regulator of the Molecular Chaperone GRP78 from a Marine Tolypocladium sp.. J Antibiot 61, 365–371 (2008). https://doi.org/10.1038/ja.2008.51
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DOI: https://doi.org/10.1038/ja.2008.51
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