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Discovery of Aminopiperidine Indoles That Activate the Guanine Nucleotide Exchange Factor SOS1 and Modulate RAS Signaling.
J Med Chem. 2018 Jul 26;61(14):6002-6017. doi: 10.1021/acs.jmedchem.8b00360. Epub 2018 Jul 11.
J Med Chem. 2018.
PMID: 29856609
Small Molecule-Mediated Activation of RAS Elicits Biphasic Modulation of Phospho-ERK Levels that Are Regulated through Negative Feedback on SOS1.
Howes JE, Akan DT, Burns MC, Rossanese OW, Waterson AG, Fesik SW.
Howes JE, et al. Among authors: akan dt.
Mol Cancer Ther. 2018 May;17(5):1051-1060. doi: 10.1158/1535-7163.MCT-17-0666. Epub 2018 Feb 13.
Mol Cancer Ther. 2018.
PMID: 29440291
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Discovery and Structure-Based Optimization of Benzimidazole-Derived Activators of SOS1-Mediated Nucleotide Exchange on RAS.
Hodges TR, Abbott JR, Little AJ, Sarkar D, Salovich JM, Howes JE, Akan DT, Sai J, Arnold AL, Browning C, Burns MC, Sobolik T, Sun Q, Beesetty Y, Coker JA, Scharn D, Stadtmueller H, Rossanese OW, Phan J, Waterson AG, McConnell DB, Fesik SW.
Hodges TR, et al. Among authors: akan dt.
J Med Chem. 2018 Oct 11;61(19):8875-8894. doi: 10.1021/acs.jmedchem.8b01108. Epub 2018 Sep 28.
J Med Chem. 2018.
PMID: 30205005
Free PMC article.
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Small Molecule SOS1 Agonists Modulate MAPK and PI3K Signaling via Independent Cellular Responses.
Akan DT, Howes JE, Sai J, Arnold AL, Beesetty Y, Phan J, Olejniczak ET, Waterson AG, Fesik SW.
Akan DT, et al.
ACS Chem Biol. 2019 Mar 15;14(3):325-331. doi: 10.1021/acschembio.8b00869. Epub 2019 Feb 18.
ACS Chem Biol. 2019.
PMID: 30735352
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Discovery of Quinazolines That Activate SOS1-Mediated Nucleotide Exchange on RAS.
Abbott JR, Patel PA, Howes JE, Akan DT, Kennedy JP, Burns MC, Browning CF, Sun Q, Rossanese OW, Phan J, Waterson AG, Fesik SW.
Abbott JR, et al. Among authors: akan dt.
ACS Med Chem Lett. 2018 Aug 8;9(9):941-946. doi: 10.1021/acsmedchemlett.8b00296. eCollection 2018 Sep 13.
ACS Med Chem Lett. 2018.
PMID: 30258545
Free PMC article.
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