Structure, Mechanism, and Inhibition of the Zinc-Dependent …
A key feature of an HDAC inhibitor is the functional group that coordinates to the active site Zn 2+ ion. The hydroxamate group is most commonly utilized and is found in three out of four of the …
HDAC1: An Essential and Conserved Member of the Diverse Zn2
Dec 2, 2023 · Zn2+-dependent histone deacetylases (HDACs) are enzymes that regulate gene expression by removing acetyl groups from histone proteins. These enzymes are essential in …
Histone deacetylase inhibitors: molecular mechanisms of action …
Histone deacetylase (HDAC) inhibitors are a relatively new class of anti-cancer agents that play important roles in epigenetic or non-epigenetic regulation, inducing death, apoptosis, and cell …
Zinc-dependent Deacetylase (HDAC) Inhibitors with Different …
The binding of ZBG groups to zinc ion plays a decisive role in the inhibition of HDAC. Therefore, we will summarize the developed HDAC inhibitors according to different ZBG groups and …
HDAC1: An Essential and Conserved Member of the Diverse Zn2
Dec 2, 2023 · Zn<sup>2+</sup>-dependent histone deacetylases (HDACs) are enzymes that regulate gene expression by removing acetyl groups from histone proteins. These enzymes …
Discovery of HDAC Inhibitors That Lack an Active Site Zn2
Apr 26, 2012 · As a step toward mitigating this issue, here, we describe the design, synthesis, and structure–activity characterizations of cyclic α 3 β-tetrapeptide HDAC inhibitors that lack the …
Redefining the Histone Deacetylase Inhibitor Pharmacophore: …
Mar 7, 2021 · A novel series of histone deacetylase (HDAC) inhibitors lacking a zinc-binding moiety has been developed and described herein. HDAC isozyme profiling and kinetic studies …
Zinc hydrolases: the mechanisms of zinc-dependent deacetylases
Jan 1, 2005 · The HDAC zinc ligands (Asp178, His180, and Asp267) and catalytically important residues (His142, His143, Asp176, and Tyr306) are conserved in the acetylpolyamine …
Slow-Binding and Covalent HDAC Inhibition: A New Paradigm?
Oct 31, 2024 · Through Zn 2+ -dependent hydrolysis of acyl-lysine modifications, histone deacetylases (HDACs) are key regulators of disease-implicated signaling pathways and …
Histone Deacetylase 6-Selective Inhibitors and the Influence of …
Sep 9, 2018 · Metal-dependent histone deacetylases (HDACs) catalyze the hydrolysis of acetyl-L-lysine to yield acetate and free L-lysine side chains in protein substrates, and reversible lysine …
- Some results have been removed