One Step at a Time — Clinical Evidence That KRAS Is Indeed Druggable

K-Ras(G12C) inhibitors allosterically control GTP affinity and effector interactions

Ostrem, J. M., Peters, U., Sos, M. L., Wells, J. A., & Shokat, K. M. (2013) · Nature · doi:10.1038/nature12796 · Cited by 2,557 · see citing works

The Clinical KRAS(G12C) Inhibitor AMG 510 Drives Anti-Tumour Immunity

Canon, J., Rex, K., Saiki, A. Y., Mohr, C., Cooke, K., Bagal, D., Gaida, K., Holt, T., Knutson, C. G., Koppada, N., et al. (2019) · Nature · doi:10.1038/s41586-019-1694-1 · Cited by 2,277 · see citing works

KRAS ^G12C Inhibition with Sotorasib in Advanced Solid Tumors

Hong, D. S., Fakih, M. G., Strickler, J. H., Desai, J., Durm, G. A., Shapiro, G. I., Falchook, G. S., Price, T. J., Sacher, A., Denlinger, C. S., et al. (2020) · New England Journal of Medicine · doi:10.1056/nejmoa1917239 · Cited by 1,733 · see citing works

The KRASG12C Inhibitor MRTX849 Provides Insight toward Therapeutic Susceptibility of KRAS-Mutant Cancers in Mouse Models and Patients

Hallin, J., Engstrom, L. D., Hargis, L., Calinisan, A., Aranda, R., Briere, D. M., Sudhakar, N., Bowcut, V., Baer, B. R., Ballard, J. A., et al. (2020) · Cancer Discovery · doi:10.1158/2159-8290.cd-19-1167 · Cited by 1,304 · see citing works

RAS-targeted therapies: is the undruggable drugged?

Moore, A. R., Rosenberg, S. C., McCormick, F., & Malek, S. (2020) · Nature Reviews Drug Discovery · doi:10.1038/s41573-020-0068-6 · Cited by 1,103 · see citing works

EGFR Blockade Reverts Resistance to KRASG12C Inhibition in Colorectal Cancer.

Amodio, V., Yaeger, R., Arcella, P., Cancelliere, C., Lamba, S., Lorenzato, A., Arena, S., Montone, M., Mussolin, B., Bian, Y., et al. (2020) · Cancer Discovery · doi:10.1158/2159-8290.cd-20-0187 · Cited by 504 · see citing works

Vertical Pathway Inhibition Overcomes Adaptive Feedback Resistance to KRASG12C Inhibition

Ryan, M. B., Fece de la Cruz, F., Phat, S., Myers, D. T., Wong, E., Shahzade, H. A., Hong, C. B., & Corcoran, R. B. (2020) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-19-3523 · Cited by 496 · see citing works

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 · see citing works

RAS, wanted dead or alive: Advances in targeting RAS mutant cancers

Stalnecker, C. A., & Der, C. J. (2020) · Science Signaling · doi:10.1126/scisignal.aay6013 · Cited by 90 · see citing works

Tumor biomarkers for diagnosis, prognosis and targeted therapy

Zhou, Y., Tao, L., Qiu, J., Xu, J., Yang, X., Zhang, Y., Tian, X., Guan, X., Cen, X., & Zhao, Y. (2024) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-024-01823-2 · Cited by 772 · see citing works

Drugging KRAS: Current perspectives and state-of-art review

Parikh, K., Banna, G., Liu, S. V., Friedlaender, A., Desai, A., Subbiah, V., & Addeo, A. (2022) · Journal of Hematology & Oncology · doi:10.1186/s13045-022-01375-4 · Cited by 164 · see citing works

Annual review of KRAS inhibitors in 2022

Wang, H., Chi, L., Yu, F., Dai, H., Gao, C., Si, X., Wang, Z., Liu, L., Zheng, J., Shan, L., et al. (2023) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2023.115124 · Cited by 48 · see citing works

Research progress on KRAS mutations in colorectal cancer

Cefalì, M., Epistolio, S., Palmarocchi, M. C., Frattini, M., & Dosso, S. D. (2021) · Journal of Cancer Metastasis and Treatment · doi:10.20517/2394-4722.2021.61 · Cited by 47 · see citing works

Precision Medicine in Oncology: A Review of Multi-Tumor Actionable Molecular Targets with an Emphasis on Non-Small Cell Lung Cancer

Stein, M. K., Oluoha, O., Patel, K., & Vanderwalde, A. M. (2021) · Journal of Personalized Medicine · doi:10.3390/jpm11060518 · Cited by 33 · see citing works

Emerging RAS-directed therapies for cancer

Conroy, M. R., Cowzer, D., Kölch, W., & Duffy, A. G. (2021) · Cancer Drug Resistance · doi:10.20517/cdr.2021.07 · Cited by 22 · see citing works

First-in-Humans PET Imaging ofKRASG12CMutation Status in Non–Small Cell Lung and Colorectal Cancer Patients Using [18F]PFPMD

Li, X., Ye, J., Wang, J., Quan, Z., Li, G., Ma, W., Zhang, M., Yang, W., Wang, J., Ma, T., et al. (2023) · Journal of Nuclear Medicine · doi:10.2967/jnumed.123.265715 · Cited by 19 · see citing works

Pharmacogenomic‐Guided Therapy in Colorectal Cancer

Diasio, R. B., Innocenti, F., & Offer, S. M. (2021) · Clinical Pharmacology & Therapeutics · doi:10.1002/cpt.2334 · Cited by 20 · see citing works

Degradation of Rat Sarcoma Proteins Targeting the Post-Translational Prenyl Modifications via Cascade Azidation/Fluorination and Click Reaction

