Development of combination therapies to maximize the impact of KRAS-G12C inhibitors in lung cancer

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Mechanisms of Resistance to KRASG12C Inhibitors

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Current therapy of KRAS-mutant lung cancer

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Tumor-Infiltrating Clonal Hematopoiesis

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Cell Type–Specific Adaptive Signaling Responses to KRASG12C Inhibition

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An Immunogenic Model of KRAS-Mutant Lung Cancer Enables Evaluation of Targeted Therapy and Immunotherapy Combinations

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KRAS G12C Mutations in NSCLC: From Target to Resistance

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Focal Adhesion Kinase (FAK) Inhibition Synergizes with KRAS G12C Inhibitors in Treating Cancer through the Regulation of the FAK–YAP Signaling

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The ERK mitogen-activated protein kinase signaling network: the final frontier in RAS signal transduction

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Defining and Targeting Adaptations to Oncogenic KRASG12C Inhibition Using Quantitative Temporal Proteomics

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Drugging the Undruggable: Advances on RAS Targeting in Cancer

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Targeting KRAS: The Elephant in the Room of Epithelial Cancers

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Overcoming Resistance to Drugs Targeting KRAS Mutation

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Sticking it to KRAS: Covalent Inhibitors Enter the Clinic

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Resistance looms for KRAS G12C inhibitors and rational tackling strategies

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KRAS: A Druggable Target in Colon Cancer Patients

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A proteomic and phosphoproteomic landscape of KRAS mutant cancers identifies combination therapies

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A review on graph neural networks for predicting synergistic drug combinations

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CRISPR–Cas9 Screening Identifies KRAS-Induced COX2 as a Driver of Immunotherapy Resistance in Lung Cancer

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Thinking Differently about Cancer Treatment Regimens

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Targeting KRAS G12C with Covalent Inhibitors

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A pan-KRAS inhibitor and its derived degrader elicit multifaceted anti-tumor efficacy in KRAS-driven cancers

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Prognostic and therapeutic impact of the KRAS G12C mutation in colorectal cancer

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Combining RAS(ON) G12C-selective inhibitor with SHP2 inhibition sensitises lung tumours to immune checkpoint blockade

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Targeting RAS mutants in malignancies: successes, failures, and reasons for hope

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Targeting MERTK and AXL in EGFR Mutant Non-Small Cell Lung Cancer

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Choosing the best first-line therapy: NSCLC with no actionable oncogenic driver

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Interactions between EGFR and EphA2 promote tumorigenesis through the action of Ephexin1

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Mutant KRAS at the heart of tumor immune evasion

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Inhibition of LSD1 Attenuates Oral Cancer Development and Promotes Therapeutic Efficacy of Immune Checkpoint Blockade and YAP/TAZ Inhibition

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Targeting RAS oncogenesis with SOS1 inhibitors

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An integrative pharmacogenomics analysis identifies therapeutic targets in KRAS-mutant lung cancer

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CRISPR Screening Identifies Mechanisms of Resistance to KRASG12C and SHP2 Inhibitor Combinations in Non-Small Cell Lung Cancer

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Spatial multiplex analysis of lung cancer reveals that regulatory T cells attenuate KRAS-G12C inhibitor–induced immune responses

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Overexpression of ABCB1 Associated With the Resistance to the KRAS-G12C Specific Inhibitor ARS-1620 in Cancer Cells

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Palmitoyl transferase ZDHHC20 promotes pancreatic cancer metastasis

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Biology, pathology, and therapeutic targeting of RAS

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Personalizing Medicine With Germline and Somatic Sequencing in Advanced Pancreatic Cancer: Current Treatments and Novel Opportunities

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Understand KRAS and the Quest for Anti-Cancer Drugs

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Inhibitor of the Nuclear Transport Protein XPO1 Enhances the Anticancer Efficacy of KRAS G12C Inhibitors in Preclinical Models of KRAS G12C–Mutant Cancers

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IL-6/ERK signaling pathway participates in type I IFN-programmed, unconventional M2-like macrophage polarization

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Metabolic synthetic lethality by targeting NOP56 and mTOR in KRAS-mutant lung cancer

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Molecular Biology and Therapeutic Perspectives for K-Ras Mutant Non-Small Cell Lung Cancers

