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...
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Nature Portfolio
2020
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oai:doaj.org-article:e6e3823b97f04066b0453b2d183e0a762021-12-02T16:31:04ZA distal regulatory region of a class I human histone deacetylase10.1038/s41467-020-17610-w2041-1723https://doaj.org/article/e6e3823b97f04066b0453b2d183e0a762020-07-01T00:00:00Zhttps://doi.org/10.1038/s41467-020-17610-whttps://doaj.org/toc/2041-1723Human 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.Nicolas D. WerbeckVaibhav Kumar ShuklaMicha B. A. KunzeHavva YalincaRuth B. PritchardLucas SiemonsSomnath MondalSimon O. R. GreenwoodJohn KirkpatrickCharles M. MarsonD. Flemming HansenNature PortfolioarticleScienceQENNature Communications, Vol 11, Iss 1, Pp 1-9 (2020) |
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Science Q |
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Science Q 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 |
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. |
format |
article |
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 |
title |
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_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_sort |
distal regulatory region of a class i human histone deacetylase |
publisher |
Nature Portfolio |
publishDate |
2020 |
url |
https://doaj.org/article/e6e3823b97f04066b0453b2d183e0a76 |
work_keys_str_mv |
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