The unfolded protein response modulators GSK2606414 and KIRA6 are potent KIT inhibitors.
Adenine
/ analogs & derivatives
Cell Survival
/ drug effects
Endocytosis
/ drug effects
HEK293 Cells
Hep G2 Cells
Humans
Imidazoles
/ chemistry
Indoles
/ chemistry
Kinetics
Lysosomes
/ drug effects
Naphthalenes
/ chemistry
Proto-Oncogene Proteins c-kit
/ antagonists & inhibitors
Pyrazines
/ chemistry
Unfolded Protein Response
/ drug effects
eIF-2 Kinase
/ antagonists & inhibitors
Journal
Cell death & disease
ISSN: 2041-4889
Titre abrégé: Cell Death Dis
Pays: England
ID NLM: 101524092
Informations de publication
Date de publication:
01 04 2019
01 04 2019
Historique:
received:
19
12
2018
accepted:
11
03
2019
revised:
10
03
2019
entrez:
2
4
2019
pubmed:
2
4
2019
medline:
19
5
2020
Statut:
epublish
Résumé
IRE1, PERK, and ATF6 are the three transducers of the mammalian canonical unfolded protein response (UPR). GSK2606414 is a potent inhibitor of PERK, while KIRA6 inhibits the kinase activity of IRE1. Both molecules are frequently used to probe the biological roles of the UPR in mammalian cells. In a direct binding assay, GSK2606414 bound to the cytoplasmic domain of KIT with dissociation constants (K
Identifiants
pubmed: 30931942
doi: 10.1038/s41419-019-1523-3
pii: 10.1038/s41419-019-1523-3
pmc: PMC6443726
doi:
Substances chimiques
7-methyl-5-(1-((3-(trifluoromethyl)phenyl)acetyl)-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo(2,3-d)pyrimidin-4-amine
0
Imidazoles
0
Indoles
0
KIRA6
0
Naphthalenes
0
Pyrazines
0
Proto-Oncogene Proteins c-kit
EC 2.7.10.1
PERK kinase
EC 2.7.11.1
eIF-2 Kinase
EC 2.7.11.1
Adenine
JAC85A2161
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
300Références
Am J Physiol Cell Physiol. 2009 Sep;297(3):C591-600
pubmed: 19587220
Nat Biotechnol. 2016 Feb;34(2):184-191
pubmed: 26780180
Blood. 2000 Aug 1;96(3):925-32
pubmed: 10910906
Cell Death Dis. 2015 Mar 05;6:e1672
pubmed: 25741597
Cell. 2014 Jul 31;158(3):534-48
pubmed: 25018104
Blood. 2014 Apr 10;123(15):2317-24
pubmed: 24569263
J Cell Sci. 2017 Dec 15;130(24):4087-4096
pubmed: 29180516
Biochim Biophys Acta. 2013 Dec;1833(12):3460-3470
pubmed: 23850759
PLoS One. 2014 Oct 03;9(10):e109441
pubmed: 25279552
Sci Signal. 2011 Sep 06;4(190):pe40
pubmed: 21917713
Mol Cancer Res. 2018 Oct;16(10):1447-1453
pubmed: 29991528
Biochim Biophys Acta Mol Basis Dis. 2018 Oct;1864(10):3164-3180
pubmed: 30293566
J Biol Chem. 2004 Jul 23;279(30):31655-63
pubmed: 15123710
Cell Death Differ. 2017 Jun;24(6):1100-1110
pubmed: 28452996
Oncogene. 2013 Feb 21;32(8):1018-29
pubmed: 22525273
Mol Cell. 2000 Nov;6(5):1099-108
pubmed: 11106749
J Med Chem. 2014 May 22;57(10):4289-301
pubmed: 24749861
Oncotarget. 2017 Jul 18;8(34):56158-56167
pubmed: 28915580
Curr Pharm Des. 2014;20(17):2849-80
pubmed: 23944364
Sci Rep. 2017 Nov 10;7(1):15278
pubmed: 29127384
Antimicrob Agents Chemother. 2018 Oct 24;62(11):
pubmed: 30181373
PLoS One. 2012;7(7):e40853
pubmed: 22815843
Cancer Res. 2006 Jan 1;66(1):473-81
pubmed: 16397263
J Med Chem. 2015 Feb 12;58(3):1426-41
pubmed: 25587754
Science. 2011 Nov 25;334(6059):1081-6
pubmed: 22116877
Oncogene. 2002 Jul 4;21(29):4508-20
pubmed: 12085229
Proc Natl Acad Sci U S A. 2013 Apr 2;110(14):5689-94
pubmed: 23493555
J Med Chem. 2012 Aug 23;55(16):7193-207
pubmed: 22827572
Cell Metab. 2017 Apr 4;25(4):883-897.e8
pubmed: 28380378
PLoS Genet. 2016 Dec 15;12(12):e1006518
pubmed: 27977682
Science. 2013 Feb 15;339(6121):819-23
pubmed: 23287718
J Pharmacol Exp Ther. 2016 Jun;357(3):554-61
pubmed: 27048659
Immunopharmacol Immunotoxicol. 2015;37(4):380-7
pubmed: 26181649
Mol Cell Biol. 1998 Apr;18(4):2089-99
pubmed: 9528781
Elife. 2017 Oct 03;6:
pubmed: 28971800
Blood. 2006 Jan 15;107(2):752-9
pubmed: 16189265