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Discovery of potent SOS1 inhibitors that block RAS activation via disruption of the RAS–SOS1 interaction

Proceedings of the National Academy of Sciences - PNAS, 2019-02, Vol.116 (7), p.2551-2560

2019

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Targeting protein-protein interaction by small molecules

Annual review of pharmacology and toxicology, 2014-01, Vol.54 (1), p.435-456

2014

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High-throughput screening identifies small molecules that bind to the RAS:SOS:RAS complex and perturb RAS signaling

Analytical biochemistry, 2018-05, Vol.548 (C), p.44-52

2018

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Discovery of Sulfonamide-Derived Agonists of SOS1-Mediated Nucleotide Exchange on RAS Using Fragment-Based Methods

Journal of medicinal chemistry, 2020-08, Vol.63 (15), p.8325-8337

2020

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Severe Lymphatic Disorder Resolved With MEK Inhibition in a Patient With Noonan Syndrome and SOS1 Mutation

Pediatrics (Evanston), 2020-12, Vol.146 (6), p.1

2020

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SOS1-inspired hydrocarbon-stapled peptide as a pan-Ras inhibitor

Bioorganic chemistry, 2023-06, Vol.135, p.106500-106500, Article 106500

2023

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The RASopathies: developmental syndromes of Ras/MAPK pathway dysregulation

Current opinion in genetics & development, 2009-06, Vol.19 (3), p.230-236

2009

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Membrane-dependent signal integration by the Ras activator Son of sevenless

Nature structural & molecular biology, 2008-05, Vol.15 (5), p.452-461

2008

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Role of the histone domain in the autoinhibition and activation of the Ras activator Son of Sevenless

Proceedings of the National Academy of Sciences - PNAS, 2010-02, Vol.107 (8), p.3430-3435

2010

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SOS1 gene overexpression increased salt tolerance in transgenic tobacco by maintaining a higher K +/Na + ratio

Journal of plant physiology, 2012-02, Vol.169 (3), p.255-261

2012

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Small Molecule Binding Sites on the Ras:SOS Complex Can Be Exploited for Inhibition of Ras Activation

Journal of medicinal chemistry, 2015-03, Vol.58 (5), p.2265-2274

2015

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Direct inhibition of oncogenic KRAS by hydrocarbon-stapled SOS1 helices

Proceedings of the National Academy of Sciences - PNAS, 2015-02, Vol.112 (6), p.1761-1766

2015

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Phospholipase D2-generated phosphatidic acid couples EGFR stimulation to Ras activation by Sos

Nature cell biology, 2007-06, Vol.9 (6), p.707-712

2007

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Design, synthesis, and bioevaluation of SOS1 PROTACs derived from pyrido[2,3-d]pyrimidin-7-one-based SOS1 inhibitor

Bioorganic & medicinal chemistry letters, 2024-07, Vol.107, p.129780-129780, Article 129780

2024

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Allosteric KRas4B Can Modulate SOS1 Fast and Slow Ras Activation Cycles

Biophysical journal, 2018-08, Vol.115 (4), p.629-641

2018

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Approach for targeting Ras with small molecules that activate SOS-mediated nucleotide exchange

Proceedings of the National Academy of Sciences - PNAS, 2014-03, Vol.111 (9), p.3401-3406

2014

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Constitutive high-level SOS1 expression and absence of HKT1;1 expression in the salt-accumulating halophyte Salicornia dolichostachya

Plant science (Limerick), 2015-05, Vol.234, p.144-154

2015

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Discovery and Structure-Based Optimization of Benzimidazole-Derived Activators of SOS1-Mediated Nucleotide Exchange on RAS

Journal of medicinal chemistry, 2018-10, Vol.61 (19), p.8875-8894

2018

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Mechanism of SOS PR-domain autoinhibition revealed by single-molecule assays on native protein from lysate

Nature communications, 2017-04, Vol.8 (1), p.15061-15061, Article 15061

2017

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Translational relevance of SOS1 targeting for KRAS‐mutant colorectal cancer

