Cell biologist’s perspective: Frontiers in Development of PROTAC-HDAC degraders.

Abstract

Structure of the article: HDACsClassificationEpigenetic regulatorsHDACs and Epigenetics of AgingNon-histone substrates of HDACsHistone modifying multiprotein complexesInsight from knockout studiesHDAC inhibitorsMolecular and cellular mechanisms of action of HDAC inhibitorsMolecular mechanism of actionCellular mechanism of actionPre-clinical and clinical use of HDAC inhibitors PROTACs and Molecular Glues: bi-valent and mono-valent degradersClass I HDAC degradersHDAC6 degradersPROTACs targeting NAD+-dependent histone deacetylasesNon-selective HDAC degradersHistone methyltransferase-specific PROTACsHDAC PROTACs: molecular mechanismsHDAC PROTACs: cellular mechanismsDesign and Development of PROTAC-mediated HDAC DegradationTesting HDAC degradersOpen key questions and perspectives in developing HDAC-degradersLiterature CitedAcknowledgments