Design and Synthesis of Styrenylcyclopropylamine LSD1 Inhibitors.
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 Jun 2020
11 Jun 2020
Historique:
received:
03
02
2020
accepted:
06
05
2020
entrez:
20
6
2020
pubmed:
20
6
2020
medline:
20
6
2020
Statut:
epublish
Résumé
Leveraging the catalytic machinery of LSD1 (KDM1A), a series of covalent styrenylcyclopropane LSD1 inhibitors were identified. These inhibitors represent a new class of mechanism-based inhibitors that target and covalently label the FAD cofactor of LSD1. The series was rapidly progressed to potent biochemical and cellular LSD1 inhibitors with good physical properties. This effort resulted in the identification of
Identifiants
pubmed: 32551003
doi: 10.1021/acsmedchemlett.0c00060
pmc: PMC7294731
doi:
Types de publication
Journal Article
Langues
eng
Pagination
1213-1220Informations de copyright
Copyright © 2020 American Chemical Society.
Déclaration de conflit d'intérêts
The authors declare no competing financial interest.
Références
ChemMedChem. 2007 Aug;2(8):1100-15
pubmed: 17530727
J Am Chem Soc. 2010 May 19;132(19):6827-33
pubmed: 20415477
Biochemistry. 2007 Apr 10;46(14):4408-16
pubmed: 17367163
Pharmacol Ther. 2015 Jun;150:1-22
pubmed: 25578037
Science. 2013 Mar 29;339(6127):1567-70
pubmed: 23539597
Eur J Cell Biol. 2010 Jul;89(7):557-63
pubmed: 20189264
Cancer Cell. 2015 Jul 13;28(1):57-69
pubmed: 26175415
SLAS Discov. 2017 Jan;22(1):3-20
pubmed: 27703080
Trends Biochem Sci. 2008 Apr;33(4):181-9
pubmed: 18343668
Cancer Res. 2011 Feb 1;71(3):655-60
pubmed: 21115810
J Biol Chem. 2010 Sep 24;285(39):29676-80
pubmed: 20705612
Int J Cancer. 2016 Jan 15;138(2):428-39
pubmed: 26240060
Mol Cell Biol. 2010 Oct;30(20):4851-63
pubmed: 20713442
Cell. 2018 Jul 26;174(3):549-563.e19
pubmed: 29937226
Cell. 2007 Feb 23;128(4):693-705
pubmed: 17320507
Cell. 2004 Dec 29;119(7):941-53
pubmed: 15620353
Cancer Cell. 2012 Apr 17;21(4):473-87
pubmed: 22464800
Cell Res. 2011 Mar;21(3):381-95
pubmed: 21321607
Nature. 2005 Sep 15;437(7057):436-9
pubmed: 16079795
Oncogene. 2012 Nov 29;31(48):5007-18
pubmed: 22310283
Biol Reprod. 2007 Nov;77(5):754-64
pubmed: 17634443
Int J Cancer. 2011 Feb 1;128(3):574-86
pubmed: 20333681
Nat Rev Drug Discov. 2007 Nov;6(11):881-90
pubmed: 17971784