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Micro-CT acquisition and image processing to track and characterize pulmonary nodules in mice

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Cytotoxicity of combinations of the pan-KRAS SOS1 inhibitor BAY-293 against pancreatic cancer cell lines

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A Pan-RAS Inhibitor with a Unique Mechanism of Action Blocks Tumor Growth and Induces Antitumor Immunity in Gastrointestinal Cancer

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Cytotoxicity of combinations of the pan-KRAS inhibitor BAY-293 against primary non-small lung cancer cells

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Covalent inhibitor targets KRasG12C: A new paradigm for drugging the undruggable and challenges ahead

Li, H., Qi, W.-L., Wang, Y., & Meng, L. (2021) · Genes & Diseases · doi:10.1016/j.gendis.2021.08.011 · Cited by 28

RAS‐targeted cancer therapy: Advances in drugging specific mutations

Liu, C., Ye, D., Yang, H., Chen, X., Su, Z., Li, X., Ding, M., & Liu, Y. (2023) · MedComm · doi:10.1002/mco2.285 · Cited by 25

Synergistic effects of FGFR1 and PLK1 inhibitors target a metabolic liability in KRAS‐mutant cancer

Zhang, Y., Liang, S., Saliakoura, M., Yang, H., Vassella, E., Konstantinidou, G., Tschan, M. P., Hegedűs, B., Zhao, L., Gao, Y., et al. (2021) · EMBO Molecular Medicine · doi:10.15252/emmm.202013193 · Cited by 23

Characterisation of a novel KRAS G12C inhibitor ASP2453 that shows potent anti-tumour activity in KRAS G12C-mutated preclinical models

Nakayama, A., Nagashima, T., Nishizono, Y., Kuramoto, K., Mori, K., Homboh, K., Yuri, M., & Shimazaki, M. (2021) · British Journal of Cancer · doi:10.1038/s41416-021-01629-x · Cited by 24

Covalent inhibitors of the GTPase KRASG12C: a review of the patent literature

Kettle, J. G., & Cassar, D. J. (2020) · Expert Opinion on Therapeutic Patents · doi:10.1080/13543776.2020.1709443 · Cited by 23

Direct GDP-KRAS G12C inhibitors and mechanisms of resistance: the tip of the iceberg

Rosen, J. C., Sacher, A. G., & Tsao, M. (2023) · Therapeutic Advances in Medical Oncology · doi:10.1177/17588359231160141 · Cited by 22

Inhalable Bottlebrush Polymer Bioconjugates as Vectors for Efficient Pulmonary Delivery of Oligonucleotides

Fang, Y., Cai, J., Ren, M., Zhong, T., Wang, D., & Zhang, K. (2023) · ACS Nano · doi:10.1021/acsnano.3c08660 · Cited by 21

Updates in the molecular pathology of non-small cell lung cancer

Paver, E. C., O'Toole, S. A., Cheng, X. M., Mahar, A. M., & Cooper, W. A. (2021) · Seminars in Diagnostic Pathology · doi:10.1053/j.semdp.2021.04.001 · Cited by 21

Signature-driven repurposing of Midostaurin for combination with MEK1/2 and KRASG12C inhibitors in lung cancer

Macaya, I., Román, M., Welch, C., Entrialgo‐Cadierno, R., Salmón, M., Santos, A., Feliu, I., Kovalski, J. R., López, I., Rodríguez‐Remírez, M., et al. (2023) · Nature Communications · doi:10.1038/s41467-023-41828-z · Cited by 22

Inhibition of RAS: proven and potential vulnerabilities

Zuberi, M., Khan, I., & O’Bryan, J. P. (2020) · Biochemical Society Transactions · doi:10.1042/bst20190023 · Cited by 20

Targeting PI3Kα overcomes resistance to KRasG12C inhibitors mediated by activation of EGFR and/or IGF1R

Qi, W.-L., Li, H.-Y., Wang, Y., Xu, L., Deng, J.-T., Zhang, X., Wang, Y.-X., & Meng, L.-H. (2023) · Acta Pharmacologica Sinica · doi:10.1038/s41401-022-01015-0 · Cited by 19

Prognostic Role of KRAS G12C Mutation in Non-Small Cell Lung Cancer: A Systematic Review and Meta-Analysis

