ArticleScience (New York, N.Y.)2023
Chemical remodeling of a cellular chaperone to target the active state of mutant KRAS.
Open access · greenAbstract read
In one paragraph
Article in Science (New York, N.Y.), 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 135 papers.
0numbers the graph read from it
0cells of the map it votes in
135citing papers in PubMed
32.5field-weighted citation impact, top 1% of its field
What it found
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The trial behind it
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
135 citing papers in PubMed, 211 citations in OpenAlex.
- Acquired resistance to the RAS(ON) multi-selective inhibitor daraxonrasib guides rational combination therapy strategies in pancreatic cancer.Nature medicine · 2026Trial
- Glecirasib in KRASNature medicine · 2025Trial
- Dermatologic Toxicities Associated With Novel Pan-RAS/RAF Inhibitors.Journal of cutaneous pathology · 2026Article
- Molecular Mechanisms and Therapeutic Advances in KRAS G12C-Mutant Non-Small Cell Lung Cancer: Toward Mechanism-Guided Longitudinal Management.Cancer innovation · 2026Review
- Article
- Activity and specificity of KRAS variants-directed Revolution Medicines Company (RMC) compounds for pleural effusion-derived non-small cell lung cancer cell lines.Translational lung cancer research · 2026Article
- A Versatile DNA-Encoded Library Platform for the Discovery of Highly Cooperative Chemical Inducers of Proximity.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2026Article
- Cell type-selective targeting by heterobifunctional protein binders via in-cell enrichment.Nature communications · 2026Article
- The Role of KRAS in Non-Small Cell Lung Cancer: From Molecular Background to Precision Medicine.International journal of molecular sciences · 2026Review
- The Landmark Series: Mutation-Based Therapy of Pancreatic Cancer.Annals of surgical oncology · 2026Review
- A bivalent molecular glue linking lysine acetyltransferases to oncogene-induced cell death.Cell · 2026Article
- Monovalent Nondegrading Molecular Glues: An Updated Overview of Emerging Mechanisms and Therapeutic Development.Pharmaceuticals (Basel, Switzerland) · 2026Review
- KRAS Inhibitor-Induced Cancer Cell Death Enhances Sensitivity to Immune-Mediated Bystander Killing of Drug-Resistant Subclones.Cancer research · 2026Article
- Genetic Drivers of Sensitivity or Resistance to RAS(ON) Multiselective Inhibitors in NRAS-Mutated Melanoma.Cancer research · 2026Article
- Targeted KRASG12V Degradation In Vivo Elicits Lung Adenocarcinoma Regression with Subsequent Relapse from Dysregulated Proteolysis.Cancer research · 2026Article
- Brønsted-basic small molecules activate GTP hydrolysis in KRAS-Q61 mutants.Nature chemical biology · 2026Article
- Ubiquitin family as novel protein partners for molecular glues.npj drug discovery · 2026Review
- Systematic Targeting of Protein Complexes with Molecular COUPLrs.Cancer discovery · 2026Article
- Evolution of KRAS molecular glues: from allele-selective to Pan-RAS and protein-protein interaction modulators.Acta pharmacologica Sinica · 2026Review
- Pancreatic Cancer: Translating Tumor Biology into Actionability.Cancer discovery · 2026Review
75 more citing papers are in PubMed but not listed here.
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
36 authors at 2 institutions in 1 country.
Christopher J Schulze *Department of Biology, Revolution Medicines, Inc., Redwood City, CA 94063, USA.ORCID 0009-0005-6736-871X
Kyle J Seamon *Department of Biology, Revolution Medicines, Inc., Redwood City, CA 94063, USA.ORCID 0009-0005-5028-3752
Yulei Zhao *Human Oncology and Pathogenesis Program, Memorial Sloan Kettering Cancer, New York, NY 10065, USA.ORCID 0000-0002-2242-3843
Yu C YangDepartment of Biology, Revolution Medicines, Inc., Redwood City, CA 94063, USA.ORCID 0000-0001-8318-1174
Jim CreggDepartment of Discovery Chemistry, Revolution Medicines, Inc., Redwood City, CA 94063, USA.
Dongsung KimHuman Oncology and Pathogenesis Program, Memorial Sloan Kettering Cancer, New York, NY 10065, USA.ORCID 0000-0003-4152-628X
Aidan TomlinsonDepartment of Discovery Chemistry, Revolution Medicines, Inc., Redwood City, CA 94063, USA.ORCID 0000-0002-9663-773X
Tiffany J ChoyDepartment of Biology, Revolution Medicines, Inc., Redwood City, CA 94063, USA.ORCID 0000-0001-6501-2123
Zhican WangDepartment of Non-clinical Development and Clinical Pharmacology, Revolution Medicines, Inc., Redwood City, CA 94063, USA.
Ben SangHuman Oncology and Pathogenesis Program, Memorial Sloan Kettering Cancer, New York, NY 10065, USA.ORCID 0000-0002-4817-8356
Yasin PourfarjamHuman Oncology and Pathogenesis Program, Memorial Sloan Kettering Cancer, New York, NY 10065, USA.
