Ubiquitin-propargylamide(Ub-PA) is one of the most widely used activity-based probe to measure the activity of deubiquitinases(DUBs) and help validate DUBs targeting inhibitors. However, current synthetic route of Ub-...Ubiquitin-propargylamide(Ub-PA) is one of the most widely used activity-based probe to measure the activity of deubiquitinases(DUBs) and help validate DUBs targeting inhibitors. However, current synthetic route of Ub-PA is cumbersome. In this work, we report a novel semi-synthetic strategy to prepare Ub-PA in large-scale. Biochemical assays prove that semi-synthetic Ub-PA is an effective probe in identifying DUBs targeting inhibitors.展开更多
基金supported by the National Natural Science Foundation of China(Nos. 91753205 and 21877024 to Y. Li and No. 31640016 to Z. Mei)the Fundamental Research Funds for the Central Universities (No. PA2017GDQT0021 to Y. Li)+2 种基金the funding of National Key R&D program of China(No. 2017YFD0500400 to Z. Mei)the Fundamental Research Funds for the Central Non-profit Scientific Institution (No. Y2016JC25 to Z. Mei)the Agricultural Science and Technology Innovation Program to Z.Mei
文摘Ubiquitin-propargylamide(Ub-PA) is one of the most widely used activity-based probe to measure the activity of deubiquitinases(DUBs) and help validate DUBs targeting inhibitors. However, current synthetic route of Ub-PA is cumbersome. In this work, we report a novel semi-synthetic strategy to prepare Ub-PA in large-scale. Biochemical assays prove that semi-synthetic Ub-PA is an effective probe in identifying DUBs targeting inhibitors.
