Alkyne derivatives of isocoumarins as clickable activity-based probes for serine proteases

U Haedke, M Götz, P Baer, SHL Verhelst

文献索引：Haedke, Ute; Goetz, Markus; Baer, Philipp; Verhelst, Steven H.L. Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 2 p. 633 - 640

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被引用次数: 24

摘要

Activity-based probes (ABPs) have found increasing use in functional proteomics studies. Recently, ABPs that can be employed in combination with click chemistry gained particular attention due to their flexible application in vitro and in vivo. Moreover, there is a continuous need for new ABPs that target small subsets of enzymes. We here report novel clickable ABPs based on the 4-chloro-isocoumarin (IC) electrophile, a mechanism-based inhibitor ...