Wankhede, D., Bontoux, C., Grover, S., & Hofman, P. M. (2023) · Diagnostics · doi:10.3390/diagnostics13193043 · Cited by 19

Targeted therapies prime oncogene-driven lung cancers for macrophage-mediated destruction

Vaccaro, K., Allen, J., Whitfield, T. W., Maoz, A., Reeves, S., Velarde, J., Yang, D., Meglan, A., Ribeiro, J., Blandin, J., et al. (2024) · Journal of Clinical Investigation · doi:10.1172/jci169315 · Cited by 19

Current status of KRAS G12C inhibitors in NSCLC and the potential for combination with anti-PD-(L)1 therapy: a systematic review

Zhang, F., Wang, B., Wu, M., Zhang, L., & Ji, M. Q. (2025) · Frontiers in Immunology · doi:10.3389/fimmu.2025.1509173 · Cited by 20

KRAS mutated NSCLC: past, present, and future directions in a rapidly evolving landscape

Frisch, A., Martin, E., Kim, S. Y., Riess, J. W., Sen, T., & Karim, N. A. (2025) · The Oncologist · doi:10.1093/oncolo/oyaf153 · Cited by 24

Targeting KRAS in pancreatic cancer: Emerging therapeutic strategies

Khan, S. U., Budamagunta, V., & Zhou, D. (2023) · Advances in cancer research · doi:10.1016/bs.acr.2023.02.004 · Cited by 21

Lung cancer immunotherapy in 2025: where we stand and what comes next?

Han, J., Yang, Z., & Hai, Z. (2026) · Frontiers in Immunology · doi:10.3389/fimmu.2025.1728163 · Cited by 17

A Deep-Learning Proteomic-Scale Approach for Drug Design

Overhoff, B., Falls, Z., Mangione, W., & Samudrala, R. (2021) · Pharmaceuticals · doi:10.3390/ph14121277 · Cited by 16

Novel approaches for the development of direct KRAS inhibitors: structural insights and drug design

Haider, K., Sharma, A., Yar, M. S., Yakkala, P. A., Shafi, S., & Kamal, Ä. (2022) · Expert Opinion on Drug Discovery · doi:10.1080/17460441.2022.2029842 · Cited by 16

Conquering oncogenic KRAS and its bypass mechanisms

Hou, P., & Wang, Y. (2022) · Theranostics · doi:10.7150/thno.71260 · Cited by 18

Abstract B073: Development of combination therapies to potentiate the impact of KRAS-G12C inhibitors in lung cancer

Molina‐Arcas, M., Moore, C., Rana, S., van Maldegem, F., Mugarza, E., Romero-Clavijo, P., Horswell, S. D., Hancock, D. C., & Downward, J. (2019) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.targ-19-b073

Dual inhibition of GTP-bound KRAS and mTOR in lung adenocarcinoma and squamous cell carcinoma harboring KRAS G12C

Ito, M., Miyata, Y., Hirano, S., Morihara, N., Takemoto, M., Irisuna, F., Kushitani, K., Suda, K., Soh, J., Takeshima, Y., et al. (2025) · Cell Communication and Signaling · doi:10.1186/s12964-025-02187-y · Cited by 6

15 Identification of new combination therapies for lung cancer tumours harbouring KRAS mutations

Molina‐Arcas, M., Moore, C., Rana, S., van Maldegem, F., Horswell, S. D., Hancock, D. C., & Downward, J. (2018) · ESMO Open · doi:10.1136/esmoopen-2018-eacr25.15 · Cited by 1

Abstract 2987: Identification of new combination therapies for lung tumors harboring KRAS mutations

Molina‐Arcas, M., Moore, C., Rana, S., van Maldegem, F., Horswell, S. D., Hancock, D. C., & Downward, J. (2018) · Cancer Research · doi:10.1158/1538-7445.am2018-2987

KRAS G12C NSCLC Models Are Sensitive to Direct Targeting of KRAS in Combination with PI3K Inhibition

Misale, S., Fatherree, J. P., Cortez, E., Li, C., Bilton, S., Timonina, D., Myers, D. T., Lee, D., Gomez-Caraballo, M., Greenberg, M., et al. (2019) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-18-0368 · Cited by 259