scholarly journals Use of the Nitrile Oxide Cycloaddition (NOC) Reaction for Molecular Probe Generation: A New Class of Enzyme Selective Histone Deacetylase Inhibitors (HDACIs) Showing Picomolar Activity at HDAC6

2008 ◽  
Vol 51 (15) ◽  
pp. 4370-4373 ◽  
Author(s):  
Alan P. Kozikowski ◽  
Subhasish Tapadar ◽  
Doris N. Luchini ◽  
Ki Hwan Kim ◽  
Daniel D. Billadeau
Keyword(s):  
Histone Deacetylase ◽  
Histone Deacetylase Inhibitors ◽  
Nitrile Oxide ◽  
Molecular Probe ◽  
New Class

scholarly journals Aryl butenoic acid derivatives as a new class of histone deacetylase inhibitors: synthesis, in vitro evaluation, and molecular docking studies

2014 ◽  
Vol 38 ◽  
pp. 338-344 ◽  
Author(s):  
Peruze AYHAN EŞİYOK ◽  
Özlem SEVEN ◽  
Gülüzar EYMUR ◽  
Gamze BORA TATAR ◽  
Didem DAYANGAÇ ERDEN ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Histone Deacetylase ◽  
Histone Deacetylase Inhibitors ◽  
Docking Studies ◽  
In Vitro Evaluation ◽  
Molecular Docking Studies ◽  
New Class ◽  
Butenoic Acid

scholarly journals Regulation of Immune Responses by Histone Deacetylase Inhibitors

2012 ◽  
Vol 2012 ◽  
pp. 1-10 ◽  
Author(s):  
Paul V. Licciardi ◽  
Tom C. Karagiannis
Keyword(s):  
Histone Deacetylase ◽  
Histone Deacetylase Inhibitors ◽  
Hdac Inhibitors ◽  
Adaptive Immune Response ◽  
Immune Gene ◽  
Epigenetic Factors ◽  
New Class ◽  
Adaptive Immune ◽  
Immune Gene Expression

Both genetic and epigenetic factors are important regulators of the immune system. There is an increasing body of evidence attesting to epigenetic modifications that influence the development of distinct innate and adaptive immune response cells. Chromatin remodelling via acetylation, methylation, phosphorylation, and ubiquitination of histone proteins as well as DNA, methylation is epigenetic mechanisms by which immune gene expression can be controlled. In this paper, we will discuss the role of epigenetics in the regulation of host immunity, with particular emphasis on histone deacetylase inhibitors. In particular, the role of HDAC inhibitors as a new class of immunomodulatory therapeutics will also be reviewed.

scholarly journals Antimalarial and Antileishmanial Activities of Aroyl-Pyrrolyl-Hydroxyamides, a New Class of Histone Deacetylase Inhibitors

2004 ◽  
Vol 48 (4) ◽  
pp. 1435-1436 ◽  
Author(s):  
Antonello Mai ◽  
Silvio Massa ◽  
Larry A. Walker ◽  
Ilaria Cerbara ◽  
Sergio Valente ◽  
...  
Keyword(s):  
Histone Deacetylase ◽  
Histone Deacetylase Inhibitors ◽  
New Class ◽  
Antileishmanial Activities

scholarly journals Discovery of a new class of histone deacetylase inhibitors with a novel zinc binding group

MedChemComm ◽  
2015 ◽  
Vol 6 (4) ◽  
pp. 613-618 ◽  
Author(s):  
Youxuan Li ◽  
Patrick M. Woster
Keyword(s):  
Histone Deacetylase ◽  
Histone Deacetylase Inhibitors ◽  
Hdac Inhibitors ◽  
Zinc Binding ◽  
New Class

Substituted 2-(oxazole-2-yl)phenols: a new class of HDAC inhibitors with a novel zinc binding group.

Histone deacetylase inhibitors: a new class of immunosuppressors targeting a novel signal pathway essential for CD154 expression

Blood ◽  
2003 ◽  
Vol 101 (4) ◽  
pp. 1430-1438 ◽  
Author(s):  
Søren Skov ◽  
Klaus Rieneck ◽  
Lone Frier Bovin ◽  
Kresten Skak ◽  
Søren Tomra ◽  
...  
Keyword(s):  
T Cells ◽  
T Cell ◽  
Histone Deacetylase ◽  
Histone Deacetylase Inhibitors ◽  
Immunosuppressive Agents ◽  
Gene Activation ◽  
Interleukin 2 ◽  
Therapeutic Interventions ◽  
Dependent Manner ◽  
New Class

Here we report that histone deacetylase inhibitors (HDAC-i) comprise a new class of immunosuppressive agents. HDAC-i inhibited CD4 T-cell proliferation in a dose-dependent manner, which was not caused by apoptosis or decreased viability. Although early intracellular signals such as tyrosine kinase activity and elevation of intracellular calcium concentration were not affected, the characteristic aggregation of T cells following activation was completely abrogated. This correlated with diminished activation-induced expression of the adhesion molecules. HDAC-i furthermore inhibited activation-induced CD25 and CD154 expression on CD4 cells, without affecting induction of CD69. HDAC-i inhibited CD154 expression by a mechanism distinctly different from cyclosporine-mediated inhibition. HDAC-i thus inhibited interleukin 2 (IL-2)–induced CD154 expression on effector T cells and constitutively expressed CD154 on various tumor cells, events that were not affected by cyclosporine. Additional studies showed that HDAC-i treatment inhibited c-Myc expression, which was further shown to be important for CD154 gene activation. These results demonstrate pronounced T-cell inhibitory activity of HDAC-i, which may form the basis of novel therapeutic interventions against autoimmune diseases and allograft rejection.

Sign in / Sign up

Export Citation Format

Share Document