Related Experiment Video

Updated: Jan 2, 2026

Direct Measurement of KDM1A Target Engagement Using Chemoprobe-based Immunoassays
11:17

Direct Measurement of KDM1A Target Engagement Using Chemoprobe-based Immunoassays

Published on: June 13, 2019

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LSD1/KDM1A inhibitors in clinical trials: advances and prospects

Yuan Fang1, Guochao Liao2, Bin Yu3,4

  • 1Joint Laboratory for Translational Cancer Research of Chinese Medicine of the Ministry of Education of the People's Republic of China, International Institute for Translational Chinese Medicine, Guangzhou University of Chinese Medicine, Guangzhou, 510006, Guangdong, China.

Journal of Hematology & Oncology
|December 6, 2019
PubMed

Insights

Targeting the histone demethylase LSD1 offers a new cancer treatment strategy. Several LSD1 inhibitors are in clinical trials for cancers like small cell lung cancer and acute myeloid leukemia.

Area of Science:

  • Oncology
  • Epigenetics
  • Pharmacology

Background:

  • Lysine-specific demethylase 1 (LSD1) is crucial in cancer development.
  • Targeting LSD1 is a promising therapeutic strategy for various cancers.

Purpose of the Study:

  • To provide a comprehensive review of LSD1 inhibitors in clinical trials.
  • To analyze their molecular mechanisms, clinical efficacy, and safety profiles.

Main Methods:

  • Literature review of published studies on LSD1 inhibitors.
  • Analysis of data from ongoing clinical trials.

Main Results:

  • Several LSD1 inhibitors (e.g., TCP, ORY-1001, GSK-2879552) are in clinical assessment.
  • These inhibitors show potential in treating small cell lung cancer (SCLC) and acute myeloid leukemia (AML).

Conclusions:

  • LSD1 inhibitors represent a developing class of anti-cancer drugs.
  • Further research into their efficacy, safety, and pharmacokinetic profiles is warranted.
Keywords:
Cancer therapyEpigeneticsHistone demethylaseLSD1 inhibitors

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