This review summarizes the past and present advances in developing degraders of epigenetic targets which play critical roles in many crucial biological pathways and therefore, targeted for the discovery of therapeutics.
Accurate prediction of protein–ligand and protein–protein interactions is essential for computational drug discovery, yet remains a significant challenge, particularly for complexes involving large, flexible ligands.
ATP-Competitive inhibitors do not inhibit a kinase's non-catalytic, scaffolding roles. Instead, this goal may be accomplished by targeted protein degradation.
Machine learning (ML) accelerates PROTAC design by optimizing linkers and protein–ligase interactions, enabling selective protein degradation for therapeutic applications, particularly targeting previously undruggable proteins.
A review on current proteolysis targeting chimeras (PROTACs) as chemical probes for histone deacetylase (HDAC) enzymes.