Zhou, H., Gan, Y., Li, Y., Chen, X., Guo, Y., & Wang, R. (2023) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.2c01721 · Cited by 16 · see citing works

Open Structural Data in Precision Medicine

Nussinov, R., Jang, H., Nir, G., Tsai, C., & Cheng, F. (2022) · Annual Review of Biomedical Data Science · doi:10.1146/annurev-biodatasci-122220-012951 · Cited by 11 · see citing works

Beyond Conventional: The New Horizon of Targeted Therapy for the Treatment of Advanced Non Small Cell Lung Cancer

Tartarone, A., Lapadula, V., Micco, C. D., Rossi, G., Ottanelli, C., Marini, A., Giorgione, R., Ferrari, K., Catalano, M., Voltolini, L., et al. (2021) · Frontiers in Oncology · doi:10.3389/fonc.2021.632256 · Cited by 11 · see citing works

KRAS Mutation Status in Relation to Clinicopathological Characteristics of Romanian Colorectal Cancer Patients

Avădănei, E.-R., Căruntu, I.-D., Nucă, I., Balan, R. A., Lozneanu, L., Giuşcă, S. E., Pricope, D. L., Dascălu, C. G., & Amălinei, C. (2025) · Current Issues in Molecular Biology · doi:10.3390/cimb47020120 · Cited by 5 · see citing works

The impact of RAS mutation on the treatment strategy of colorectal cancer

Pirvu, E. E., Severin, E. M., Niţă, I., & Toma, Ş. A. (2023) · Medicine and Pharmacy Reports · doi:10.15386/mpr-2408 · Cited by 4 · see citing works

Personalized Medicine in Oncology

Vanderwalde, A. M. (2022) · MDPI eBooks · doi:10.3390/books978-3-0365-2820-5 · Cited by 4 · see citing works

Proteolysis-targeting chimera (PROTAC) in cancer: design principles and applications on “undruggable” targets

Lu, X., Qin, J., Dong, S., Yuan, Y., Zhang, Z., Zhang, B., Chen, X., Gan, X., Liang, H., & Liu, F. (2026) · Biomarker Research · doi:10.1186/s40364-026-00937-9 · Cited by 3 · see citing works

KRAS and MYC synergistic inhibition: a powerful strategy targeting KRAS-mutant cancers

Yan, M., Liu, K., Xu, J., Liu, Y., Ji, L., & Zhang, S. (2026) · Molecular Cancer · doi:10.1186/s12943-026-02659-w · Cited by 1 · see citing works

Sotorasib als mögliche neue zielgerichtete Therapie KRAS-G12C-mutierter Tumoren

Marnau, H., Spory, L., & Dunst, J. (2021) · InFo Hämatologie + Onkologie · doi:10.1007/s15004-021-8640-8

Discovery of a novel drug using lipid-based formulation targeting G12D-mutated KRAS4B through non-covalent bondsPreprint

Lu, H., Hu, Z., Faraudo, J., & Martı́, J. (2023) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2023.04.05.535682 · Cited by 1 · see citing works

Characterization and economic burden of KRASG12C-mutant lung cancer in real-world Spanish practice: a retrospective observational study (SILK study)

Reguart, N., Sampietro-Colom, L., Juan, Ó., Aguiló, M., Arriola, E., Sánchez, J., Fernández-Barceló, C., Abbas, I., Gomez, C. L., Botella, X., et al. (2025) · Lung Cancer · doi:10.1016/j.lungcan.2025.108677

A Pan-KRAS-Targeted PET Probe for Noninvasive Quantitative Imaging of KRAS Expression

Guo, Q., Wang, D., Du, J., 刘金剑, Yang, L., & Liu, J. (2026) · Molecular Pharmaceutics · doi:10.1021/acs.molpharmaceut.6c01137

BindingDB Entry 50019814: Annual review of KRAS inhibitors in 2022.

BindingDB (2024) · UC San Diego · doi:10.7270/q2sx6jm1

Targeting KRAS for cancer therapy

Jia, J., Liu, R., Adamide, T. A., Fernandez, I. E., & Stathopoulos, G. T. (2026) · British Journal of Pharmacology · doi:10.1111/bph.70546 · Cited by 3 · see citing works

Drugging the Undruggable: Advances on RAS Targeting in Cancer

Molina‐Arcas, M., Samani, A., & Downward, J. (2021) · Genes · doi:10.3390/genes12060899 · Cited by 73 · see citing works

KRAS G12C–Targeted Therapy in Non-Small Cell Lung Cancer: From Resistant Salvage to Potential First-Line Backbone

Rosas, D., Barad, P., Wright, J., & Raez, L. E. (2026) · International Journal of Molecular Sciences · doi:10.3390/ijms27146455 · Cited by 5 · see citing works

Targeting KRAS in non-small-cell lung cancer: recent progress and new approaches

Reck, M., Carbone, D. P., Garassino, M., & Barlesi, F. (2021) · Annals of Oncology · doi:10.1016/j.annonc.2021.06.001 · Cited by 326 · see citing works

KRAS-targeted therapy in oncology: From four decades of failed attempts to a new era of precision medicine

Arshinnikova Anna, S., Tararina Valeria, V., Zuban Polina, A., Leshcheva Elizaveta, A., Bogdanova Irena, V., Fishchenko Ekaterina, A., Nadaraia Mariam, S., Zeynalova Sabina, I., Gorodkova Maria, E., Kamurzoev Ismail, A., et al. (2026) · International Journal of Science and Research Archive · doi:10.30574/ijsra.2026.20.1.1495