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

83 Citationer (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.

Originalsprog	Engelsk
Tidsskrift	Bioorganic & Medicinal Chemistry
Vol/bind	19
Udgave nummer	12
Sider (fra-til)	3625-3636
Antal sider	11
ISSN	0968-0896
DOI	https://doi.org/10.1016/j.bmc.2011.01.046
Status	Udgivet - 15 jun. 2011

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10.1016/j.bmc.2011.01.046

Citationsformater

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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 - 2011/6/15

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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.

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JO - Bioorganic & Medicinal Chemistry

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Inhibitors of histone demethylases

Abstract

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