Towards the development of activity-based probes for detection of lysine-specific demethylase-1 activity
作者： Maria E. Ourailidou , Alessia Lenoci , Clemens Zwergel , Dante Rotili , Antonello Mai
DOI: 10.1016/J.BMC.2016.11.043
关键词: Diagnostic tools 、 LYSINE-SPECIFIC DEMETHYLASE 1 、 Biotinylation 、 Biochemistry 、 Biological activity 、 Chemistry 、 Tranylcypromine 、 Function (biology) 、 Recombinant DNA 、 Enzyme
摘要: The implications of lysine-specific demethylase-1 (LSD1) in tumorigenesis have urged scientists to develop diagnostic tools order explore the function this enzyme. In work, we present our efforts on development tranylcypromine (TCP)-based functionalized probes for activity-based protein profiling (ABPP) LSD1 activity. Biotinylated forms selected compounds enabled dose-dependent enzyme labeling recombinant LSD1. However, treatment with inhibitors did not clearly reduce efficiency thus indicating that using these is activity dependent. This calls alternative strategies ABPP
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