Discovery of potent SOS1 inhibitors that block RAS activation via disruption of the RAS-SOS1 interaction.
RAS
SOS
crystal structure
fragment screen
small-molecule inhibitor
Journal
Proceedings of the National Academy of Sciences of the United States of America
ISSN: 1091-6490
Titre abrégé: Proc Natl Acad Sci U S A
Pays: United States
ID NLM: 7505876
Informations de publication
Date de publication:
12 02 2019
12 02 2019
Historique:
pubmed:
27
1
2019
medline:
25
6
2019
entrez:
27
1
2019
Statut:
ppublish
Résumé
Since the late 1980s, mutations in the
Identifiants
pubmed: 30683722
pii: 1812963116
doi: 10.1073/pnas.1812963116
pmc: PMC6377443
doi:
Substances chimiques
SOS1 Protein
0
Proto-Oncogene Proteins p21(ras)
EC 3.6.5.2
Banques de données
PDB
['5OVD', '5OVE', '5OVF', '5OVG', '5OVH', '5OVI', '6EIE', '6EPL', '6EPM', '6EPN', '6EPO', '6EPP']
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
2551-2560Informations de copyright
Copyright © 2019 the Author(s). Published by PNAS.
Déclaration de conflit d'intérêts
Conflict of interest statement: R.C.H. B.S., J.S., D.M., A.H., C.M.S., N.D.W., H.B., U.B., J.W., V.B., J.M., K.P., G.S., N.B., K.E., K.G., L.W., F.v.N., and B.B. are or have been employees and stockholders of Bayer AG. J.D.K. and D.W. are employees of Evotec AG. R.C.H., B.S., J.S., D.M., H.B., K.P., N.B., K.E., L.W., F.v.N., and B.B. are coauthors of a patent application.
Références
Proc Natl Acad Sci U S A. 2015 Feb 10;112(6):1761-6
pubmed: 25624485
Angew Chem Int Ed Engl. 2016 Dec 23;55(52):15982-15988
pubmed: 27635522
Nat Rev Drug Discov. 2014 Nov;13(11):828-51
pubmed: 25323927
Genes Cancer. 2011 Mar;2(3):298-305
pubmed: 21779500
Nature. 1982 Jul 22;298(5872):343-7
pubmed: 6283384
Acta Crystallogr D Biol Crystallogr. 2010 Apr;66(Pt 4):486-501
pubmed: 20383002
Cell. 2003 Mar 7;112(5):685-95
pubmed: 12628188
Curr Med Chem. 2011;18(7):943-63
pubmed: 21254978
Proc Natl Acad Sci U S A. 1982 Jun;79(11):3637-40
pubmed: 6285355
J Appl Crystallogr. 2007 Aug 1;40(Pt 4):658-674
pubmed: 19461840
Nature. 1998 Jul 23;394(6691):337-43
pubmed: 9690470
J Cell Sci. 2016 Apr 1;129(7):1287-92
pubmed: 26985062
Nat Rev Cancer. 2003 Jan;3(1):11-22
pubmed: 12509763
Acta Crystallogr D Biol Crystallogr. 2011 Apr;67(Pt 4):235-42
pubmed: 21460441
Chem Biol. 2014 Dec 18;21(12):1618-28
pubmed: 25455859
Mol Cancer Ther. 2018 May;17(5):1051-1060
pubmed: 29440291
Acta Crystallogr D Biol Crystallogr. 2011 Apr;67(Pt 4):355-67
pubmed: 21460454
Nat Rev Cancer. 2011 Oct 24;11(11):775-91
pubmed: 22020205
Mol Cancer Res. 2015 Sep;13(9):1325-35
pubmed: 26037647
Nat Rev Drug Discov. 2016 Nov;15(11):771-785
pubmed: 27469033
Nat Rev Cancer. 2010 Dec;10(12):842-57
pubmed: 21102635
Cell. 2018 Jan 25;172(3):578-589.e17
pubmed: 29373830
Nature. 2003 Dec 4;426(6966):525-30
pubmed: 14654833
Acta Crystallogr D Biol Crystallogr. 2004 Aug;60(Pt 8):1355-63
pubmed: 15272157
Science. 2015 Nov 27;350(6264):1096-101
pubmed: 26472758
Proc Natl Acad Sci U S A. 2014 Mar 4;111(9):3401-6
pubmed: 24550516
Trends Cancer. 2017 Oct;3(10):686-697
pubmed: 28958387
Science. 2016 Feb 5;351(6273):604-8
pubmed: 26841430
Biochemistry. 1997 Mar 25;36(12):3640-4
pubmed: 9132016
Angew Chem Int Ed Engl. 2012 Jun 18;51(25):6140-3
pubmed: 22566140
Nat Chem Biol. 2011 Jul 17;7(9):585-7
pubmed: 21765406
Cancer Discov. 2016 Mar;6(3):316-29
pubmed: 26739882
Acta Crystallogr D Biol Crystallogr. 2010 Feb;66(Pt 2):125-32
pubmed: 20124692
Cancer Res. 2010 Jan 15;70(2):440-6
pubmed: 20068163
J Biol Chem. 2002 Nov 29;277(48):46265-72
pubmed: 12196540
Cell. 2017 Jun 29;170(1):17-33
pubmed: 28666118
Cancer Cell. 2014 Mar 17;25(3):272-81
pubmed: 24651010
Proc Natl Acad Sci U S A. 2006 Nov 7;103(45):16692-7
pubmed: 17075039
Anal Biochem. 2018 May 1;548:44-52
pubmed: 29444450
J Med Chem. 2015 Mar 12;58(5):2265-74
pubmed: 25695162
Nature. 1982 Jun 10;297(5866):474-8
pubmed: 6283357