Discovery timeline of HDAC8-degrading PROTACs.
This study presents the synthesis of enzyme-responsive nanoparticles targeting HDAC8, an epigenetic enzyme, through a deacetylation reaction. This first-time report highlights the potential for these particles to mimic synthetic histones.
A review on current proteolysis targeting chimeras (PROTACs) as chemical probes for histone deacetylase (HDAC) enzymes.
Single-molecule analysis reveals how ligand modifications synergistically control HDAC8 catalysis by stabilizing active conformations, providing mechanistic insights into ligand-regulated enzymatic catalysis.
A three-step catalytic mechanism is obtained from MP2/MM geometry optimization for HDAC8. Comparison of different QM/MM methods highlights the importance of using accurate QM methods in the study of enzyme catalysis.