Cited by 1,134Melanoma and MAPK PathwaysLung Cancer Treatments and MutationsCancer Mechanisms and Therapy

The DOI matches its Crossref record; 29 of the 29 references it cites were found in a registry or an index.

Widespread potential for growth-factor-driven resistance to anticancer kinase inhibitors

Open access

Wilson, Timothy R., Fridlyand, Jane, Yan, Yibing, Penuel, Elicia, Burton, Luciana, Chan, Emily, Peng, Jing, Lin, Eva, Wang, Yulei, Sosman, Jeff, Ribas, Antoni, Li, Jiang, Moffat, John, Sutherlin, Daniel P., Koeppen, Hartmut, Merchant, Mark, Neve, Richard, Settleman, Jeff·2012·Nature

DOI 10.1038/nature11249PMC PMC3724525

Open this paper in CoChat — free account

Abstract

Mutationally activated kinases define a clinically validated class of targets for cancer drug therapy. However, the efficacy of kinase inhibitors in patients whose tumours harbour such alleles is invariably limited by innate or acquired drug resistance. The identification of resistance mechanisms has revealed a recurrent theme—the engagement of survival signals redundant to those transduced by the targeted kinase. Cancer cells typically express multiple receptor tyrosine kinases (RTKs) that mediate signals that converge on common critical downstream cell-survival effectors—most notably, phosphatidylinositol-3-OH kinase (PI(3)K) and mitogen-activated protein kinase (MAPK). Consequently, an increase in RTK-ligand levels, through autocrine tumour-cell production, paracrine contribution from tumour stroma or systemic production, could confer resistance to inhibitors of an oncogenic kinase with a similar signalling output. Here, using a panel of kinase-'addicted' human cancer cell lines, we found that most cells can be rescued from drug sensitivity by simply exposing them to one or more RTK ligands. Among the findings with clinical implications was the observation that hepatocyte growth factor (HGF) confers resistance to the BRAF inhibitor PLX4032 (vemurafenib) in BRAF-mutant melanoma cells. These observations highlight the extensive redundancy of RTK-transduced signalling in cancer cells and the potentially broad role of widely expressed RTK ligands in innate and acquired resistance to drugs targeting oncogenic kinases.

The claims and statistics of this paper haven’t been checked yet.

Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.

Integrity signals

Registry

Crossref · 10.1038/nature11249

Cites

29 of 29 references verified0 citation errors · 0 not checkable

Statistics

Claims the paper makes

The claims and statistics of this paper haven’t been checked yet.

Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.

Claims other papers make about this one

Each is checked against this paper’s own text: does it say what the citing paper says it does?

Self-check

Percentages, sums and reported differences re-computed from the paper’s own numbers.

The self-check needs the paper’s full text.

