Histone acetyl transferases as emerging drug targets

Frank J. Dekker; Hidde J. Haisma

doi:10.1016/j.drudis.2009.06.008

Histone acetyl transferases as emerging drug targets

Frank J. Dekker^*, Hidde J. Haisma

^*Corresponding author for this work

Research output: Contribution to journal › Review article › peer-review

266 Citations (Scopus)

Abstract

Post-translational modifications, such as acetylation or phosphorylation, play a crucial role in the regulation of gene transcription in eukaryotes. Different subtypes of histone acetyl transferases (HATs) catalyze the acetylation of histones on specific lysine residues. A potential role of HATs in the pathology of cancer, asthma, COPD and viral infection has been described. This indicates that specific HAT inhibitors are potential tools for pharmacological research and might find therapeutic applications. This review focuses on the role of the HATs p300, CBP, PCAF and GCN5 in different diseases and the development of small-molecule inhibitors of these enzymes as potential drugs.

Original language	English
Pages (from-to)	942-948
Number of pages	7
Journal	Drug Discovery Today
Volume	14
Issue number	19-20
DOIs	https://doi.org/10.1016/j.drudis.2009.06.008
Publication status	Published - Oct-2009

Keywords

SIMILARITY CLUSTERING PSSC
SMALL-MOLECULE MODULATORS
GLOBAL GENE-EXPRESSION
MODIFYING ENZYMES
ACETYLTRANSFERASE INHIBITOR
CHROMATIN TRANSCRIPTION
MONOCYTIC LEUKEMIA
G1/S TRANSITION
ANACARDIC ACID
HIGH-AFFINITY

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title = "Histone acetyl transferases as emerging drug targets",

abstract = "Post-translational modifications, such as acetylation or phosphorylation, play a crucial role in the regulation of gene transcription in eukaryotes. Different subtypes of histone acetyl transferases (HATs) catalyze the acetylation of histones on specific lysine residues. A potential role of HATs in the pathology of cancer, asthma, COPD and viral infection has been described. This indicates that specific HAT inhibitors are potential tools for pharmacological research and might find therapeutic applications. This review focuses on the role of the HATs p300, CBP, PCAF and GCN5 in different diseases and the development of small-molecule inhibitors of these enzymes as potential drugs.",

keywords = "SIMILARITY CLUSTERING PSSC, SMALL-MOLECULE MODULATORS, GLOBAL GENE-EXPRESSION, MODIFYING ENZYMES, ACETYLTRANSFERASE INHIBITOR, CHROMATIN TRANSCRIPTION, MONOCYTIC LEUKEMIA, G1/S TRANSITION, ANACARDIC ACID, HIGH-AFFINITY",

author = "Dekker, {Frank J.} and Haisma, {Hidde J.}",

year = "2009",

month = oct,

doi = "10.1016/j.drudis.2009.06.008",

language = "English",

volume = "14",

pages = "942--948",

journal = "Drug Discovery Today",

issn = "1359-6446",

publisher = "ELSEVIER SCI LTD",

number = "19-20",

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TY - JOUR

T1 - Histone acetyl transferases as emerging drug targets

AU - Dekker, Frank J.

AU - Haisma, Hidde J.

PY - 2009/10

Y1 - 2009/10

N2 - Post-translational modifications, such as acetylation or phosphorylation, play a crucial role in the regulation of gene transcription in eukaryotes. Different subtypes of histone acetyl transferases (HATs) catalyze the acetylation of histones on specific lysine residues. A potential role of HATs in the pathology of cancer, asthma, COPD and viral infection has been described. This indicates that specific HAT inhibitors are potential tools for pharmacological research and might find therapeutic applications. This review focuses on the role of the HATs p300, CBP, PCAF and GCN5 in different diseases and the development of small-molecule inhibitors of these enzymes as potential drugs.

AB - Post-translational modifications, such as acetylation or phosphorylation, play a crucial role in the regulation of gene transcription in eukaryotes. Different subtypes of histone acetyl transferases (HATs) catalyze the acetylation of histones on specific lysine residues. A potential role of HATs in the pathology of cancer, asthma, COPD and viral infection has been described. This indicates that specific HAT inhibitors are potential tools for pharmacological research and might find therapeutic applications. This review focuses on the role of the HATs p300, CBP, PCAF and GCN5 in different diseases and the development of small-molecule inhibitors of these enzymes as potential drugs.

KW - SIMILARITY CLUSTERING PSSC

KW - SMALL-MOLECULE MODULATORS

KW - GLOBAL GENE-EXPRESSION

KW - MODIFYING ENZYMES

KW - ACETYLTRANSFERASE INHIBITOR

KW - CHROMATIN TRANSCRIPTION

KW - MONOCYTIC LEUKEMIA

KW - G1/S TRANSITION

KW - ANACARDIC ACID

KW - HIGH-AFFINITY

U2 - 10.1016/j.drudis.2009.06.008

DO - 10.1016/j.drudis.2009.06.008

M3 - Review article

SN - 1359-6446

VL - 14

SP - 942

EP - 948

JO - Drug Discovery Today

JF - Drug Discovery Today

IS - 19-20

ER -

Histone acetyl transferases as emerging drug targets

Abstract

Keywords

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