Discovery of Reversible Inhibitors of KDM1A Efficacious in Acute Myeloid Leukemia Models.
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:
14 May 2020
14 May 2020
Historique:
received:
16
12
2019
accepted:
13
02
2020
entrez:
22
5
2020
pubmed:
22
5
2020
medline:
22
5
2020
Statut:
epublish
Résumé
Lysine-specific demethylase 1 (LSD1 or KDM1A) is a FAD-dependent enzyme that acts as a transcription corepressor or coactivator by regulating the methylation status of histone H3 lysines K4 and K9, respectively. KDM1A represents an attractive target for cancer therapy. While, in the past, the main medicinal chemistry strategy toward KDM1A inhibition was based on the optimization of ligands that irreversibly bind the FAD cofactor within the enzyme catalytic site, we and others have also identified reversible inhibitors. Herein we reported the discovery of 5-imidazolylthieno[3,2-
Identifiants
pubmed: 32435381
doi: 10.1021/acsmedchemlett.9b00604
pmc: PMC7236255
doi:
Types de publication
Journal Article
Langues
eng
Pagination
754-759Subventions
Organisme : Medical Research Council
ID : G0800892
Pays : United Kingdom
Informations de copyright
Copyright © 2020 American Chemical Society.
Déclaration de conflit d'intérêts
The authors declare no competing financial interest.
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