JmjC ‐domain‐containing histone demethylases

Histone lysine demethylases (KDMs) play a pivotal role in the epigenetic modulation of higher order chromatin structure and transcriptional activity in eukaryotic cells by regulating the methylation states on histones. KDMs are involved in fundamental cellular processes such as proliferation, differ...

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Bibliografski detalji
Glavni autori: Højrup, C, Coleman, OD, Bukowski, J-P, Clausen, RP, Kawamura, A
Daljnji autori: Sippl, W
Format: Book section
Jezik:English
Izdano: Wiley 2019
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author Højrup, C
Coleman, OD
Bukowski, J-P
Clausen, RP
Kawamura, A
author2 Sippl, W
author_facet Sippl, W
Højrup, C
Coleman, OD
Bukowski, J-P
Clausen, RP
Kawamura, A
author_sort Højrup, C
collection OXFORD
description Histone lysine demethylases (KDMs) play a pivotal role in the epigenetic modulation of higher order chromatin structure and transcriptional activity in eukaryotic cells by regulating the methylation states on histones. KDMs are involved in fundamental cellular processes such as proliferation, differentiation, genome integrity, and development. This chapter provides an overview of the Jumonji C (JmjC)‐domain‐containing KDM family, with a particular focus on their therapeutic potential and the recent progress in the development of JmjC‐KDM inhibitors. It overviews the different inhibitor development strategies employed for targeting the JmjC domain of KDMs and highlights some of the subfamily‐targeted inhibitors reported to date. Due to the different domain architectures between each subfamily, as well as greater diversity between the reader domains than between their respective JmjCs, it offers better opportunities for achieving selectivity.
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spelling oxford-uuid:7f7c91c3-f4a3-47ff-bd8d-9e17fd5b49732022-03-26T21:17:19ZJmjC ‐domain‐containing histone demethylasesBook sectionhttp://purl.org/coar/resource_type/c_1843uuid:7f7c91c3-f4a3-47ff-bd8d-9e17fd5b4973EnglishSymplectic ElementsWiley2019Højrup, CColeman, ODBukowski, J-PClausen, RPKawamura, ASippl, WJung, MHistone lysine demethylases (KDMs) play a pivotal role in the epigenetic modulation of higher order chromatin structure and transcriptional activity in eukaryotic cells by regulating the methylation states on histones. KDMs are involved in fundamental cellular processes such as proliferation, differentiation, genome integrity, and development. This chapter provides an overview of the Jumonji C (JmjC)‐domain‐containing KDM family, with a particular focus on their therapeutic potential and the recent progress in the development of JmjC‐KDM inhibitors. It overviews the different inhibitor development strategies employed for targeting the JmjC domain of KDMs and highlights some of the subfamily‐targeted inhibitors reported to date. Due to the different domain architectures between each subfamily, as well as greater diversity between the reader domains than between their respective JmjCs, it offers better opportunities for achieving selectivity.
spellingShingle Højrup, C
Coleman, OD
Bukowski, J-P
Clausen, RP
Kawamura, A
JmjC ‐domain‐containing histone demethylases
title JmjC ‐domain‐containing histone demethylases
title_full JmjC ‐domain‐containing histone demethylases
title_fullStr JmjC ‐domain‐containing histone demethylases
title_full_unstemmed JmjC ‐domain‐containing histone demethylases
title_short JmjC ‐domain‐containing histone demethylases
title_sort jmjc domain containing histone demethylases
work_keys_str_mv AT højrupc jmjcdomaincontaininghistonedemethylases
AT colemanod jmjcdomaincontaininghistonedemethylases
AT bukowskijp jmjcdomaincontaininghistonedemethylases
AT clausenrp jmjcdomaincontaininghistonedemethylases
AT kawamuraa jmjcdomaincontaininghistonedemethylases