Histone demethylases in chromatin biology and beyond

Dimitrova, Emilia; Turberfield, Anne H.

doi:10.15252/embr.201541113

Cited by 177 publications

(151 citation statements)

References 241 publications

(325 reference statements)

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“…In vitro systems have provided evidence of the importance of KDM6 and its demethylase activity in establishing gene expression programs specifying lineage commitment (46). However, its in vivo roles, in particular, the specific contribution of the enzymatic activity, are less clear and possibly more nuanced.…”

Section: Discussionmentioning

confidence: 99%

Histone Demethylase KDM6A Controls the Mammary Luminal Lineage through Enzyme-Independent Mechanisms

Yoo

Kang

et al. 2016

Molecular and Cellular Biology

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Section: Discussionmentioning

confidence: 99%

Histone Demethylase KDM6A Controls the Mammary Luminal Lineage through Enzyme-Independent Mechanisms

Yoo

Kang

et al. 2016

Molecular and Cellular Biology

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“…There are two classes of evolutionary conserved family of histone demethylases, the LSD and the Jumonji C (JmjC)-domain containing proteins (reviewed in Dimitrova et al, 2015). LSD1, also known as KDM1A, was the first histone demethylase enzyme to be identified (Shi et al, 2004).…”

Section: Chromatin Dynamics Driven By Metabolitesmentioning

confidence: 99%

Interplay between Metabolism and Epigenetics: A Nuclear Adaptation to Environmental Changes

2016

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The physiological identity of every cell is maintained by highly specific transcriptional networks that establish a coherent molecular program that is in-tune with nutritional conditions. The regulation of cell-specific transcriptional networks is accomplished by an epigenetic program via chromatin modifying enzymes, whose activity is directly dependent on metabolites such as acetyl-CoA, S-adenosylmethionine and NAD+ among others. Therefore, these nuclear activities are directly influenced by the nutritional status of the cell. In addition to nutritional availability, this highly collaborative program between epigenetic dynamics and metabolism is further interconnected with other environmental cues provided by the day-night cycles imposed by circadian rhythms. Herein, we review molecular pathways and their metabolites associated with epigenetic adaptations modulated by histone- and DNA-modifying enzymes and their responsiveness to the environment in the context of health and disease.

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“…KDM6B has been shown to bind PcG target genes regulating their H3K27me3 levels and transcriptional activity 67 . The inhibitor of KDM6, GSK-J4, has accordingly shown potential in rheumatoid arthritis (RA) reducing production of the pro-inflammatory cytokine TNF-α from macrophages derived from RA patients 68 .…”

Section: Inflammationmentioning

confidence: 99%

Chemical probes targeting epigenetic proteins: Applications beyond oncology

Ackloo

Brown

Müller³

2017

Epigenetics

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Epigenetic chemical probes are potent, cell-active, small molecule inhibitors or antagonists of specific domains in a protein; they have been indispensable for studying bromodomains and protein methyltransferases. The Structural Genomics Consortium (SGC), comprising scientists from academic and pharmaceutical laboratories, has generated most of the current epigenetic chemical probes. Moreover, the SGC has shared about 4 thousand aliquots of these probes, which have been used primarily for phenotypic profiling or to validate targets in cell lines or primary patient samples cultured in vitro. Epigenetic chemical probes have been critical tools in oncology research and have uncovered mechanistic insights into well-established targets, as well as identify new therapeutic starting points. Indeed, the literature primarily links epigenetic proteins to oncology, but applications in inflammation, viral, metabolic and neurodegenerative diseases are now being reported. We summarize the literature of these emerging applications and provide examples where existing probes might be used.

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Histone demethylases in chromatin biology and beyond

Cited by 177 publications

References 241 publications

Histone Demethylase KDM6A Controls the Mammary Luminal Lineage through Enzyme-Independent Mechanisms

Histone Demethylase KDM6A Controls the Mammary Luminal Lineage through Enzyme-Independent Mechanisms

Interplay between Metabolism and Epigenetics: A Nuclear Adaptation to Environmental Changes

Chemical probes targeting epigenetic proteins: Applications beyond oncology

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