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

DanStem

302 Citationer (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.

Originalsprog	Engelsk
Tidsskrift	Nature Reviews. Drug Discovery
Vol/bind	12
Udgave nummer	12
Sider (fra-til)	917-30
Antal sider	14
ISSN	1474-1776
DOI	https://doi.org/10.1038/nrd4154
Status	Udgivet - dec. 2013

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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.",

keywords = "Animals, Antineoplastic Agents, Drug Delivery Systems, Histone Deacetylase Inhibitors, Histone Demethylases, Humans, Neoplasms",

author = "H{\o}jfeldt, {Jonas W} and Karl Agger and Kristian Helin",

year = "2013",

month = dec,

doi = "10.1038/nrd4154",

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T1 - Histone lysine demethylases as targets for anticancer therapy

AU - Højfeldt, Jonas W

AU - Agger, Karl

AU - Helin, Kristian

PY - 2013/12

Y1 - 2013/12

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

C2 - 24232376

SN - 1474-1776

VL - 12

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

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