Improved survival with vemurafenib in melanoma with BRAF V600E mutation
Chapman, P. B., Hauschild, A., Robert, C., Haanen, J. B., Ascierto, P., Larkin, J., Dummer, R., Garbe, C., Testori, A., Maio, M., et al. (2011) · New England Journal of Medicine · doi:10.1056/nejmoa1103782 · Cited by 7,720
MET Amplification Leads to Gefitinib Resistance in Lung Cancer by Activating ERBB3 Signaling
Engelman, J. A., Zejnullahu, K., Mitsudomi, T., Song, Y., Hyland, C., Park, J. O., Lindeman, N., Gale, C.-M., Zhao, X., Christensen, J., et al. (2007) · Science · doi:10.1126/science.1141478 · Cited by 4,496
Anaplastic Lymphoma Kinase Inhibition in Non–Small-Cell Lung Cancer
Kwak, E. L., Bang, Y., Camidge, D. R., Shaw, A. T., Solomon, B., Maki, R. G., Ou, S. I., Dezube, B. J., Janne, P. A., Costa, D. B., et al. (2010) · New England Journal of Medicine · doi:10.1056/nejmoa1006448 · Cited by 4,477
Genotypic and Histological Evolution of Lung Cancers Acquiring Resistance to EGFR Inhibitors
Sequist, L. V., Waltman, B. A., Dias-Santagata, D., Digumarthy, S., Turke, A. B., Fidias, P., Bergethon, K., Shaw, A. T., Gettinger, S., Cosper, A. K., et al. (2011) · Science Translational Medicine · doi:10.1126/scitranslmed.3002003 · Cited by 3,499
A Chromatin-Mediated Reversible Drug-Tolerant State in Cancer Cell Subpopulations
Sharma, S. V., Lee, D. Y., Li, B., Quinlan, M. P., Takahashi, F., Maheswaran, S., McDermott, U., Azizian, N., Zou, L., Fischbach, M. A., et al. (2010) · Cell · doi:10.1016/j.cell.2010.02.027 · Cited by 2,770
Melanomas acquire resistance to B-RAF(V600E) inhibition by RTK or N-RAS upregulation
Nazarian, R., Shi, H., Wang, Q., Kong, X., Koya, R. C., Lee, H., Chen, Z., Lee, M., Attar, N., Sazegar, H., et al. (2010) · Nature · doi:10.1038/nature09626 · Cited by 2,244
Friends or foes — bipolar effects of the tumour stroma in cancer
Mueller, M. M., & Fusenig, N. E. (2004) · Nature reviews. Cancer · doi:10.1038/nrc1477 · Cited by 1,817
Tumour micro-environment elicits innate resistance to RAF inhibitors through HGF secretion
Straussman, R., Morikawa, T., Shee, K., Barzily-Rokni, M., Qian, Z. R., Du, J., Davis, A., Mongare, M. M., Gould, J., Frederick, D. T., et al. (2012) · Nature · doi:10.1038/nature11183 · Cited by 1,771
Self-citation
COT drives resistance to RAF inhibition through MAP kinase pathway reactivation
Johannessen, C. M., Boehm, J. S., Kim, S. Y., Thomas, S. R., Wardwell, L., Johnson, L. A., Emery, C. M., Stransky, N., Cogdill, A. P., Barretina, J., et al. (2010) · Nature · doi:10.1038/nature09627 · Cited by 1,460
Preexistence and clonal selection of MET amplification in EGFR mutant NSCLC
Turke, A. B., Zejnullahu, K., Wu, Y.-L., Song, Y., Dias-Santagata, D., Lifshits, E., Toschi, L., Rogers, A., Mok, T., Sequist, L., et al. (2010) · Cancer Cell · doi:10.1016/j.ccr.2009.11.022 · Cited by 1,059

