Histone lysine demethylases as targets for anticancer therapy

Jonas W Højfeldt; Karl Agger; Kristian Helin

doi:10.1038/nrd4154

Histone lysine demethylases as targets for anticancer therapy

Jonas W Højfeldt, Karl Agger, Kristian Helin

The Danish Stem Cell Center

302 Citations (Scopus)

Abstract

It has recently been demonstrated that the genes controlling the epigenetic programmes that are required for maintaining chromatin structure and cell identity include genes that drive human cancer. This observation has led to an increased awareness of chromatin-associated proteins as potentially interesting drug targets. The successful introduction of DNA methylation and histone deacetylase (HDAC) inhibitors for the treatment of specific subtypes of cancer has paved the way for the use of epigenetic therapy. Here, we highlight key biological findings demonstrating the roles of members of the histone lysine demethylase class of enzymes in the development of cancers, discuss the potential and challenges of therapeutically targeting them, and highlight emerging small-molecule inhibitors of these enzymes.

Original language	English
Journal	Nature Reviews. Drug Discovery
Volume	12
Issue number	12
Pages (from-to)	917-30
Number of pages	14
ISSN	1474-1776
DOIs	https://doi.org/10.1038/nrd4154
Publication status	Published - Dec 2013

Keywords

Animals
Antineoplastic Agents
Drug Delivery Systems
Histone Deacetylase Inhibitors
Histone Demethylases
Humans
Neoplasms

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1038/nrd4154

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title = "Histone lysine demethylases as targets for anticancer therapy",

abstract = "It has recently been demonstrated that the genes controlling the epigenetic programmes that are required for maintaining chromatin structure and cell identity include genes that drive human cancer. This observation has led to an increased awareness of chromatin-associated proteins as potentially interesting drug targets. The successful introduction of DNA methylation and histone deacetylase (HDAC) inhibitors for the treatment of specific subtypes of cancer has paved the way for the use of epigenetic therapy. Here, we highlight key biological findings demonstrating the roles of members of the histone lysine demethylase class of enzymes in the development of cancers, discuss the potential and challenges of therapeutically targeting them, and highlight emerging small-molecule inhibitors of these enzymes.",

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AU - Højfeldt, Jonas W

AU - Agger, Karl

AU - Helin, Kristian

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N2 - It has recently been demonstrated that the genes controlling the epigenetic programmes that are required for maintaining chromatin structure and cell identity include genes that drive human cancer. This observation has led to an increased awareness of chromatin-associated proteins as potentially interesting drug targets. The successful introduction of DNA methylation and histone deacetylase (HDAC) inhibitors for the treatment of specific subtypes of cancer has paved the way for the use of epigenetic therapy. Here, we highlight key biological findings demonstrating the roles of members of the histone lysine demethylase class of enzymes in the development of cancers, discuss the potential and challenges of therapeutically targeting them, and highlight emerging small-molecule inhibitors of these enzymes.

AB - It has recently been demonstrated that the genes controlling the epigenetic programmes that are required for maintaining chromatin structure and cell identity include genes that drive human cancer. This observation has led to an increased awareness of chromatin-associated proteins as potentially interesting drug targets. The successful introduction of DNA methylation and histone deacetylase (HDAC) inhibitors for the treatment of specific subtypes of cancer has paved the way for the use of epigenetic therapy. Here, we highlight key biological findings demonstrating the roles of members of the histone lysine demethylase class of enzymes in the development of cancers, discuss the potential and challenges of therapeutically targeting them, and highlight emerging small-molecule inhibitors of these enzymes.

KW - Animals

KW - Antineoplastic Agents

KW - Drug Delivery Systems

KW - Histone Deacetylase Inhibitors

KW - Histone Demethylases

KW - Humans

KW - Neoplasms

U2 - 10.1038/nrd4154

DO - 10.1038/nrd4154

M3 - Review

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SP - 917

EP - 930

JO - Nature Reviews Drug Discovery

JF - Nature Reviews Drug Discovery

IS - 12

ER -

Histone lysine demethylases as targets for anticancer therapy

Abstract

Keywords

UN SDGs

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