Medicinal chemistry advances in targeting class I histone deacetylases.
Histone deacetylases
cap group
epigenetic regulation
medicinal chemistry
small-molecule inhibitors
zinc-binding group
Journal
Exploration of targeted anti-tumor therapy
ISSN: 2692-3114
Titre abrégé: Explor Target Antitumor Ther
Pays: United States
ID NLM: 101770662
Informations de publication
Date de publication:
2023
2023
Historique:
received:
28
03
2023
accepted:
22
06
2023
medline:
15
9
2023
pubmed:
15
9
2023
entrez:
15
9
2023
Statut:
ppublish
Résumé
Histone deacetylases (HDACs) are a class of zinc (Zn)-dependent metalloenzymes that are responsible for epigenetic modifications. HDACs are largely associated with histone proteins that regulate gene expression at the DNA level. This tight regulation is controlled by acetylation [via histone acetyl transferases (HATs)] and deacetylation (via HDACs) of histone and non-histone proteins that alter the coiling state of DNA, thus impacting gene expression as a downstream effect. For the last two decades, HDACs have been studied extensively and indicated in a range of diseases where HDAC dysregulation has been strongly correlated with disease emergence and progression-most prominently, cancer, neurodegenerative diseases, HIV, and inflammatory diseases. The involvement of HDACs as regulators in these biochemical pathways established them as an attractive therapeutic target. This review summarizes the drug development efforts exerted to create HDAC inhibitors (HDACis), specifically class I HDACs, with a focus on the medicinal chemistry, structural design, and pharmacology aspects of these inhibitors.
Identifiants
pubmed: 37711592
doi: 10.37349/etat.2023.00166
pmc: PMC10497394
doi:
Types de publication
Journal Article
Review
Langues
eng
Pagination
757-779Informations de copyright
© The Author(s) 2023.
Déclaration de conflit d'intérêts
The authors declare that they have no conflicts of interest.
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