ArticleACS medicinal chemistry letters2017
Covalent Guanosine Mimetic Inhibitors of G12C KRAS.
Article in ACS medicinal chemistry letters, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 36 papers.
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Who cites it
36 citing papers in PubMed, 71 citations in OpenAlex.
- ELOVL6 activity attenuation induces mutant KRAS degradation.Nature chemical biology · 2026Article
- Targeting oncogenic K-RAS mutants with small-molecule degrader XMU-MP-9 through NEDD4-1.Acta pharmaceutica Sinica. B · 2026Article
- RAS Pathway Inhibitors Combined with Targeted Agents Are Active in Patient-Derived Spheroids with Oncogenic KRAS Variants from Multiple Cancer Types.Cancer research communications · 2025Article
- A New Dawn for Targeted Cancer Therapy: Small Molecule Covalent Binding Inhibitor Targeting K-Ras (G12C).Current medicinal chemistry · 2025Review
- New insights into protein-protein interaction modulators in drug discovery and therapeutic advance.Signal transduction and targeted therapy · 2024Review
- Recent advances in targeting the "undruggable" proteins: from drug discovery to clinical trials.Signal transduction and targeted therapy · 2023Review
- Article
- Drugging KRAS: current perspectives and state-of-art review.Journal of hematology & oncology · 2022Review
- Therapeutic Targeting the Allosteric Cysteinome of RAS and Kinase Families.Journal of molecular biology · 2022Review
- KRAS G12C Mutations in NSCLC: From Target to Resistance.Cancers · 2021Review
- GLOBAL AND TARGETED PROFILING OF GTP-BINDING PROTEINS IN BIOLOGICAL SAMPLES BY MASS SPECTROMETRY.Mass spectrometry reviews · 2021Review
- Approaches to inhibiting oncogenic K-Ras.Small GTPases · 2021Review
- Inhibition of Nonfunctional Ras.Cell chemical biology · 2021Review
- Characterization With KRAS Mutant Is a Critical Determinant in Immunotherapy and Other Multiple Therapies for Non-Small Cell Lung Cancer.Frontiers in oncology · 2021Review
- Structure-based inhibitor design of mutant RAS proteins-a paradigm shift.Cancer metastasis reviews · 2020Review
- NMR in integrated biophysical drug discovery for RAS: past, present, and future.Journal of biomolecular NMR · 2020Review
- The Frequency of Ras Mutations in Cancer.Cancer research · 2020Review
- KRasG12C inhibitors in clinical trials: a short historical perspective.RSC medicinal chemistry · 2020Review
- Covalent Inhibitors Allosterically Block the Activation of Rho Family Proteins and Suppress Cancer Cell Invasion.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2020Article
- KRAS as a druggable target in NSCLC: Rising like a phoenix after decades of development failures.Cancer treatment reviews · 2020Review
Corrections and comments
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Authors and funding
12 authors at 5 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Ras proteins are members of a large family of GTPase enzymes that are commonly mutated in cancer where they act as dominant oncogenes. We previously developed an irreversible guanosine-derived inhibitor, SML-8-73-1, of mutant G12C RAS that forms a covalent bond with cysteine 12. Here we report exploration of the structure-activity relationships (SAR) of hydrolytically stable analogues of SML-8-73-1 as covalent G12C KRAS inhibitors. We report the discovery of difluoromethylene bisphosphonate analogues such as compound
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Registered trials
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.