[HTML][HTML] Structural and functional analysis of the human HDAC4 catalytic domain reveals a regulatory structural zinc-binding domain
MJ Bottomley, PL Surdo, P Di Giovine, A Cirillo… - Journal of Biological …, 2008 - ASBMB
Histone deacetylases (HDACs) regulate chromatin status and gene expression, and their
inhibition is of significant therapeutic interest. To date, no biological substrate for class IIa
HDACs has been identified, and only low activity on acetylated lysines has been
demonstrated. Here, we describe inhibitor-bound and inhibitor-free structures of the histone
deacetylase-4 catalytic domain (HDAC4cd) and of an HDAC4cd active site mutant with
enhanced enzymatic activity toward acetylated lysines. The structures presented, coupled …
inhibition is of significant therapeutic interest. To date, no biological substrate for class IIa
HDACs has been identified, and only low activity on acetylated lysines has been
demonstrated. Here, we describe inhibitor-bound and inhibitor-free structures of the histone
deacetylase-4 catalytic domain (HDAC4cd) and of an HDAC4cd active site mutant with
enhanced enzymatic activity toward acetylated lysines. The structures presented, coupled …