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LSD1: biologic roles and therapeutic targeting.
Alba Maiques-Diaz1, Tim Cp Somervaille1
1Leukaemia Biology Laboratory, Cancer Research UK Manchester Institute, The University of Manchester, Wilmslow Road, Manchester, M20 4BX, UK.
Epigenomics
|August 2, 2016
Summary
Lysine-specific demethylase 1 (LSD1) regulates gene expression and is a target for cancer therapy. Tranylcypromine derivative LSD1 inhibitors are being evaluated in early clinical trials for oncology applications.
Area of Science:
- Biochemistry
- Epigenetics
- Oncology
Background:
- Lysine-specific demethylase 1 (LSD1) is the first identified histone demethylase.
- LSD1 plays crucial roles in mammalian biology and is overexpressed in many human cancers.
Purpose of the Study:
- To summarize structural and biochemical knowledge of LSD1.
- To review functional and preclinical oncology studies of LSD1 inhibitors.
Main Methods:
- Structural analysis of LSD1.
- Biochemical assays to understand enzymatic activity.
- Review of preclinical cancer studies.
Main Results:
- LSD1 inhibitors, particularly tranylcypromine derivatives, show promise.
- Extensive preclinical data support clinical evaluation.
Conclusions:
- LSD1 is a key epigenetic regulator with significant therapeutic potential in oncology.
- Early phase clinical trials are investigating LSD1 inhibitors.
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