Thirty years of HDAC inhibitors: 2020 hindsight

Terence C. S. Ho, Alex H. Y. Chan, A. Ganesan

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It is now thirty years since the first report of a potent zinc-dependent histone deacetylase (HDAC) inhibitor appeared. Since then, five HDAC inhibitors have received regulatory approval for cancer chemotherapy, while many others are in clinical development for oncology as well as other therapeutic indications. This perspective reviews the biological and medicinal chemistry advances over the last three decades with an emphasis on the design of selective inhibitors that discriminate between the eleven human HDAC isoforms.
Original languageEnglish
Pages (from-to)12460–12484
Number of pages25
JournalJournal of Medicinal Chemistry
Issue number21
Early online date1 Jul 2020
Publication statusPublished - 12 Nov 2020

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