A selective inhibitor and probe of the cellular functions of Jumonji C domain-containing histone demethylases.
Histone methylations are important chromatin marks that regulate gene expression, genomic stability, DNA repair, and genomic imprinting. Histone demethylases are the most recent family of histone-modifying enzymes discovered. Here, we report the characterization of a small-molecule inhibitor of Jumo...
| Main Authors: | , , , , , , , , , , , |
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| Format: | Journal article |
| Language: | English |
| Published: |
2011
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| _version_ | 1797101449667149824 |
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| author | Luo, X Liu, Y Kubicek, S Myllyharju, J Tumber, A Ng, S Che, K Podoll, J Heightman, T Oppermann, U Schreiber, S Wang, X |
| author_facet | Luo, X Liu, Y Kubicek, S Myllyharju, J Tumber, A Ng, S Che, K Podoll, J Heightman, T Oppermann, U Schreiber, S Wang, X |
| author_sort | Luo, X |
| collection | OXFORD |
| description | Histone methylations are important chromatin marks that regulate gene expression, genomic stability, DNA repair, and genomic imprinting. Histone demethylases are the most recent family of histone-modifying enzymes discovered. Here, we report the characterization of a small-molecule inhibitor of Jumonji C domain-containing histone demethylases. The inhibitor derives from a structure-based design and preferentially inhibits the subfamily of trimethyl lysine demethylases. Its methyl ester prodrug, methylstat, selectively inhibits Jumonji C domain-containing his-tone demethylases in cells and may be a useful small-molecule probe of chromatin and its role in epigenetics. |
| first_indexed | 2024-03-07T05:52:06Z |
| format | Journal article |
| id | oxford-uuid:e93f4054-f095-4d8e-aa65-8d20d9a2258b |
| institution | University of Oxford |
| language | English |
| last_indexed | 2024-03-07T05:52:06Z |
| publishDate | 2011 |
| record_format | dspace |
| spelling | oxford-uuid:e93f4054-f095-4d8e-aa65-8d20d9a2258b2022-03-27T10:52:50ZA selective inhibitor and probe of the cellular functions of Jumonji C domain-containing histone demethylases.Journal articlehttp://purl.org/coar/resource_type/c_dcae04bcuuid:e93f4054-f095-4d8e-aa65-8d20d9a2258bEnglishSymplectic Elements at Oxford2011Luo, XLiu, YKubicek, SMyllyharju, JTumber, ANg, SChe, KPodoll, JHeightman, TOppermann, USchreiber, SWang, XHistone methylations are important chromatin marks that regulate gene expression, genomic stability, DNA repair, and genomic imprinting. Histone demethylases are the most recent family of histone-modifying enzymes discovered. Here, we report the characterization of a small-molecule inhibitor of Jumonji C domain-containing histone demethylases. The inhibitor derives from a structure-based design and preferentially inhibits the subfamily of trimethyl lysine demethylases. Its methyl ester prodrug, methylstat, selectively inhibits Jumonji C domain-containing his-tone demethylases in cells and may be a useful small-molecule probe of chromatin and its role in epigenetics. |
| spellingShingle | Luo, X Liu, Y Kubicek, S Myllyharju, J Tumber, A Ng, S Che, K Podoll, J Heightman, T Oppermann, U Schreiber, S Wang, X A selective inhibitor and probe of the cellular functions of Jumonji C domain-containing histone demethylases. |
| title | A selective inhibitor and probe of the cellular functions of Jumonji C domain-containing histone demethylases. |
| title_full | A selective inhibitor and probe of the cellular functions of Jumonji C domain-containing histone demethylases. |
| title_fullStr | A selective inhibitor and probe of the cellular functions of Jumonji C domain-containing histone demethylases. |
| title_full_unstemmed | A selective inhibitor and probe of the cellular functions of Jumonji C domain-containing histone demethylases. |
| title_short | A selective inhibitor and probe of the cellular functions of Jumonji C domain-containing histone demethylases. |
| title_sort | selective inhibitor and probe of the cellular functions of jumonji c domain containing histone demethylases |
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