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 voor dit werk

Onderzoeksoutput › peer review

266 Citaten (Scopus)

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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.

Originele taal-2	English
Pagina's (van-tot)	942-948
Aantal pagina's	7
Tijdschrift	Drug Discovery Today
Volume	14
Nummer van het tijdschrift	19-20
DOI's	https://doi.org/10.1016/j.drudis.2009.06.008
Status	Published - okt.-2009

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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",

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T1 - Histone acetyl transferases as emerging drug targets

AU - Dekker, Frank J.

AU - Haisma, Hidde J.

PY - 2009/10

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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

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