Molecular carcinogenesis, 2023-07, Vol.62 (7), p.1025-1037

2023

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Discovery of Aminopiperidine Indoles That Activate the Guanine Nucleotide Exchange Factor SOS1 and Modulate RAS Signaling

Journal of medicinal chemistry, 2018-07, Vol.61 (14), p.6002-6017

2018

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Discovery of a Potent Dual Son of Sevenless 1 (SOS1) and Epidermal Growth Factor Receptor (EGFR) Inhibitor for the Treatment of Prostate Cancer

Journal of medicinal chemistry, 2024-05, Vol.67 (9), p.7130-7145

2024

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Role of Electrostatic Interactions in Binding of Peptides and Intrinsically Disordered Proteins to Their Folded Targets. 1. NMR and MD Characterization of the Complex between the c‑Crk N‑SH3 Domain and the Peptide Sos

Biochemistry (Easton), 2014-10, Vol.53 (41), p.6473-6495

2014

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Identification and Characterization of Oncogenic SOS1 Mutations in Lung Adenocarcinoma

Molecular cancer research, 2019-04, Vol.17 (4), p.1002-1012

2019

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Germline gain-of-function mutations in SOS1 cause Noonan syndrome

Nature genetics, 2007-01, Vol.39 (1), p.70-74

2007

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Discovery of potent SOS1 inhibitors that block RAS activation via disruption of the RAS–SOS1 interaction

Targeting protein-protein interaction by small molecules

High-throughput screening identifies small molecules that bind to the RAS:SOS:RAS complex and perturb RAS signaling

Discovery of Sulfonamide-Derived Agonists of SOS1-Mediated Nucleotide Exchange on RAS Using Fragment-Based Methods

Severe Lymphatic Disorder Resolved With MEK Inhibition in a Patient With Noonan Syndrome and SOS1 Mutation

SOS1-inspired hydrocarbon-stapled peptide as a pan-Ras inhibitor

The RASopathies: developmental syndromes of Ras/MAPK pathway dysregulation

Membrane-dependent signal integration by the Ras activator Son of sevenless

Role of the histone domain in the autoinhibition and activation of the Ras activator Son of Sevenless

SOS1 gene overexpression increased salt tolerance in transgenic tobacco by maintaining a higher K +/Na + ratio

Small Molecule Binding Sites on the Ras:SOS Complex Can Be Exploited for Inhibition of Ras Activation

Direct inhibition of oncogenic KRAS by hydrocarbon-stapled SOS1 helices

Phospholipase D2-generated phosphatidic acid couples EGFR stimulation to Ras activation by Sos

Design, synthesis, and bioevaluation of SOS1 PROTACs derived from pyrido[2,3-d]pyrimidin-7-one-based SOS1 inhibitor

Allosteric KRas4B Can Modulate SOS1 Fast and Slow Ras Activation Cycles

Approach for targeting Ras with small molecules that activate SOS-mediated nucleotide exchange

Constitutive high-level SOS1 expression and absence of HKT1;1 expression in the salt-accumulating halophyte Salicornia dolichostachya

Discovery and Structure-Based Optimization of Benzimidazole-Derived Activators of SOS1-Mediated Nucleotide Exchange on RAS

Mechanism of SOS PR-domain autoinhibition revealed by single-molecule assays on native protein from lysate

Translational relevance of SOS1 targeting for KRAS‐mutant colorectal cancer

Discovery of Aminopiperidine Indoles That Activate the Guanine Nucleotide Exchange Factor SOS1 and Modulate RAS Signaling

Discovery of a Potent Dual Son of Sevenless 1 (SOS1) and Epidermal Growth Factor Receptor (EGFR) Inhibitor for the Treatment of Prostate Cancer

Role of Electrostatic Interactions in Binding of Peptides and Intrinsically Disordered Proteins to Their Folded Targets. 1. NMR and MD Characterization of the Complex between the c‑Crk N‑SH3 Domain and the Peptide Sos

Identification and Characterization of Oncogenic SOS1 Mutations in Lung Adenocarcinoma

Germline gain-of-function mutations in SOS1 cause Noonan syndrome

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