Flagged first, then by citations

Show all 29 references

Sorted by citations

Items 501–600 of 1,000

High circulating hepatocyte growth factor levels associate with epithelial to mesenchymal transition and poor outcome in small cell lung cancer patients
Cañadas, I., Taus, Á., González, I., Villanueva, X., Gimeno, J., Pijuán, L., Dómine, M., Sánchez‐Font, A., Vollmer, I., Menéndez, S., et al. (2014) · Oncotarget · doi:10.18632/oncotarget.2124 · Cited by 40
Epigenetic Silencing of SPINT2 Promotes Cancer Cell Motility via HGF-MET Pathway Activation in Melanoma
Hwang, S., Kim, H., Min, M. S., Raghunathan, R., Panova, I. P., Munshi, R., & Ryu, B. (2015) · Journal of Investigative Dermatology · doi:10.1038/jid.2015.160 · Cited by 40
Inhibition of pro-HGF activation by SRI31215, a novel approach to block oncogenic HGF/MET signaling
Owusu, B. Y., Bansal, N., Venukadasula, P. K. M., Ross, L. J., Messick, T. E., Goel, S., Galemmo, R. A., & Klampfer, L. (2016) · Oncotarget · doi:10.18632/oncotarget.8785 · Cited by 40
Overcoming resistance to HER2 inhibitors through state-specific kinase binding
Novotny, C. J., Pollari, S., Park, J. H., Lemmon, M. A., Shen, W., & Shokat, K. M. (2016) · Nature Chemical Biology · doi:10.1038/nchembio.2171 · Cited by 39
Preclinical Evaluation of MET Inhibitor INC-280 With or Without the Epidermal Growth Factor Receptor Inhibitor Erlotinib in Non–Small-Cell Lung Cancer
Lara, M. S., Holland, W. S., Chinn, D. C., Burich, R. A., Lara, P. N., Gandara, D. R., Kelly, K. L., & Mack, P. C. (2016) · Clinical Lung Cancer · doi:10.1016/j.cllc.2016.11.006 · Cited by 40
EGF Induced RET Inhibitor Resistance inCCDC6-RETLung Cancer Cells
Chang, H. K., Sung, J. H., Moon, S. U., Kim, H.-S., Kim, J. W., & Lee, J. S. (2016) · Yonsei Medical Journal · doi:10.3349/ymj.2017.58.1.9 · Cited by 40
Preclinical Evaluation of SCC244 (Glumetinib), a Novel, Potent, and Highly Selective Inhibitor of c-Met in MET-dependent Cancer Models
Ai, J., Chen, Y., Xia, P., Ji, Y., Xi, Y., Shen, Y., Yang, X., Su, Y., Sun, Y., Gao, Y., et al. (2017) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-17-0368 · Cited by 40
Resistance to Raf inhibition in cancer
Haarberg, H. E., & Smalley, K. S. M. (2014) · Drug Discovery Today Technologies · doi:10.1016/j.ddtec.2013.12.004 · Cited by 40
Computation as the Mechanistic Bridge Between Precision Medicine and Systems Therapeutics
Hansen, J., & Iyengar, R. (2012) · Clinical Pharmacology & Therapeutics · doi:10.1038/clpt.2012.199 · Cited by 40
Copy Number Changes Are Associated with Response to Treatment with Carboplatin, Paclitaxel, and Sorafenib in Melanoma
Wilson, M. A., Zhao, F., Khare, S., Roszik, J., Woodman, S. E., D'Andrea, K. P., Wubbenhorst, B. S., Rimm, D. L., Kirkwood, J. M., Kluger, H. M., et al. (2015) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-15-1162 · Cited by 39
Resistance to dual blockade of the kinases PI3K and mTOR in KRAS -mutant colorectal cancer models results in combined sensitivity to inhibition of the receptor tyrosine kinase EGFR
Belmont, P. J., Jiang, P., McKee, T. D., Xie, T., Isaacson, J., Baryla, N. E., Roper, J., Sinnamon, M. J., Lee, N. V., Kan, J. L. C., et al. (2014) · Science Signaling · doi:10.1126/scisignal.2005516 · Cited by 39
Dominant mechanisms of primary resistance differ from dominant mechanisms of secondary resistance to targeted therapies
