Literature DB >> 27989416

Towards the development of activity-based probes for detection of lysine-specific demethylase-1 activity.

Maria E Ourailidou1, Alessia Lenoci2, Clemens Zwergel2, Dante Rotili2, Antonello Mai3, Frank J Dekker4.   

Abstract

The implications of lysine-specific demethylase-1 (LSD1) in tumorigenesis have urged scientists to develop diagnostic tools in order to explore the function of this enzyme. In this work, we present our efforts on the development of tranylcypromine (TCP)-based functionalized probes for activity-based protein profiling (ABPP) of LSD1 activity. Biotinylated forms of selected compounds enabled dose-dependent enzyme labeling of recombinant LSD1. However, treatment with LSD1 inhibitors did not clearly reduce the LSD1 labeling efficiency thus indicating that labeling using these probes is not activity dependent. This calls for alternative strategies to develop probes for ABPP of the enzyme LSD1.
Copyright © 2016 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Enzyme labeling; Irreversible inhibition; Lysine demethylation; Tranylcypromine; Tumorigenesis

Mesh：

Substances：

Year:  2016        PMID： 27989416      PMCID： PMC5292237          DOI： 10.1016/j.bmc.2016.11.043

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN： 0968-0896            Impact factor:   3.641


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