Therapeutic targeting of BET bromodomain and other epigenetic acetylrecognition domain–containing factors

Gold, Sarah; Shilatifard, Ali

doi:10.1016/j.gde.2024.102181

Current Opinion in Genetics & Development

2024

DOI: 10.1016/j.gde.2024.102181

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Therapeutic targeting of BET bromodomain and other epigenetic acetylrecognition domain–containing factors

Sarah Gold,

Ali Shilatifard

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2024

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Cited by 2 publications

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Editorial overview: Breaking boundaries: new frontiers in chromatin regulation for cancer therapy

Shilatifard,

Lauberth

2024

Current Opinion in Genetics & Development

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Editorial overview: Breaking boundaries: new frontiers in chromatin regulation for cancer therapy

Shilatifard,

Lauberth

2024

Current Opinion in Genetics & Development

View full text Add to dashboard Cite

Epigenetic therapies targeting histone lysine methylation: complex mechanisms and clinical challenges

Gold,

Shilatifard

2024

Journal of Clinical Investigation

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As epigenetic therapies continue to gain ground as potential treatment strategies for cancer and other diseases, compounds that target histone lysine methylation and the enzyme complexes represent a major frontier for therapeutic development. Clinically viable therapies targeting the activities of histone lysine methyltransferases (HKMT) and demethylases (HKDMs) have only recently begun to emerge following FDA approval of the EZH2 inhibitor tazemetostat in 2020 and remain limited to compounds targeting the well-studied SET domain–containing HKMTs and their opposing HKDMs. These include the H3K27 methyltransferases EZH2/EZH1, the singular H3K79 methyltransferase DOT1L, and the H3K4 methyltransferase MLL1/COMPASS as well as H3K9 and H3K36 methyltransferases. They additionally include the H3K4/9-preferential demethylase LSD1 and the H3K4-, H3K27-, and H3K36-preferential KDM5, KDM6, and KDM2 demethylase subfamilies, respectively. This Review discusses the results of recent clinical and preclinical studies relevant to all of these existing and potential therapies. It provides an update on advancements in therapeutic development, as well as more basic molecular understanding, within the past 5 years approximately. It also offers a perspective on histone lysine methylation that departs from the long-predominant “histone code” metaphor, emphasizing complex-disrupting inhibitors and proximity-based approaches rather than catalytic domain inhibitors in the outlook for future therapeutic development.

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Therapeutic targeting of BET bromodomain and other epigenetic acetylrecognition domain–containing factors

Cited by 2 publications

References 76 publications

Editorial overview: Breaking boundaries: new frontiers in chromatin regulation for cancer therapy

Editorial overview: Breaking boundaries: new frontiers in chromatin regulation for cancer therapy

Epigenetic therapies targeting histone lysine methylation: complex mechanisms and clinical challenges

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