Inhibitors of histone demethylases

Brian Lohse; Jesper L Kristensen; Line H Kristensen; Karl Agger; Kristian Helin; Michael Gajhede; Rasmus P Clausen

doi:10.1016/j.bmc.2011.01.046

Inhibitors of histone demethylases

Brian Lohse, Jesper L Kristensen, Line H Kristensen, Karl Agger, Kristian Helin, Michael Gajhede, Rasmus P Clausen

Research output: Contribution to journal › Review › peer-review

90 Citations (Scopus)

Abstract

Methylated lysines are important epigenetic marks. The enzymes involved in demethylation have recently been discovered and found to be involved in cancer development and progression. Despite the relative recent discovery of these enzymes a number of inhibitors have already appeared. Most of the inhibitors are either previously reported inhibitors of related enzymes or compounds derived from these. Development in terms of selectivity and potency is still pertinent. Several reports on the development of functional assays have been published.

Original language	English
Journal	Bioorganic & Medicinal Chemistry
Volume	19
Issue number	12
Pages (from-to)	3625-3636
Number of pages	11
ISSN	0968-0896
DOIs	https://doi.org/10.1016/j.bmc.2011.01.046
Publication status	Published - 1 Feb 2011

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10.1016/j.bmc.2011.01.046

Cite this

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title = "Inhibitors of histone demethylases",

abstract = "Methylated lysines are important epigenetic marks. The enzymes involved in demethylation have recently been discovered and found to be involved in cancer development and progression. Despite the relative recent discovery of these enzymes a number of inhibitors have already appeared. Most of the inhibitors are either previously reported inhibitors of related enzymes or compounds derived from these. Development in terms of selectivity and potency is still pertinent. Several reports on the development of functional assays have been published.",

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T1 - Inhibitors of histone demethylases

AU - Lohse, Brian

AU - Kristensen, Jesper L

AU - Kristensen, Line H

AU - Agger, Karl

AU - Helin, Kristian

AU - Gajhede, Michael

AU - Clausen, Rasmus P

PY - 2011/2/1

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N2 - Methylated lysines are important epigenetic marks. The enzymes involved in demethylation have recently been discovered and found to be involved in cancer development and progression. Despite the relative recent discovery of these enzymes a number of inhibitors have already appeared. Most of the inhibitors are either previously reported inhibitors of related enzymes or compounds derived from these. Development in terms of selectivity and potency is still pertinent. Several reports on the development of functional assays have been published.

AB - Methylated lysines are important epigenetic marks. The enzymes involved in demethylation have recently been discovered and found to be involved in cancer development and progression. Despite the relative recent discovery of these enzymes a number of inhibitors have already appeared. Most of the inhibitors are either previously reported inhibitors of related enzymes or compounds derived from these. Development in terms of selectivity and potency is still pertinent. Several reports on the development of functional assays have been published.

U2 - 10.1016/j.bmc.2011.01.046

DO - 10.1016/j.bmc.2011.01.046

M3 - Review

C2 - 21596573

VL - 19

SP - 3625

EP - 3636

JO - Bioorganic & Medicinal Chemistry

JF - Bioorganic & Medicinal Chemistry

SN - 0968-0896

IS - 12

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