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LSD1 inhibition: a therapeutic strategy in cancer?

James T Lynch1, William J Harris, Tim C P Somervaille

  • 1The University of Manchester, Paterson Institute for Cancer Research, Cancer Research UK Leukaemia Biology Laboratory, Manchester, M20 4BX, UK.

Expert Opinion on Therapeutic Targets
|September 11, 2012
PubMed
Abstract

Insights

Histone demethylase LSD1 (also known as KDM1A) inhibitors show promise as cancer therapeutics. Further research is needed to clarify dosing and combinations for acute myeloid leukemia and other cancers.

Area of Science:

  • Epigenetics
  • Enzymology
  • Cancer Biology

Background:

  • Epigenetic dysfunction is increasingly recognized as a driver of cancer.
  • Enzymes regulating chromatin structure and function are emerging as potential therapeutic targets.
  • Lysine-specific demethylase 1 (LSD1) is a key histone demethylase and a candidate for targeted cancer therapy.

Purpose of the Study:

  • To review the literature on LSD1, including its structure, function, and role in cancer.
  • To discuss the development and therapeutic potential of LSD1 inhibitors.

Main Methods:

  • Comprehensive literature search of PubMed for studies on LSD1 (KDM1A).
  • Analysis of LSD1's structure, enzymatic activity, and role in chromatin complexes.
  • Review of LSD1's function in normal and malignant tissues.
  • Examination of pharmacological inhibitors and their therapeutic applications.

Main Results:

  • LSD1 plays critical roles in chromatin regulation and is implicated in various cancers.
  • Novel, potent LSD1 inhibitors have been developed, showing promising pre-clinical activity.
  • Encouraging pre-clinical data exists for LSD1 inhibitors in acute myeloid leukemia.

Conclusions:

  • LSD1 inhibitors demonstrate therapeutic potential, particularly in acute myeloid leukemia.
  • Optimal dosing and combination strategies for LSD1 inhibitors require further investigation.
  • Development of potent and selective LSD1 inhibitors is crucial for exploring indications in other hematological malignancies and solid tumors.

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