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Towards the development of activity-based probes for detection of lysine-specific demethylase-1 activity.
Ourailidou, Maria E; Lenoci, Alessia; Zwergel, Clemens; Rotili, Dante; Mai, Antonello; Dekker, Frank J.
Affiliation
  • Ourailidou ME; Department of Chemical and Pharmaceutical Biology, Groningen Research Institute of Pharmacy, University of Groningen, Antonius Deusinglaan 1, Groningen 9713 AV, The Netherlands.
  • Lenoci A; Department of Drug Chemistry and Technologies, 'Sapienza' University, P.le A. Moro 5, 00185 Rome, Italy.
  • Zwergel C; Department of Drug Chemistry and Technologies, 'Sapienza' University, P.le A. Moro 5, 00185 Rome, Italy.
  • Rotili D; Department of Drug Chemistry and Technologies, 'Sapienza' University, P.le A. Moro 5, 00185 Rome, Italy.
  • Mai A; Department of Drug Chemistry and Technologies, 'Sapienza' University, P.le A. Moro 5, 00185 Rome, Italy; Pasteur Institute, Cenci Bolognetti Foundation, 'Sapienza' University, P.le A. Moro 5, 00185 Rome, Italy. Electronic address: antonello.mai@uniroma1.it.
  • Dekker FJ; Department of Chemical and Pharmaceutical Biology, Groningen Research Institute of Pharmacy, University of Groningen, Antonius Deusinglaan 1, Groningen 9713 AV, The Netherlands. Electronic address: f.j.dekker@rug.nl.
Bioorg Med Chem ; 25(3): 847-856, 2017 02 01.
Article in En | MEDLINE | ID: mdl-27989416
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.
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Full text: 1 Database: MEDLINE Main subject: Tranylcypromine / Molecular Probes / Enzyme Inhibitors / Histone Demethylases Type of study: Diagnostic_studies Limits: Humans Language: En Year: 2017 Type: Article
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Full text: 1 Database: MEDLINE Main subject: Tranylcypromine / Molecular Probes / Enzyme Inhibitors / Histone Demethylases Type of study: Diagnostic_studies Limits: Humans Language: En Year: 2017 Type: Article