Publication

Histone acetyl transferases as emerging drug targets

Dekker, F. J. & Haisma, H. J., Oct-2009, In : Drug Discovery Today. 14, 19-20, p. 942-948 7 p.

Research output: Contribution to journalReview articleAcademicpeer-review

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 languageEnglish
Pages (from-to)942-948
Number of pages7
JournalDrug Discovery Today
Volume14
Issue number19-20
Publication statusPublished - 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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