IOA-244 is a Non-ATP-competitive, Highly Selective, Tolerable PI3K Delta Inhibitor That Targets Solid Tumors and Breaks Immune Tolerance.
Journal
Cancer research communications
ISSN: 2767-9764
Titre abrégé: Cancer Res Commun
Pays: United States
ID NLM: 9918281580506676
Informations de publication
Date de publication:
04 2023
04 2023
Historique:
received:
22
11
2022
revised:
21
12
2022
accepted:
14
03
2023
medline:
18
4
2023
entrez:
17
4
2023
pubmed:
18
4
2023
Statut:
epublish
Résumé
PI3K delta (PI3Kδ) inhibitors are used to treat lymphomas but safety concerns and limited target selectivity curbed their clinical usefulness. PI3Kδ inhibition in solid tumors has recently emerged as a potential novel anticancer therapy through the modulation of T-cell responses and direct antitumor activity. Here we report the exploration of IOA-244/MSC2360844, a first-in-class non-ATP-competitive PI3Kδ inhibitor, for the treatment of solid tumors. We confirm IOA-244's selectivity as tested against a large set of kinases, enzymes, and receptors. IOA-244 inhibits the IOA-244 is a first-in-class non-ATP-competitive, PI3Kδ inhibitor with direct antitumor
Identifiants
pubmed: 37066023
doi: 10.1158/2767-9764.CRC-22-0477
pii: CRC-22-0477
pmc: PMC10103717
doi:
Substances chimiques
Phosphatidylinositol 3-Kinases
EC 2.7.1.-
Phosphoinositide-3 Kinase Inhibitors
0
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Pagination
576-591Informations de copyright
© 2023 The Authors; Published by the American Association for Cancer Research.
Références
Clin Cancer Res. 2018 Jan 1;24(1):120-129
pubmed: 29066507
Front Oncol. 2013 Mar 01;3:40
pubmed: 23459844
J Exp Med. 2021 Apr 5;218(4):
pubmed: 33566112
Curr Med Chem. 2010;17(25):2804-21
pubmed: 20586715
Proc Natl Acad Sci U S A. 2005 Jan 18;102(3):802-7
pubmed: 15647370
J Exp Med. 2002 Sep 16;196(6):753-63
pubmed: 12235209
Lancet Oncol. 2018 Apr;19(4):486-496
pubmed: 29475723
Clin Cancer Res. 2008 Feb 15;14(4):1172-81
pubmed: 18281552
Cancer Cell. 2014 Jun 16;25(6):809-821
pubmed: 24909985
J Immunother Cancer. 2022 Mar;10(3):
pubmed: 35288465
Eur J Immunol. 2008 May;38(5):1215-24
pubmed: 18412166
Lancet Oncol. 2022 May;23(5):563-566
pubmed: 35429996
Front Immunol. 2021 Aug 06;12:708908
pubmed: 34421914
Hepatology. 2018 Dec;68(6):2285-2300
pubmed: 30300952
J Clin Pharmacol. 2015 Aug;55(8):909-19
pubmed: 25760671
Cancer Chemother Pharmacol. 2016 Jan;77(1):89-98
pubmed: 26645408
RSC Adv. 2019 Feb 21;9(11):6409-6418
pubmed: 35517257
Lancet Oncol. 2022 Aug;23(8):e364
pubmed: 35901825
Nat Immunol. 2019 Mar;20(3):326-336
pubmed: 30778252
Front Immunol. 2017 Sep 29;8:1221
pubmed: 29033940
Cancers (Basel). 2021 Nov 04;13(21):
pubmed: 34771694
Science. 2002 May 31;296(5573):1655-7
pubmed: 12040186
Chem Res Toxicol. 2018 Jul 16;31(7):548-555
pubmed: 29896955
Immunity. 2019 Jan 15;50(1):195-211.e10
pubmed: 30635237
Cancer Res. 2017 Apr 15;77(8):1892-1904
pubmed: 28108509
Sci Rep. 2019 May 17;9(1):7509
pubmed: 31101835
Blood. 2010 Sep 2;116(9):1460-8
pubmed: 20505158
Curr Opin Pharmacol. 2015 Aug;23:82-91
pubmed: 26093105
Front Immunol. 2014 May 22;5:233
pubmed: 24904582
Oncoimmunology. 2019 Mar 16;8(5):e1581556
pubmed: 31069145
Cell Death Dis. 2018 Sep 17;9(10):935
pubmed: 30224718
Cell Death Dis. 2018 Jun 7;9(6):678
pubmed: 29880805
Nature. 2014 Jun 19;510(7505):407-411
pubmed: 24919154
PLoS One. 2012;7(7):e40677
pubmed: 22815789
Nat Rev Drug Discov. 2021 Oct;20(10):741-769
pubmed: 34127844
ACS Med Chem Lett. 2019 Oct 17;10(11):1554-1560
pubmed: 31749910
Oncologist. 2020 Nov;25(11):e1604-e1613
pubmed: 32356383
Nat Rev Immunol. 2003 Apr;3(4):317-30
pubmed: 12669022
Haematologica. 2020 Jan 09;105(11):2584-2591
pubmed: 33131247
J Med Chem. 2020 Oct 8;63(19):11235-11257
pubmed: 32865410
Nature. 2004 Oct 21;431(7011):1007-11
pubmed: 15496927
Nature. 2022 May;605(7911):741-746
pubmed: 35508656
Cancer Cell. 2015 Jan 12;27(1):109-22
pubmed: 25544636
Cancer Res. 2017 Aug 1;77(15):4135-4145
pubmed: 28615225
Chem Biol. 2011 Jun 24;18(6):699-710
pubmed: 21700206
FASEB J. 2006 Mar;20(3):455-65
pubmed: 16507763
J Pharmacol Exp Ther. 2020 Jul;374(1):211-222
pubmed: 32345620