ArticleJournal of medicinal chemistry2022
Design and Discovery of MRTX0902, a Potent, Selective, Brain-Penetrant, and Orally Bioavailable Inhibitor of the SOS1:KRAS Protein-Protein Interaction.
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Article in Journal of medicinal chemistry, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 44 papers, 1 of them a synthesis that pooled it.
0numbers the graph read from it
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44citing papers in PubMed, 1 pooled it
7.0field-weighted citation impact, top 2% of its field
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
44 citing papers in PubMed, 1 synthesis or guideline pooled it, 88 citations in OpenAlex.
- Current status of KRAS G12C inhibitors in NSCLC and the potential for combination with anti-PD-(L)1 therapy: a systematic review.Frontiers in immunology · 2025Pooled it
- Review
- Structural and Biophysical Characterization of Aminobenzo[ACS medicinal chemistry letters · 2026Article
- The SOS1 Inhibitor BI 1701963 as Monotherapy or in Combination with Trametinib in Patients with KRAS Mutation-Positive Solid Tumors.Clinical cancer research : an official journal of the American Association for Cancer Research · 2026Article
- Targeted therapeutic strategies forTranslational lung cancer research · 2026Review
- Fibroblast-mediated KRAS activation in double-negative prostate cancer.Cell death & disease · 2026Article
- SOS1: tracking the evolving path from promising to actionable therapeutic target in RAS-dependent cancers.Molecular cancer · 2026Review
- Disrupting the KRAS-SOS1 protein-protein interaction: mechanistic rationale for pan-KRAS pathway suppression and combination therapy.Frontiers in chemistry · 2026Review
- Unravelling Resistance: Integrating Metabolism, Epigenetics, Immunology, and Proteostasis in Strategies against Kirsten Rat Sarcoma Viral Oncogene Homolog-mutant Colorectal Cancer.International journal of biological sciences · 2026Review
- Wild-type KRAS activation drives evasion of interferon-mediated immunity and resistance to immunotherapy in hepatocellular carcinoma.Nature communications · 2025Article
- Focused Structure-Based Virtual Screening Identifies Novel Inhibitors of SOS1.ACS medicinal chemistry letters · 2025Article
- Novel paradigms in KRAS targeting: Unveiling strategies to combat drug resistance.Chinese medical journal · 2025Review
- Design and Development of Potent SOS1 Inhibitors with Effective Antitumor ActivitiesACS medicinal chemistry letters · 2025Article
- Identification of Novel 2‑(Azetidin-3-ylamino)-nicotinamide Derivatives as Potent KRAS::SOS1 Inhibitors.ACS medicinal chemistry letters · 2025Article
- Optimizing blood-brain barrier permeability in KRAS inhibitors: A structure-constrained molecular generation approach.Journal of pharmaceutical analysis · 2025Article
- In Silico Identification of Putative Allosteric Pockets and Inhibitors for the KRASG13D-SOS1 Complex in Cancer Therapy.International journal of molecular sciences · 2025Article
- SOS1 inhibitor BI-3406 shows in vivo antitumor activity akin to genetic ablation and synergizes with a KRASProceedings of the National Academy of Sciences of the United States of America · 2025Article
- Exploiting Solvent Exposed Salt-Bridge Interactions for the Discovery of Potent Inhibitors of SOS1 Using Free-Energy Perturbation Simulations.ACS medicinal chemistry letters · 2025Article
- Exploring the pathway: clinical utility and open challenges of targeting BRAF alterations in biliary tract cancers and gastrointestinal malignancies.ESMO gastrointestinal oncology · 2025Review
- Discovery of Small Molecules that Bind to Son of Sevenless 2 (SOS2).Journal of medicinal chemistry · 2025Article
Corrections and comments
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Authors and funding
26 authors at 1 institution in 1 country.
John M KetchamMirati Therapeutics, 3545 Cray Court, San Diego, California 92121, United States.ORCID 0000-0001-5011-9593
Jacob HalingMirati Therapeutics, 3545 Cray Court, San Diego, California 92121, United States.
Shilpi KhareMirati Therapeutics, 3545 Cray Court, San Diego, California 92121, United States.
Vickie BowcutMirati Therapeutics, 3545 Cray Court, San Diego, California 92121, United States.
David M BriereMirati Therapeutics, 3545 Cray Court, San Diego, California 92121, United States.
Aaron C BurnsMirati Therapeutics, 3545 Cray Court, San Diego, California 92121, United States.
Robin J GunnMirati Therapeutics, 3545 Cray Court, San Diego, California 92121, United States.
Anthony IvetacMirati Therapeutics, 3545 Cray Court, San Diego, California 92121, United States.
Jon KuehlerMirati Therapeutics, 3545 Cray Court, San Diego, California 92121, United States.
Svitlana KulykMirati Therapeutics, 3545 Cray Court, San Diego, California 92121, United States.
Jade LaguerMirati Therapeutics, 3545 Cray Court, San Diego, California 92121, United States.
J David LawsonMirati Therapeutics, 3545 Cray Court, San Diego, California 92121, United States.ORCID 0000-0002-5232-4539
Krystal MoyaMirati Therapeutics, 3545 Cray Court, San Diego, California 92121, United States.
Natalie NguyenMirati Therapeutics, 3545 Cray Court, San Diego, California 92121, United States.
Lisa RahbaekMirati Therapeutics, 3545 Cray Court, San Diego, California 92121, United States.
Barbara SaechaoMirati Therapeutics, 3545 Cray Court, San Diego, California 92121, United States.
Christopher R SmithMirati Therapeutics, 3545 Cray Court, San Diego, California 92121, United States.
Niranjan SudhakarMirati Therapeutics, 3545 Cray Court, San Diego, California 92121, United States.
Nicole C ThomasMirati Therapeutics, 3545 Cray Court, San Diego, California 92121, United States.
Laura VegarMirati Therapeutics, 3545 Cray Court, San Diego, California 92121, United States.
Darin VanderpoolMirati Therapeutics, 3545 Cray Court, San Diego, California 92121, United States.
Xiaolun WangMirati Therapeutics, 3545 Cray Court, San Diego, California 92121, United States.
Larry YanMirati Therapeutics, 3545 Cray Court, San Diego, California 92121, United States.
Peter OlsonMirati Therapeutics, 3545 Cray Court, San Diego, California 92121, United States.
James G ChristensenMirati Therapeutics, 3545 Cray Court, San Diego, California 92121, United States.
Matthew A MarxMirati Therapeutics, 3545 Cray Court, San Diego, California 92121, United States.ORCID 0000-0003-2351-4787
Mirati Therapeutics (United States) · US
Funding
User Training and OutreachP30GM124165 · NIGMS · CORNELL UNIVERSITY · PI MALCOLM S. CAPEL · 2018 to 2026
$34.2MPixel Array Detector for Macromolecular CrystallographyS10OD021527 · OD · CORNELL UNIVERSITY · PI EALICK, STEVEN E · 2016 to 2016
$2.0MNIGMS NIH HHS P30 GM124165NIH HHS S10 OD021527
Abstract
SOS1 is one of the major guanine nucleotide exchange factors that regulates the ability of KRAS to cycle through its "on" and "off" states. Disrupting the SOS1:KRAS
Indexed as
BrainProto-Oncogene Proteins p21(ras)AcetonitrilesAnimalsCell Line, TumorHumansMiceMutationPiperazinesPyrimidinesSOS1 ProteinAcetonitrilesadagrasibKRAS protein, humanPiperazinesProto-Oncogene Proteins p21(ras)PyrimidinesSOS1 Protein
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LicenceCC BY
Read underepoch 390
Registered trials
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.