PROTAC chemical probes for histone deacetylase enzymes.
Journal
RSC chemical biology
ISSN: 2633-0679
Titre abrégé: RSC Chem Biol
Pays: England
ID NLM: 101768727
Informations de publication
Date de publication:
30 Aug 2023
30 Aug 2023
Historique:
received:
27
06
2023
accepted:
27
07
2023
medline:
1
9
2023
pubmed:
1
9
2023
entrez:
1
9
2023
Statut:
epublish
Résumé
Over the past three decades, we have witnessed the progression of small molecule chemical probes designed to inhibit the catalytic active site of histone deacetylase (HDAC) enzymes into FDA approved drugs. However, it is only in the past five years we have witnessed the emergence of proteolysis targeting chimeras (PROTACs) capable of promoting the proteasome mediated degradation of HDACs. This is a field still in its infancy, however given the current progress of PROTACs in clinical trials and the fact that FDA approved HDAC drugs are already in the clinic, there is significant potential in developing PROTACs to target HDACs as therapeutics. Beyond therapeutics, PROTACs also serve important applications as chemical probes to interrogate fundamental biology related to HDACs
Identifiants
pubmed: 37654508
doi: 10.1039/d3cb00105a
pii: d3cb00105a
pmc: PMC10467623
doi:
Types de publication
Journal Article
Review
Langues
eng
Pagination
623-634Informations de copyright
This journal is © The Royal Society of Chemistry.
Déclaration de conflit d'intérêts
J. T. H. and J. P. S. are inventors on the PCT patent application WO2021148811A1 and the following patents: JP2023-510947, US2023-0120211A1.
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