Prominent role of histone lysine demethylases in cancer epigenetics and therapy

Avilala Janardhan, Chandrasekhar Kathera, Amrutha Darsi, Wajid Ali, Lingfeng He, Yanhua Yang, Libo Luo _ and Zhigang Guo

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Oncotarget. 2018; 9:34429-34448. https://doi.org/10.18632/oncotarget.24319

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Avilala Janardhan1,2, Chandrasekhar Kathera2, Amrutha Darsi2, Wajid Ali2, Lingfeng He2, Yanhua Yang1, Libo Luo1 and Zhigang Guo2

1The No. 7 People’s Hospital of Changzhou, Changzhou, China

2Jiangsu Key Laboratory for Molecular and Medical Biotechnology, College of Life Sciences, Nanjing Normal University, Nanjing, China

Correspondence to:

Libo Luo, email: [email protected]

Zhigang Guo, email: [email protected]

Keywords: epigenetics; histone modifications; protein methylation; lysine specific demethylases; therapeutics

Received: November 11, 2017     Accepted: December 04, 2017      Epub: January 25, 2018     Published: September 28, 2018


Protein methylation has an important role in the regulation of chromatin, gene expression and regulation. The protein methyl transferases are genetically altered in various human cancers. The enzymes that remove histone methylation have led to increased awareness of protein interactions as potential drug targets. Specifically, Lysine Specific Demethylases (LSD) removes methylated histone H3 lysine 4 (H3K4) and H3 lysine 9 (H3K9) through formaldehyde-generating oxidation. It has been reported that LSD1 and its downstream targets are involved in tumor-cell growth and metastasis. Functional studies of LSD1 indicate that it regulates activation and inhibition of gene transcription in the nucleus. Here we made a discussion about the summary of histone lysine demethylase and their functions in various human cancers.

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