1354547-63-9Relevant academic research and scientific papers
Selective Inhibition of Histone Deacetylase 10: Hydrogen Bonding to the Gatekeeper Residue is Implicated
Géraldy, Magalie,Morgen, Michael,Sehr, Peter,Steimbach, Raphael R.,Moi, Davide,Ridinger, Johannes,Oehme, Ina,Witt, Olaf,Malz, Mona,Nogueira, Mauro S.,Koch, Oliver,Gunkel, Nikolas,Miller, Aubry K.
, p. 4426 - 4443 (2019/05/17)
The discovery of isozyme-selective histone deacetylase (HDAC) inhibitors is critical for understanding the biological functions of individual HDACs and for validating HDACs as drug targets. The isozyme HDAC10 contributes to chemotherapy resistance and has
Second-generation histone deacetylase 6 inhibitors enhance the immunosuppressive effects of Foxp3+ T-regulatory cells
Kalin, Jay H.,Butler, Kyle V.,Akimova, Tatiana,Hancock, Wayne W.,Kozikowski, Alan P.
experimental part, p. 639 - 651 (2012/03/11)
Second-generation Tubastatin A analogues were synthesized and evaluated for their ability to inhibit selectively histone deacetylase 6 (HDAC6). Substitutions to the carboline cap group were well-tolerated with substitution at the 2-position of both β- and γ-carbolines being optimal for HDAC6 activity and selectivity. Some compounds in this series were determined to have subnanomolar activity at HDAC6 with more than 7000 fold selectivity for HDAC6 versus HDAC1. Selected compounds were then evaluated for their ability to augment the immunosuppressive effect of Foxp3+ regulatory T cells. All compounds tested were found to enhance the ability of regulatory T cells to inhibit the mitotic division of effector T cells both in vitro and in vivo, suggesting that further investigation into the use of these compounds for the treatment of autoimmune disorders is warranted.
