Definitions
from Wiktionary, Creative Commons Attribution/Share-Alike License.
- noun medicine A
drug that protectscells fromapoptosis
Etymologies
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Examples
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Synergistic enhancement of PSI cytotoxicity by salubrinal was largely independent of eIF2α phosphorylation since neither salubrinal at 10 µM nor the combination of salubrinal with a proteasome inhibitor blocked PP1 phosphatase activity or led to a marked increase in eIF2α phosphorylation.
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However, a recent proteomic study demonstrated that the number of proteins actually affected by salubrinal treatment appeared to be very limited
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It will be interesting therefore to find out, which phosphatase exactly is affected by salubrinal, cantharidin. and similar inhibitors.
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(A) Combined caspase 3 and 7 activities in K562 cells treated with 5 nM PSI, 10 µM salubrinal and 2 mM VPA as indicated for 18 h.
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Long K, Boyce M, Lin H, Yuan J, Ma D (2005) Structure-activity relationship studies of salubrinal lead to its active biotinylated derivative.
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Further investigations will reveal, whether salubrinal or derivatives thereoff can be included in a therapeutic strategy that is based on the induction of ER stress and maintains a strong and selective toxicity for the tumor cells on the one hand but confers protection to neuronal and other non-transformed cells on the other.
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These observations demonstrated that none of the inhibitors including salubrinal was able to activate XBP on its own. and that the combination of PSI with salubrinal or VPA was required for efficient XBP1 splicing.
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Furthermore, the observation that salubrinal also enhanced the toxic effects of thapsigargin, a bona fide ER stress inducer, excluded the possibility of inhibitor class-specific effects and instead suggested that there are intrinsic cell type specific differences in the orchestration of the PERK-eIF2α signaling cascade.
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To further characterize the effect of salubrinal on K562 cells, the cell cycle distribution of the viable cell population was examined.
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Shown are representative blots obtained from at least two independent experiments with similar results (C) K562 cells exposed to 5 nM PSI, 10 µM salubrinal and 2 mM VPA as indicated were stained with propidium iodide and analyzed by fluorescence-activated cell sorting.
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