Plant growth regulator daminozide is a selective inhibitor of human KDM2/7 histone demethylases.
The JmjC oxygenases catalyze the N-demethylation of N(ε)-methyl lysine residues in histones and are current therapeutic targets. A set of human 2-oxoglutarate analogues were screened using a unified assay platform for JmjC demethylases and related oxygenases. Results led to the finding that daminozi...
| Main Authors: | , , , , , , , , , , , , , , , , , , , , , , , , |
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| Format: | Journal article |
| Language: | English |
| Published: |
2012
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| _version_ | 1797093912819531776 |
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| author | Rose, N Woon, E Tumber, A Walport, L Chowdhury, R Li, X King, O Lejeune, C Ng, S Krojer, T Chan, M Rydzik, A Hopkinson, R Che, K Daniel, M Strain-Damerell, C Gileadi, C Kochan, G Leung, I Dunford, J Yeoh, K Ratcliffe, P Burgess-Brown, N von Delft, F Muller, S |
| author_facet | Rose, N Woon, E Tumber, A Walport, L Chowdhury, R Li, X King, O Lejeune, C Ng, S Krojer, T Chan, M Rydzik, A Hopkinson, R Che, K Daniel, M Strain-Damerell, C Gileadi, C Kochan, G Leung, I Dunford, J Yeoh, K Ratcliffe, P Burgess-Brown, N von Delft, F Muller, S |
| author_sort | Rose, N |
| collection | OXFORD |
| description | The JmjC oxygenases catalyze the N-demethylation of N(ε)-methyl lysine residues in histones and are current therapeutic targets. A set of human 2-oxoglutarate analogues were screened using a unified assay platform for JmjC demethylases and related oxygenases. Results led to the finding that daminozide (N-(dimethylamino)succinamic acid, 160 Da), a plant growth regulator, selectively inhibits the KDM2/7 JmjC subfamily. Kinetic and crystallographic studies reveal that daminozide chelates the active site metal via its hydrazide carbonyl and dimethylamino groups. |
| first_indexed | 2024-03-07T04:06:55Z |
| format | Journal article |
| id | oxford-uuid:c67ca6f0-9687-4806-8a9d-18ad921b832a |
| institution | University of Oxford |
| language | English |
| last_indexed | 2024-03-07T04:06:55Z |
| publishDate | 2012 |
| record_format | dspace |
| spelling | oxford-uuid:c67ca6f0-9687-4806-8a9d-18ad921b832a2022-03-27T06:38:30ZPlant growth regulator daminozide is a selective inhibitor of human KDM2/7 histone demethylases.Journal articlehttp://purl.org/coar/resource_type/c_dcae04bcuuid:c67ca6f0-9687-4806-8a9d-18ad921b832aEnglishSymplectic Elements at Oxford2012Rose, NWoon, ETumber, AWalport, LChowdhury, RLi, XKing, OLejeune, CNg, SKrojer, TChan, MRydzik, AHopkinson, RChe, KDaniel, MStrain-Damerell, CGileadi, CKochan, GLeung, IDunford, JYeoh, KRatcliffe, PBurgess-Brown, Nvon Delft, FMuller, SThe JmjC oxygenases catalyze the N-demethylation of N(ε)-methyl lysine residues in histones and are current therapeutic targets. A set of human 2-oxoglutarate analogues were screened using a unified assay platform for JmjC demethylases and related oxygenases. Results led to the finding that daminozide (N-(dimethylamino)succinamic acid, 160 Da), a plant growth regulator, selectively inhibits the KDM2/7 JmjC subfamily. Kinetic and crystallographic studies reveal that daminozide chelates the active site metal via its hydrazide carbonyl and dimethylamino groups. |
| spellingShingle | Rose, N Woon, E Tumber, A Walport, L Chowdhury, R Li, X King, O Lejeune, C Ng, S Krojer, T Chan, M Rydzik, A Hopkinson, R Che, K Daniel, M Strain-Damerell, C Gileadi, C Kochan, G Leung, I Dunford, J Yeoh, K Ratcliffe, P Burgess-Brown, N von Delft, F Muller, S Plant growth regulator daminozide is a selective inhibitor of human KDM2/7 histone demethylases. |
| title | Plant growth regulator daminozide is a selective inhibitor of human KDM2/7 histone demethylases. |
| title_full | Plant growth regulator daminozide is a selective inhibitor of human KDM2/7 histone demethylases. |
| title_fullStr | Plant growth regulator daminozide is a selective inhibitor of human KDM2/7 histone demethylases. |
| title_full_unstemmed | Plant growth regulator daminozide is a selective inhibitor of human KDM2/7 histone demethylases. |
| title_short | Plant growth regulator daminozide is a selective inhibitor of human KDM2/7 histone demethylases. |
| title_sort | plant growth regulator daminozide is a selective inhibitor of human kdm2 7 histone demethylases |
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