A state-of-the-art review on LSD1 and its inhibitors in breast cancer: Molecular mechanisms and therapeutic significance.

Front Pharmacol

State Key Laboratory for Managing Biotic and Chemical Threats to the Quality and Safety of Agro-products, Ningbo University, Ningbo, Zhejiang, China.

Published: September 2022

AI Article Synopsis

  • Breast cancer (BC) is the most commonly diagnosed cancer globally since 2020, and histone methylation plays a significant role in its development.
  • Lysine-specific demethylase 1 (LSD1) is a key enzyme that removes methyl groups from histones and is implicated in cancer progression, particularly in breast cancer through various mechanisms.
  • The review discusses LSD1's structure, its mechanisms of action in breast cancer, the potential of LSD1 inhibitors as a treatment, and the future challenges and opportunities in targeting LSD1 for BC therapy.

Article Abstract

Breast cancer (BC) is a kind of malignant cancer in women, and it has become the most diagnosed cancer worldwide since 2020. Histone methylation is a common biological epigenetic modification mediating varieties of physiological and pathological processes. Lysine-specific demethylase 1 (LSD1), a first identified histone demethylase, mediates the removal of methyl groups from histones H3K4me1/2 and H3K9me1/2 and plays a crucial role in varieties of cancer progression. It is also specifically amplified in breast cancer and contributes to BC tumorigenesis and drug resistance both demethylase and non-demethylase manners. This review will provide insight into the overview structure of LSD1, summarize its action mechanisms in BC, describe the therapeutic potential of LSD1 inhibitors in BC, and prospect the current opportunities and challenges of targeting LSD1 for BC therapy.

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Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC9523086PMC
http://dx.doi.org/10.3389/fphar.2022.989575DOI Listing

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