Histone demethylases (HDMs) are the most recently discovered class of histone-modifying enzymes. These often display tissue-specific expression and play critical roles in a wide range of cellular processes, including gene expression, meiosis, and embryonic stem cell self-renewal, as well as disease processes, such as those leading to the development of cancer and mental retardation. However, many important questions remain elusive in this field, such as the cellular functions, substrate specificity, and �druggability� of HDMs. We have designed, synthesized, and characterized a series of highly selective probes to address these questions.

Histone demethylases: A chemist's perspective

246th National Meeting (2013)

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