HDAC inhibitors in cancer therapy

A. Ganesan

doi:10.1016/B978-0-12-816422-8.00002-7

HDAC inhibitors in cancer therapy

A. Ganesan

Research output: Chapter in Book/Report/Conference proceeding › Chapter

3 Citations (Scopus)

Abstract

Reversible lysine acetylation is a major posttranslational modification in histones and nonhistone proteins. Modulation of this process is an important target for drug discovery, most successfully through the inhibition of zinc-dependent histone deacetylases (HDACs). There are five HDAC inhibitors approved for the treatment of hematological cancers and more than 20 others in clinical development. This chapter reviews the current state of the art of HDAC therapy in terms of the biological functions of the enzymes, the structural classes of HDAC inhibitors, and their utility in cancer therapy based on the data from recent clinical trials.

Original language	English
Title of host publication	Histone Modifications in Therapy
Publisher	Elsevier
Chapter	2
Pages	19-49
Number of pages	31
ISBN (Electronic)	9780128164228
ISBN (Print)	9780128164228
DOIs	https://doi.org/10.1016/B978-0-12-816422-8.00002-7
Publication status	Published - 2020

Keywords

Cancer chemotherapy
Drug discovery
Enzyme inhibitors
Epigenetics
Histone deacetylases
Metal-binding drugs
Posttranslational modifications

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

Access to Document

10.1016/B978-0-12-816422-8.00002-7

https://linkinghub.elsevier.com/retrieve/pii/B9780128164228000027

Cite this

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abstract = "Reversible lysine acetylation is a major posttranslational modification in histones and nonhistone proteins. Modulation of this process is an important target for drug discovery, most successfully through the inhibition of zinc-dependent histone deacetylases (HDACs). There are five HDAC inhibitors approved for the treatment of hematological cancers and more than 20 others in clinical development. This chapter reviews the current state of the art of HDAC therapy in terms of the biological functions of the enzymes, the structural classes of HDAC inhibitors, and their utility in cancer therapy based on the data from recent clinical trials.",

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T1 - HDAC inhibitors in cancer therapy

AU - Ganesan, A.

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AB - Reversible lysine acetylation is a major posttranslational modification in histones and nonhistone proteins. Modulation of this process is an important target for drug discovery, most successfully through the inhibition of zinc-dependent histone deacetylases (HDACs). There are five HDAC inhibitors approved for the treatment of hematological cancers and more than 20 others in clinical development. This chapter reviews the current state of the art of HDAC therapy in terms of the biological functions of the enzymes, the structural classes of HDAC inhibitors, and their utility in cancer therapy based on the data from recent clinical trials.

KW - Cancer chemotherapy

KW - Drug discovery

KW - Enzyme inhibitors

KW - Epigenetics

KW - Histone deacetylases

KW - Metal-binding drugs

KW - Posttranslational modifications

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U2 - 10.1016/B978-0-12-816422-8.00002-7

DO - 10.1016/B978-0-12-816422-8.00002-7

M3 - Chapter

SN - 9780128164228

SP - 19

EP - 49

BT - Histone Modifications in Therapy

PB - Elsevier

ER -

HDAC inhibitors in cancer therapy

Abstract

Keywords

UN SDGs

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