Histone Demethylases

Dear Colleagues,

Histone demethylases are an expanding group of epigenetic regulators of chromatin structure and gene expression and play diverse roles in both embryonal development and disease. These histone demethylating enzymes antagonize the activity of histone methyl transferases by removing methyl groups from the specific lysine residue in the histones and in other non-histone target proteins, such as p53.

The first histone demethylase to be discovered was LSD1 (KDM1), an enzyme of critical importance for embryogenesis and embryonic stem cells. Recent evidence indicates that histone demethylases play important roles in tumorigenesis, epithelial-to-mesenchymal transition, invasion, metastases, and cancer stem cell phenotypes. For instance, Jumonji family histone demethylases collaborate with pathogenic H3K27M mutations in pediatric diffuse intrinsic pontine gliomas by removing the tri-methylation mark from histone H3 lysine 27, thus triggering global de-repression of genes involved in cancer stemness. Accordingly, overexpression of Jumonji family demethylases has been linked to chemotherapy and radiation resistance, and poor prognosis. Emerging are the functions of histone demethylases in neurodegenerative diseases, such as Alzheimer’s and Parkinson’s diseases.  

The aim of this Topical Collection is to highlight the diverse roles histone demethylases play in embryonic development and human diseases, such as cancer and neurodegenerative disease. We are particularly interested in experimental basic science and translational research studies focusing on pharmacological targeting histone demethylases, as well as review articles that would illuminate recent advances in our understanding of histone demethylase functions in cancer and other diseases.

Dr. Anatoly Nikolaev
Collection Editor

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