ArticleBioorganic & medicinal chemistry2017
Towards the development of activity-based probes for detection of lysine-specific demethylase-1 activity.
Article in Bioorganic & medicinal chemistry, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.
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Who cites it
7 citing papers in PubMed, 12 citations in OpenAlex.
- Tranylcypromine-Based LSD1 Inhibitors as Useful Agents to Reduce Viability ofACS infectious diseases · 2025Article
- Carborane-Containing Hydroxamate MMP Ligands for the Treatment of Tumors Using Boron Neutron Capture Therapy (BNCT): Efficacy without Tumor Cell Entry.International journal of molecular sciences · 2023Article
- Chemical modulation ofWellcome open research · 2023Article
- Activity-Based Protein Profiling (ABPP) of Oxidoreductases.Chembiochem : a European journal of chemical biology · 2021Review
- Pharmacological inhibition of lysine-specific demethylase 1 (LSD1) induces global transcriptional deregulation and ultrastructural alterations that impair viability in Schistosoma mansoni.PLoS neglected tropical diseases · 2020Article
- Epigenetic polypharmacology: A new frontier for epi-drug discovery.Medicinal research reviews · 2020Review
- Chemoprobe-based assays of histone lysine demethylase 1A target occupation enableThe Journal of biological chemistry · 2019Article
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Authors and funding
6 authors at 3 institutions in 2 countries.
Funding
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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Registered trials
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