Fig. 3
From: Targeting the CoREST complex with dual histone deacetylase and demethylase inhibitors
Corin exhibits sustained inhibition of CoREST complex HDAC activity. a Relative CoREST complex HDAC activity. b Relative MiDAC complex HDAC activity. Protein complexes at 500 nM and all compounds at 5 µM preincubated for 30 min prior to dialysis and dilution to measure HDAC activity at 2 nM (CoREST complex) or 8 nM (MiDAC complex). 50 µM acetylated P53379–382 tetrapeptide (RHKK(Ac)) was used as substrate. c Corin exhibits near irreversible inhibition of CoREST complex HDAC activity relative to unifunctional LSD1 and HDAC inhibitors after jump dilution (CoREST complex = 0.5 µM, inhibitor = 5 µM, substrate = 200 µM acetylated P53379–382 tetrapeptide RHKK(Ac)). d Model depicting dual engagement mechanism of corin leading to sustained inhibition of CoREST complex HDAC activity. Data (mean ± SEM) are representative of at least two independent experiments
