Compound class:
Synthetic organic
Comment: Compound IU1 is a reversible, small molecule inhibitor, discovered in a high-throughput study to identify inhibitors of the human proteasome-associated deubiquitinating enzyme USP14 [1]. Based on in vitro and in vivo results, the authors hypothesise that inhibition of USP14 may protect cells from the toxic effects of oxidised proteins produced in cells experiencing oxidative stress and that this may be a useful strategy for limiting the damaging effects of certain proteasome substrates associated with neurodegenerative diseases.
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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References |
1. Lee BH, Lee MJ, Park S, Oh DC, Elsasser S, Chen PC, Gartner C, Dimova N, Hanna J, Gygi SP et al.. (2010)
Enhancement of proteasome activity by a small-molecule inhibitor of USP14. Nature, 467 (7312): 179-84. [PMID:20829789] |