A distal regulatory region of a class I human histone deacetylase
Human Histone Deacetylases (HDACs) regulate gene expression and are important drug targets. Here, the authors combine NMR measurements, enzymatic assays and molecular dynamics simulations and show that HDAC8 samples a catalytically active and an inactive state and further demonstrate that mutations...
| Main Authors: | , , , , , , , , , , |
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| Format: | Article |
| Language: | English |
| Published: |
Nature Portfolio
2020-07-01
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| Series: | Nature Communications |
| Online Access: | https://doi.org/10.1038/s41467-020-17610-w |
| _version_ | 1818430408434384896 |
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| author | Nicolas D. Werbeck Vaibhav Kumar Shukla Micha B. A. Kunze Havva Yalinca Ruth B. Pritchard Lucas Siemons Somnath Mondal Simon O. R. Greenwood John Kirkpatrick Charles M. Marson D. Flemming Hansen |
| author_facet | Nicolas D. Werbeck Vaibhav Kumar Shukla Micha B. A. Kunze Havva Yalinca Ruth B. Pritchard Lucas Siemons Somnath Mondal Simon O. R. Greenwood John Kirkpatrick Charles M. Marson D. Flemming Hansen |
| author_sort | Nicolas D. Werbeck |
| collection | DOAJ |
| description | Human Histone Deacetylases (HDACs) regulate gene expression and are important drug targets. Here, the authors combine NMR measurements, enzymatic assays and molecular dynamics simulations and show that HDAC8 samples a catalytically active and an inactive state and further demonstrate that mutations and ligand binding alter the populations of the two states, which is of interest for inhibitor design. |
| first_indexed | 2024-12-14T15:32:56Z |
| format | Article |
| id | doaj.art-e6e3823b97f04066b0453b2d183e0a76 |
| institution | Directory Open Access Journal |
| issn | 2041-1723 |
| language | English |
| last_indexed | 2024-12-14T15:32:56Z |
| publishDate | 2020-07-01 |
| publisher | Nature Portfolio |
| record_format | Article |
| series | Nature Communications |
| spelling | doaj.art-e6e3823b97f04066b0453b2d183e0a762022-12-21T22:55:49ZengNature PortfolioNature Communications2041-17232020-07-011111910.1038/s41467-020-17610-wA distal regulatory region of a class I human histone deacetylaseNicolas D. Werbeck0Vaibhav Kumar Shukla1Micha B. A. Kunze2Havva Yalinca3Ruth B. Pritchard4Lucas Siemons5Somnath Mondal6Simon O. R. Greenwood7John Kirkpatrick8Charles M. Marson9D. Flemming Hansen10Institute of Structural and Molecular Biology, Division of Biosciences, University College LondonInstitute of Structural and Molecular Biology, Division of Biosciences, University College LondonInstitute of Structural and Molecular Biology, Division of Biosciences, University College LondonInstitute of Structural and Molecular Biology, Division of Biosciences, University College LondonInstitute of Structural and Molecular Biology, Division of Biosciences, University College LondonInstitute of Structural and Molecular Biology, Division of Biosciences, University College LondonInstitute of Structural and Molecular Biology, Division of Biosciences, University College LondonInstitute of Structural and Molecular Biology, Division of Biosciences, University College LondonInstitute of Structural and Molecular Biology, Division of Biosciences, University College LondonDepartment of Chemistry, University College LondonInstitute of Structural and Molecular Biology, Division of Biosciences, University College LondonHuman Histone Deacetylases (HDACs) regulate gene expression and are important drug targets. Here, the authors combine NMR measurements, enzymatic assays and molecular dynamics simulations and show that HDAC8 samples a catalytically active and an inactive state and further demonstrate that mutations and ligand binding alter the populations of the two states, which is of interest for inhibitor design.https://doi.org/10.1038/s41467-020-17610-w |
| spellingShingle | Nicolas D. Werbeck Vaibhav Kumar Shukla Micha B. A. Kunze Havva Yalinca Ruth B. Pritchard Lucas Siemons Somnath Mondal Simon O. R. Greenwood John Kirkpatrick Charles M. Marson D. Flemming Hansen A distal regulatory region of a class I human histone deacetylase Nature Communications |
| title | A distal regulatory region of a class I human histone deacetylase |
| title_full | A distal regulatory region of a class I human histone deacetylase |
| title_fullStr | A distal regulatory region of a class I human histone deacetylase |
| title_full_unstemmed | A distal regulatory region of a class I human histone deacetylase |
| title_short | A distal regulatory region of a class I human histone deacetylase |
| title_sort | distal regulatory region of a class i human histone deacetylase |
| url | https://doi.org/10.1038/s41467-020-17610-w |
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