Thirty years of HDAC inhibitors: 2020 hindsight

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

doi:10.1021/acs.jmedchem.0c00830

Thirty years of HDAC inhibitors: 2020 hindsight

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

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Abstract

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 language	English
Pages (from-to)	12460–12484
Number of pages	25
Journal	Journal of Medicinal Chemistry
Volume	63
Issue number	21
Early online date	1 Jul 2020
DOIs	https://doi.org/10.1021/acs.jmedchem.0c00830
Publication status	Published - 12 Nov 2020

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abstract = "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.",

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AU - Ganesan, A.

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AB - 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.

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Thirty years of HDAC inhibitors: 2020 hindsight

Abstract

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