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

Ourailidou, M. E., Lenoci, A., Zwergel, C., Rotili, D., Mai, A. & Dekker, F. J., 1-Feb-2017, In : Bioorganic & Medicinal Chemistry. 25, 3, p. 847-856 10 p.

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DOI

  • Maria E. Ourailidou
  • Alessia Lenoci
  • Clemens Zwergel
  • Dante Rotili
  • Antonello Mai
  • Frank J Dekker

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.

Original languageEnglish
Pages (from-to)847-856
Number of pages10
JournalBioorganic & Medicinal Chemistry
Volume25
Issue number3
Publication statusPublished - 1-Feb-2017

    Keywords

  • Lysine demethylation, Tumorigenesis, Tranylcypromine, Irreversible inhibition, Enzyme labeling, LSD1 HISTONE DEMETHYLASE, OXIDATIVE HECK REACTION, THERAPEUTIC STRATEGY, BIOLOGICAL-ACTIVITY, STRUCTURAL BASIS, HDAC INHIBITORS, BREAST-CANCER, PROTEIN, CELLS, DERIVATIVES

ID: 38064620