scholarly journals Histone Deacetylase 8: Characterization of Physiological Divalent Metal Catalysis

2016 ◽  
Vol 120 (26) ◽  
pp. 5884-5895 ◽  
Author(s):  
Michael R. Nechay ◽  
Nathan M. Gallup ◽  
Amanda Morgenstern ◽  
Quentin A. Smith ◽  
Mark E. Eberhart ◽  
...  
Keyword(s):  
Histone Deacetylase ◽  
Divalent Metal ◽  
Metal Catalysis ◽  
Histone Deacetylase 8

scholarly journals Characterization of Histone Deacetylase 8 (HDAC8) Selective Inhibition Reveals Specific Active Site Structural and Functional Determinants

2018 ◽  
Vol 61 (22) ◽  
pp. 10000-10016 ◽  
Author(s):  
Martin Marek ◽  
Tajith B. Shaik ◽  
Tino Heimburg ◽  
Alokta Chakrabarti ◽  
Julien Lancelot ◽  
...  
Keyword(s):  
Histone Deacetylase ◽  
Active Site ◽  
Selective Inhibition ◽  
Histone Deacetylase 8

Screening and Phenotypical Characterization of Schistosoma mansoni Histone Deacetylase 8 (SmHDAC8) Inhibitors as Multistage Antischistosomal Agents

2019 ◽  
Vol 6 (1) ◽  
pp. 100-113 ◽  
Author(s):  
Fulvio Saccoccia ◽  
Margherita Brindisi ◽  
Roberto Gimmelli ◽  
Nicola Relitti ◽  
Alessandra Guidi ◽  
...  
Keyword(s):  
Schistosoma Mansoni ◽  
Histone Deacetylase ◽  
Histone Deacetylase 8

Cloning and characterization of human histone deacetylase 8

FEBS Letters ◽  
2000 ◽  
Vol 478 (1-2) ◽  
pp. 77-83 ◽  
Author(s):  
Ilse Van den Wyngaert ◽  
Winfred de Vries ◽  
Andreas Kremer ◽  
Jean-Marc Neefs ◽  
Peter Verhasselt ◽  
...  
Keyword(s):  
Histone Deacetylase ◽  
Histone Deacetylase 8

scholarly journals Kinetic Characterization of Human Histone Deacetylase 8 With Medium-Chain Fatty Acyl Lysine

2021 ◽  
Vol 14 ◽  
pp. 251686572110656
Author(s):  
Harrison Yoo ◽  
Gregory A Polsinelli
Keyword(s):  
Histone Deacetylase ◽  
Histone Deacetylases ◽  
Histone Deacetylase Inhibitors ◽  
Decanoic Acid ◽  
Fatty Acyl ◽  
Peptide Substrate ◽  
Medium Chain ◽  
Histone Deacetylase 8 ◽  
Lysine Residues

Histone deacetylases (HDACs) catalyze the removal of Ɛ-acetyl-lysine residues of histones via hydrolysis. Removal of acetyl groups results in condensation of chromatin structure and alteration of gene expression by repression. HDACs are considered targets for the treatment of cancer due to their role in regulating transcription. HDAC8 inhibition may be an important anti-proliferative factor for histone deacetylase inhibitors on cancer cells and may give rise to the progression of apoptosis. HDAC8 activity was analyzed with various peptides where the target lysine is modified with medium-chain fatty acyl group. Kinetic data were determined for each p53 peptide substrate. The results suggest that there was HDAC8 deacetylase activity on peptide substrate as well as deacylase activity with acylated peptide substrate variants. HDAC8 inhibition by hexanoic and decanoic acid was also examined. The Ki for hexanoic and decanoic acid were determined to be 2.35 ± 0.341 and 4.48 ± 0.221 mM, respectively.

Structure-Based Design and Biological Characterization of Selective Histone Deacetylase 8 (HDAC8) Inhibitors with Anti-Neuroblastoma Activity

2017 ◽  
Vol 60 (24) ◽  
pp. 10188-10204 ◽  
Author(s):  
Tino Heimburg ◽  
Fiona R. Kolbinger ◽  
Patrik Zeyen ◽  
Ehab Ghazy ◽  
Daniel Herp ◽  
...  
Keyword(s):  
Histone Deacetylase ◽  
Biological Characterization ◽  
Histone Deacetylase 8 ◽  
Hdac8 Inhibitors

Rapid Discovery of Highly Potent and Selective Inhibitors of Histone Deacetylase 8 Using Click Chemistry to Generate Candidate Libraries

2012 ◽  
Vol 55 (22) ◽  
pp. 9562-9575 ◽  
Author(s):  
Takayoshi Suzuki ◽  
Yosuke Ota ◽  
Masaki Ri ◽  
Masashige Bando ◽  
Aogu Gotoh ◽  
...  
Keyword(s):  
Click Chemistry ◽  
Histone Deacetylase ◽  
Selective Inhibitors ◽  
Histone Deacetylase 8

scholarly journals The inhibition of histone deacetylase 8 suppresses proliferation and inhibits apoptosis in gastric adenocarcinoma

2015 ◽  
Vol 47 (5) ◽  
pp. 1819-1828 ◽  
Author(s):  
SHIYUAN SONG ◽  
YING WANG ◽  
PO XU ◽  
RUINA YANG ◽  
ZHIKUN MA ◽  
...  
Keyword(s):  
Histone Deacetylase ◽  
Gastric Adenocarcinoma ◽  
Histone Deacetylase 8
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