Jessica LucasHuman Oncology and Pathogenesis Program, Memorial Sloan Kettering Cancer, New York, NY 10065, USA.ORCID 0000-0002-6462-7975
Antonio Cuevas-NavarroHuman Oncology and Pathogenesis Program, Memorial Sloan Kettering Cancer, New York, NY 10065, USA.ORCID 0000-0001-6208-6944
Carlos Ayala-SantosHuman Oncology and Pathogenesis Program, Memorial Sloan Kettering Cancer, New York, NY 10065, USA.ORCID 0009-0000-7583-0023
Alberto VidesHuman Oncology and Pathogenesis Program, Memorial Sloan Kettering Cancer, New York, NY 10065, USA.ORCID 0009-0009-7273-2167
Chuanchuan LiHuman Oncology and Pathogenesis Program, Memorial Sloan Kettering Cancer, New York, NY 10065, USA.ORCID 0000-0003-3699-5823
Abby MarquezDepartment of Discovery Chemistry, Revolution Medicines, Inc., Redwood City, CA 94063, USA.ORCID 0000-0001-5104-2823
Mengqi ZhongDepartment of Discovery Chemistry, Revolution Medicines, Inc., Redwood City, CA 94063, USA.ORCID 0000-0003-0525-6999
Vidyasiri VemulapalliDepartment of Biology, Revolution Medicines, Inc., Redwood City, CA 94063, USA.ORCID 0000-0002-3368-4766
Caroline WellerDepartment of Biology, Revolution Medicines, Inc., Redwood City, CA 94063, USA.
Andrea GouldDepartment of Biology, Revolution Medicines, Inc., Redwood City, CA 94063, USA.
Daniel M WhalenDepartment of Discovery Chemistry, Revolution Medicines, Inc., Redwood City, CA 94063, USA.
Anthony SalvadorDepartment of Discovery Chemistry, Revolution Medicines, Inc., Redwood City, CA 94063, USA.ORCID 0009-0000-3551-4608
Anthony MilinDepartment of Discovery Chemistry, Revolution Medicines, Inc., Redwood City, CA 94063, USA.ORCID 0000-0002-1923-7441
Mae Saldajeno-ConcarDepartment of Discovery Chemistry, Revolution Medicines, Inc., Redwood City, CA 94063, USA.
Nuntana DinglasanDepartment of Biology, Revolution Medicines, Inc., Redwood City, CA 94063, USA.
Anqi ChenDepartment of Discovery Chemistry, Revolution Medicines, Inc., Redwood City, CA 94063, USA.ORCID 0000-0002-3259-5868
Jim EvansDepartment of Biology, Revolution Medicines, Inc., Redwood City, CA 94063, USA.
John E KnoxDepartment of Discovery Chemistry, Revolution Medicines, Inc., Redwood City, CA 94063, USA.
Elena S KoltunDepartment of Discovery Chemistry, Revolution Medicines, Inc., Redwood City, CA 94063, USA.ORCID 0009-0005-8720-9097
Mallika SinghDepartment of Biology, Revolution Medicines, Inc., Redwood City, CA 94063, USA.
Robert NicholsDepartment of Biology, Revolution Medicines, Inc., Redwood City, CA 94063, USA.
David WildesDepartment of Biology, Revolution Medicines, Inc., Redwood City, CA 94063, USA.
Adrian L GillDepartment of Discovery Chemistry, Revolution Medicines, Inc., Redwood City, CA 94063, USA.
Jacqueline A M SmithDepartment of Biology, Revolution Medicines, Inc., Redwood City, CA 94063, USA.ORCID 0000-0001-5028-8725
Piro LitoHuman Oncology and Pathogenesis Program, Memorial Sloan Kettering Cancer, New York, NY 10065, USA.ORCID 0000-0003-2196-3503
Revolution Medicines (United States) · USMemorial Sloan Kettering Cancer Center · US
Funding
X-RAY CRYSTALLOGRAPHYP30CA008748 · NCI · SLOAN-KETTERING INSTITUTE FOR CANCER RES · PI Nicholas D Socci · 1985 to 2026
$347.4MThe Role of Focal Oncogene Amplifications in Lung CancerP01CA129243 · NCI · SLOAN-KETTERING INST CAN RESEARCH · PI Piro Lito · 2007 to 2026
$31.2MDissecting KRAS oncoprotein signaling with small molecule inhibitorsR01CA230745 · NCI · SLOAN-KETTERING INST CAN RESEARCH · PI Piro Lito · 2018 to 2026
$3.8MStudies on the effects of a novel intermittent therapy on intratumoral clonal architecture and resistanceR01CA230267 · NCI · SLOAN-KETTERING INST CAN RESEARCH · PI LITO, PIRO · 2019 to 2023
$2.0MMechanisms of adaptation and resistance to emerging therapies for lung cancerR01CA279264 · NCI · SLOAN-KETTERING INST CAN RESEARCH · PI Piro Lito · 2023 to 2026
$2.0MNCI NIH HHS P30 CA008748NCI NIH HHS R01 CA230267NCI NIH HHS R01 CA230745NCI NIH HHS R01 CA279264
Abstract
The discovery of small-molecule inhibitors requires suitable binding pockets on protein surfaces. Proteins that lack this feature are considered undruggable and require innovative strategies for therapeutic targeting.
Indexed as
Biological ProductsCyclophilin AImmunophilinsMolecular ChaperonesNeoplasmsProto-Oncogene Proteins p21(ras)CysteineHumansSignal TransductionBiological ProductsCyclophilin ACysteineImmunophilinsKRAS protein, humanMolecular ChaperonesProto-Oncogene Proteins p21(ras)
Identifiers
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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.