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PYR-41
PYR-41 is the first cell permeable inhibitor of ubiquitin-activating enzyme E1,irreversibly inhibits ubiquitin-activating enzyme activity.It is a pyrazone compound that showed little or no activity on E2,E3.〔(【引用サイトリンク】title=biological activity of PYR41 in selleckchem )〕
Unexpectedly, despite of ubiquitylation inhibition, PYR-41 also enhances total sumoylation in cells.
PYR41 also blocks the downstream ubiquitination and ubiquitination-dependent protein degradation or other ubiquitination-mediated cellular activities. Besides, PYR-41 inhibits degradation of p53, a tumour suppressor and also activates the transcription activity of it. PYR-41 and related pyrazones selectively kill transformed p53 expressing cells, suggesting that E1 inhibitors may be potential therapeutics in cancer. ==References==
抄文引用元・出典: フリー百科事典『 ウィキペディア(Wikipedia)』 ■ウィキペディアで「PYR-41」の詳細全文を読む
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