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Updated: Jul 10, 2025

Direct Measurement of KDM1A Target Engagement Using Chemoprobe-based Immunoassays
Published on: June 13, 2019
Lysine-specific demethylase 1 as a therapeutic cancer target: observations from preclinical study
Jessica D Johnson1, Salvador Alejo1, Sridharan Jayamohan1
1Department of Obstetrics and Gynecology, UT Health San Antonio, San Antonio, TX, USA.
Introduction:
Lysine-specific histone demethylase 1A (KDM1A/LSD1) has emerged as an important therapeutic target in various cancer types. LSD1 regulates a wide range of biological processes that influence cancer development, progression, metastasis, and therapy resistance. However, recent studies have revealed novel aspects of LSD1 biology, shedding light on its involvement in immunogenicity, antitumor immunity, and DNA damage response. These emerging findings have the potential to be leveraged in the design of effective LSD1-targeted therapies.
Areas Covered:
This paper discusses the latest developments in the field of LSD1 biology, focusing on its role in regulating immunogenicity, antitumor immunity, and DNA damage response mechanisms. The newfound understanding of these mechanisms has opened possibilities for the development of novel LSD1-targeted therapies for cancer treatment. Additionally, the paper provides an overview of LSD1 inhibitor-based combination therapies for the treatment of cancer.
Expert Opinion:
Exploiting LSD1 role in antitumor immunity and DNA damage response provides cues to not only understand the LSD1-resistant mechanisms but also rationally design new combination therapies that are more efficient and less toxic than monotherapy. The exploration of LSD1 biology and the development of LSD1-targeted therapies hold great promise for the future of cancer treatment.
Insights
Lysine-specific demethylase 1A (LSD1) is a key target in cancer therapy. Targeting LSD1 in combination therapies may improve cancer treatment efficacy and reduce toxicity by modulating antitumor immunity and DNA damage response.
Area of Science:
- Oncology
- Epigenetics
- Cancer Biology
Background:
- Lysine-specific demethylase 1A (KDM1A/LSD1) is implicated in cancer progression and therapy resistance.
- Emerging research highlights LSD1's role in immunogenicity, antitumor immunity, and DNA damage response.
Purpose of the Study:
- To review recent advancements in LSD1 biology.
- To explore LSD1's function in immune response and DNA repair.
- To discuss novel therapeutic strategies involving LSD1 inhibitors.
Main Methods:
- Literature review of recent studies on LSD1.
- Analysis of LSD1's involvement in cancer immunogenicity and DNA damage.
- Overview of LSD1 inhibitor-based combination therapies.
Main Results:
- LSD1 influences cancer development, metastasis, and resistance to therapy.
- Novel roles of LSD1 in antitumor immunity and DNA damage response identified.
- LSD1 inhibitors show potential in combination therapies.
Conclusions:
- Understanding LSD1's role in immunity and DNA damage response offers new therapeutic avenues.
- Targeting LSD1 can help overcome resistance mechanisms.
- LSD1-targeted combination therapies promise more effective and less toxic cancer treatments.

