Son, Se In published the artcileActivity-guided design of HDAC11-specific inhibitors, Application of 2-Chloro-5-(trifluoromethyl)pyrazine, the main research area is HDAC11 inhibitor histone dacetylase.
Mammalian histone deacetylases (HDACs) are a class of enzymes that play important roles in biol. pathways. Existing HDAC inhibitors target multiple HDACs without much selectivity. Inhibitors that target one particular HDAC will be useful for investigating the biol. functions of HDACs and for developing better therapeutics. Here, we report the development of HDAC11-specific inhibitors using an activity-guided rational design approach. The enzymic activity and biol. function of HDAC11 have been little known, but recent reports suggest that it has efficient defatty-acylation activity and that inhibiting it could be useful for treating a variety of human diseases, including viral infection, multiple sclerosis, and metabolic diseases. Our best inhibitor, SIS17(I), is active in cells and inhibited the demyristoylation of a known HDAC11 substrate, serine hydroxymethyl transferase 2, without inhibiting other HDACs. The activity-guided design may also be useful for the development of isoform-specific inhibitors for other classes of enzymes.
ACS Chemical Biology published new progress about Histone deacetylase inhibitors. 799557-87-2 belongs to class pyrazines, name is 2-Chloro-5-(trifluoromethyl)pyrazine, and the molecular formula is C5H2ClF3N2, Application of 2-Chloro-5-(trifluoromethyl)pyrazine.