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Relative and absolute configuration of versipelostatin, a down-regulator of molecular chaperone GRP78 expression.
[structure: see text] Versipelostatin is the first compound which specifically inhibits the expression of GRP78 and the resultant robust cell death under stress conditions, in contrast to the weak
Novel GRP78 Molecular Chaperone Expression Down-regulators JBIR-04 and -05 Isolated from Streptomyces violaceoniger
JBIR-04 and -05 inhibited the expression of GRP78 induced by 2-deoxyglucose in human fibrosarcoma HT1080 cells, but their activities were highly reduced compared with those of 3 and SW-163A.
A Novel Versipelostatin Analogue, Versipelostatin F Isolated from Streptomyces versipellis 4083-SVS6
A novel versipelostatin F (2) was isolated from Streptomyces versipellis 4083-SVS6 and inhibited the expression of GRP78 induced by 2-deoxyglucose with an IC50 value of 0.3 μM, which is 10-times more potent compared with that of 1.5 μM.
Efficient synthesis of the deoxysugar part of versipelostatin by direct and stereoselective glycosylation and revision of the structure of the trisaccharide unit.
Comparison of the synthetic and natural VST products using NMR indicates that versipelostatin has a beta-D-digitoxose-(1,4)-alpha-L-oleandrose-(1-4)-beta- D- digitoxose trisaccharide, and results of a biological assay indicate that the deoxyoligosaccharides unit of the Synthetic glycoside was important for biological activity of the compound.
Prunustatin A, a Novel GRP78 Molecular Chaperone Down-regulator Isolated from Streptomyces violaceoniger
Punustatin A inhibited the expression of GRP78 induced by 2-deoxyglucose in human fibrosarcoma HT1080 cells accompanied by global cell death without showing cytotoxicity under normal nutrient condition.
New glycosylated derivatives of versipelostatin, the GRP78/Bip molecular chaperone down-regulator, from Streptomyces versipellis 4083-SVS6.
Results suggest that the alpha-L-oleandropyranosyl (1-->4)-beta-D-digitoxopyranosol residue in the sugar moiety may play an important role in down-regulating GRP78 expression induced by 2-deoxyglucose.
A Novel Antimycin-like Compound, JBIR-06, from Streptomyces sp. ML55
A novel compound of antimycin family, JBIR-06 (1), was isolated from Streptomyces sp. ML55. The structure of 1 was established as a twelve-membered macrocyclic skeleton with a