Asić, K. (2015) · Critical Reviews in Oncology/Hematology · doi:10.1016/j.critrevonc.2015.08.004 · Cited by 38
An HTS-Compatible 3D Colony Formation Assay to Identify Tumor-Specific Chemotherapeutics
Horman, S. R., To, J., & Orth, A. P. (2013) · SLAS DISCOVERY · doi:10.1177/1087057113499405 · Cited by 39
Inhibition of FGF/FGFR autocrine signaling in mesothelioma with the FGF ligand trap, FP-1039/GSK3052230
Blackwell, C., Sherk, C. S., Fricko, M., Ganji, G., Barnette, M. S., Hoang, B. Q., Tunstead, J. R., Skedzielewski, T., Alsaid, H., Jucker, B. M., et al. (2016) · Oncotarget · doi:10.18632/oncotarget.9515 · Cited by 38
Heparan Sulfate Glycosaminoglycans in Glioblastoma Promote Tumor Invasion
Tran, V. M., Wade, A., McKinney, A., Chen, K. Y., Lindberg, O. R., Engler, J. R., Persson, A. I., & Phillips, J. J. (2017) · Molecular Cancer Research · doi:10.1158/1541-7786.mcr-17-0352 · Cited by 39
Drug persistence – From antibiotics to cancer therapies
Kochanowski, K., Morinishi, L. S., Altschuler, S. J., & Wu, L. F. (2018) · Current Opinion in Systems Biology · doi:10.1016/j.coisb.2018.03.003 · Cited by 39
Mechanisms of Resistance to RAF Inhibition in Melanomas Harboring a BRAF Mutation
Chapman, P. B. (2013) · American Society of Clinical Oncology Educational Book · doi:10.14694/edbook_am.2013.33.e80 · Cited by 41
Molecular mechanisms of resistance to kinase inhibitors in thyroid cancers
Hofmann, M.-C. C., Kunnimalaiyaan, M., Wang, J. R., Busaidy, N. L., Sherman, S. I., Lai, S. Y., Zafereo, M., & Cabanillas, M. E. (2022) · Endocrine Related Cancer · doi:10.1530/erc-22-0129 · Cited by 39
Developing biomarkers to predict benefit from HGF / MET pathway inhibitors
Koeppen, H., Rost, S., & Yauch, R. L. (2013) · The Journal of Pathology · doi:10.1002/path.4268 · Cited by 37
Palmitoylation regulates the intracellular trafficking and stability of c-Met
Coleman, D. T., Gray, A. L., Kridel, S. J., & Cardelli, J. A. (2016) · Oncotarget · doi:10.18632/oncotarget.8706 · Cited by 37
VEGF blockade enhances the antitumor effect of BRAFV600E inhibition
Comunanza, V., Corà, D., Orso, F., Consonni, F. M., Middonti, E., Nicolantonio, F. D., Buzdin, A. A., Sica, A., Médico, E., Sangiolo, D., et al. (2016) · EMBO Molecular Medicine · doi:10.15252/emmm.201505774 · Cited by 39
Transcriptomics and Transposon Mutagenesis Identify Multiple Mechanisms of Resistance to the FGFR Inhibitor AZD4547
Kas, S. M., de Ruiter, J. R., Schipper, K., Schut, E., Bombardelli, L., Wientjens, E., Drenth, A. P., de Korte‐Grimmerink, R., Mahakena, S., Phillips, C., et al. (2018) · Cancer Research · doi:10.1158/0008-5472.can-18-0757 · Cited by 37
An acetyl-histone vulnerability in PI3K/AKT inhibition-resistant cancers is targetable by both BET and HDAC inhibitors
Wu, D., Yan, Y., Wei, T., Ye, Z., Xiao, Y., Pan, Y., Orme, J. J., Wang, D., Wang, L., Ren, S., et al. (2021) · Cell Reports · doi:10.1016/j.celrep.2021.108744 · Cited by 37
Co-targeting BRAF and cyclin dependent kinases 4/6 for BRAF mutant cancers
Yadav, V., Chen, S.-H., Yue, Y. G., Buchanan, S. G., Beckmann, R. P., & Peng, S.-B. (2014) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2014.12.003 · Cited by 36
A Pharmacodynamic/Pharmacokinetic Study of Ficlatuzumab in Patients with Advanced Solid Tumors and Liver Metastases
