Titel (eng)

Medicinal chemistry advances in targeting class I histone deacetylases

Autor*in

Diaaeldin I. Abdallah   University of Toronto

Patrick T. Gunning   University of Toronto

Oliver H. Krämer   University of Mainz

Richard Moriggl   University of Veterinary Medicine Vienna

Lina S. Hasan   University of Toronto

Elvin D de Araujo   University of Toronto

Naman H. Patel   University of Toronto

Verlag

Open Exploration

Beschreibung (eng)

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.

Sprache des Objekts

Englisch

Datum

2023

Rechte

Dieses Werk bzw. dieser Inhalt steht unter einer
CC BY 4.0 - Creative Commons Namensnennung 4.0 International Lizenz.

CC BY 4.0 International

http://creativecommons.org/licenses/by/4.0/

Klassifikation

cap group; epigenetic regulation; Histone deacetylases; medicinal chemistry; small-molecule inhibitors; zinc-binding group

Mitglied in der/den Collection(s) (1)