Lead Optimization of Small Molecule ENL YEATS Inhibitors to Enable
Journal
ACS medicinal chemistry letters
ISSN: 1948-5875
Titre abrégé: ACS Med Chem Lett
Pays: United States
ID NLM: 101521073
Informations de publication
Date de publication:
11 Apr 2024
11 Apr 2024
Historique:
received:
10
01
2024
revised:
04
03
2024
accepted:
07
03
2024
pmc-release:
11
04
2025
medline:
17
4
2024
pubmed:
17
4
2024
entrez:
17
4
2024
Statut:
epublish
Résumé
Eleven-nineteen leukemia (ENL) is an epigenetic reader protein that drives oncogenic transcriptional programs in acute myeloid leukemia (AML). AML is one of the deadliest hematopoietic malignancies, with an overall 5-year survival rate of 27%. The epigenetic reader activity of ENL is mediated by its YEATS domain that binds to acetyl and crotonyl marks on histone tails and colocalizes with promoters of actively transcribed genes that are essential for leukemia. Prior to the discovery of
Identifiants
pubmed: 38628784
doi: 10.1021/acsmedchemlett.4c00016
pmc: PMC11017412
doi:
Types de publication
Journal Article
Langues
eng
Pagination
524-532Informations de copyright
© 2024 American Chemical Society.
Déclaration de conflit d'intérêts
The authors declare the following competing financial interest(s): T.A.K., M.M., M.W.M., Y.F., A.W.S., P.T.M., S.K., N.J.L., and D.J.H. are current or former employees of the Sanders Tri-Institutional Therapeutics Discovery Institute (TDI) and may benefit from the further development and licensure of molecules described herein.