Fragment-Based Discovery of a Novel, Brain Penetrant, Orally Active HDAC2 Inhibitor.
Sign Up to like & getrecommendations! Published in 2022 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.2c00272
Abstract: Fragment-based ligand discovery was successfully applied to histone deacetylase HDAC2. In addition to the anticipated hydroxamic acid- and benzamide-based fragment screening hits, a low affinity (∼1 mM) α-amino-amide zinc binding fragment was identified, as well… read more here.
Keywords: fragment based; brain penetrant; hdac2 inhibitor; hdac2 ... See more keywords
HDAC2/3 inhibitor MI192 mitigates oligodendrocyte loss and reduces microglial activation upon injury: A potential role of epigenetics
Sign Up to like & getrecommendations! Published in 2021 at "Open Veterinary Journal"
DOI: 10.5455/ovj.2021.v11.i3.18
Abstract: Background: During development, oligodendrocyte (OL) lineage cells are susceptible to injury, leading to life-long clinical neurodevelopmental deficits, which lack effective treatments. Drugs targeting epigenetic modifications that inhibit histone deacetylases (HDACs) protect from many clinical neurodegenerative… read more here.
Keywords: microglial activation; inhibitor mi192; hdac2 inhibitor; pathology ... See more keywords