Tabernero, J. M., Élez, E., Herranz, M., Rico, I., Prudkin, L., Andreu, J., Mateos, J., Carreras, M. J., Han, M., Gifford, J., et al. (2014) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-13-1837 · Cited by 36
MET and ERBB2 Are Coexpressed in ERBB2+ Breast Cancer and Contribute to Innate Resistance
Paulson, A. K., Linklater, E. S., Berghuis, B. D., App, C. A., Oostendorp, L. D., Paulson, J. E., Pettinga, J., Melnik, M. K., Woude, G. F. V., & Graveel, C. R. (2013) · Molecular Cancer Research · doi:10.1158/1541-7786.mcr-13-0042 · Cited by 38
89Zr-Onartuzumab PET imaging of c-MET receptor dynamics
Pool, M., van Scheltinga, A. G. T. T., Kol, A., Giesen, D., de Vries, E. G. E., & Hooge, M. N. L. (2017) · European Journal of Nuclear Medicine and Molecular Imaging · doi:10.1007/s00259-017-3672-x · Cited by 36
An epithelial-to-mesenchymal transition-inducing potential of granulocyte macrophage colony-stimulating factor in colon cancer
Chen, Y., Zhao, Z. J., Chen, Y., Lv, Z., Ding, X., Wang, R., He, X., Hou, C., Shen, B., Feng, J., et al. (2017) · Scientific Reports · doi:10.1038/s41598-017-08047-1 · Cited by 36
ProNGF increases breast tumor aggressiveness through functional association of TrkA with EphA2
Lévêque, R., Corbet, C., Aubert, L., Guilbert, M., Lagadec, C. H., Adriaenssens, É., Duval, J., Finetti, P., Birnbaum, D., Magné, N., et al. (2019) · Cancer Letters · doi:10.1016/j.canlet.2019.02.019 · Cited by 37
Novel computational method for predicting polytherapy switching strategies to overcome tumor heterogeneity and evolution
Jönsson, V. D., Blakely, C. M., Lin, L., Asthana, S., Matni, N., Olivas, V. R., Pazarentzos, E., Gubens, M. A., Bastian, B. C., Taylor, B. S., et al. (2017) · Scientific Reports · doi:10.1038/srep44206 · Cited by 36
Therapeutic Options for Metastatic Breast Cancer
Sambi, M., Qorri, B., Harless, W. W., & Szewczuk, M. R. (2019) · Advances in experimental medicine and biology · doi:10.1007/978-3-030-20301-6_8 · Cited by 37
Individual Cells Can Resolve Variations in Stimulus Intensity along the IGF-PI3K-AKT Signaling Axis
Gross, S. M., Dane, M. A., Bucher, E., & Heiser, L. M. (2019) · Cell Systems · doi:10.1016/j.cels.2019.11.005 · Cited by 32
Bad Neighborhood: Fibrotic Stroma as a New Player in Melanoma Resistance to Targeted Therapies
Diazzi, S., Tartare‐Deckert, S., & Deckert, M. (2020) · Cancers · doi:10.3390/cancers12061364 · Cited by 44
Exploiting receptor tyrosine kinase co-activation for cancer therapy
Tan, A. C., Vyse, S., & Huang, P. H. (2016) · Drug Discovery Today · doi:10.1016/j.drudis.2016.07.010 · Cited by 37
Magnetic nanoparticle-based hyperthermia: A prospect in cancer stem cell tracking and therapy
Montazersaheb, P., Pishgahzadeh, E., Jahani, V. B., Farahzadi, R., & Montazersaheb, S. (2023) · Life Sciences · doi:10.1016/j.lfs.2023.121714 · Cited by 38
A multiplex single-cell RNA-Seq pharmacotranscriptomics pipeline for drug discovery
Dini, A., Barker, H. R., Piki, E., Sharma, S., Raivola, J., Murumägi, A., & Ungureanu, D. (2024) · Nature Chemical Biology · doi:10.1038/s41589-024-01761-8 · Cited by 40
3-Dimensional Patient-Derived Lung Cancer Assays Reveal Resistance to Standards-of-Care Promoted by Stromal Cells but Sensitivity to Histone Deacetylase Inhibitors
