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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Bibliographic Details
Main Authors: 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
Format: Article
Language:English
Published: Nature Portfolio 2020-07-01
Series:Nature Communications
Online Access:https://doi.org/10.1038/s41467-020-17610-w
Description
Summary: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.
ISSN:2041-1723