Onion, D., Argent, R. H., Reece-Smith, A. M., Craze, M. L., Pineda, R. G., Clarke, P. A., Ratan, H. L., Parsons, S. L., Lobo, D. N., Duffy, J. P., et al. (2016) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-15-0598 · Cited by 35
Systematic Analysis of Quantitative Logic Model Ensembles Predicts Drug Combination Effects on Cell Signaling Networks
Morris, M. K., Clarke, D. C., Osimiri, L., & Lauffenburger, D. A. (2016) · CPT Pharmacometrics & Systems Pharmacology · doi:10.1002/psp4.12104 · Cited by 36
Nothing in cancer makes sense except…
Greaves, M. F. (2018) · BMC Biology · doi:10.1186/s12915-018-0493-8 · Cited by 36
Combination of EGFR Inhibitor Lapatinib and MET Inhibitor Foretinib Inhibits Migration of Triple Negative Breast Cancer Cell Lines
Simiczyjew, A., Dratkiewicz, E., Troys, M. V., Ampè, C., Styczeń, I., & Nowak, D. (2018) · Cancers · doi:10.3390/cancers10090335 · Cited by 33
Pathologic and prognostic impacts of FGFR2 amplification in gastric cancer: a meta-analysis and systemic review
Kim, H. S., Kim, J. H., & Jang, H. J. (2019) · Journal of Cancer · doi:10.7150/jca.29184 · Cited by 35
A multi-omic analysis of MCF10A cells provides a resource for integrative assessment of ligand-mediated molecular and phenotypic responses
Gross, S. M., Dane, M. A., Smith, R. L., Devlin, K. L., McLean, I. C., Derrick, D. S., Mills, C. E., Subramanian, K., London, A. B., Torre, D., et al. (2022) · Communications Biology · doi:10.1038/s42003-022-03975-9 · Cited by 29
Neuroendocrine tumors: insights into innovative therapeutic options and rational development of targeted therapies
Barbieri, F., Albertelli, M., Grillo, F., Mohamed, A., Saveanu, A., Barlier, A., Ferone, D., & Florio, T. (2013) · Drug Discovery Today · doi:10.1016/j.drudis.2013.10.015 · Cited by 34
Combined SFK/mTOR Inhibition Prevents Rapamycin-Induced Feedback Activation of AKT and Elicits Efficient Tumor Regression
Yori, J. L., Lozada, K. L., Seachrist, D. D., Mosley, J. D., Abdul‐Karim, F. W., Booth, C. N., Flask, C. A., & Keri, R. A. (2014) · Cancer Research · doi:10.1158/0008-5472.can-13-3627 · Cited by 34
New and emerging factors in tumorigenesis: an overview
Kim, S. (2015) · Cancer Management and Research · doi:10.2147/cmar.s47797 · Cited by 34
Varying effects of EGF, HGF and TGFβ on formation of invadopodia and invasiveness of melanoma cell lines of different origin
Makowiecka, A., Simiczyjew, A., Nowak, D., & Mazur, A. J. (2016) · European Journal of Histochemistry · doi:10.4081/ejh.2016.2728 · Cited by 34
Loss of TGF-β signaling in osteoblasts increases basic-FGF and promotes prostate cancer bone metastasis
Meng, X., Ark, A. V., Daft, P. G., Woodford, E., Wang, J., Madaj, Z., & Li, X. (2018) · Cancer Letters · doi:10.1016/j.canlet.2018.01.018 · Cited by 34
MET amplification increases the metastatic spread of EGFR-mutated NSCLC
Baldacci, S., Kherrouche, Z., Cockenpot, V., Stoven, L., Copin, M. C., Werkmeister, E., Marchand, N., Kyheng, M., Tulasne, D., & Cortot, A. B. (2018) · Lung Cancer · doi:10.1016/j.lungcan.2018.09.008 · Cited by 34
Therapeutic activity of DCC‐2036, a novel tyrosine kinase inhibitor, against triple‐negative breast cancer patient‐derived xenografts by targeting AXL/MET
Shen, Y., Zhang, W., Liu, J., He, J., Cao, R., Chen, X., Peng, X., Xu, H., Zhao, Q., Zhong, J., et al. (2018) · International Journal of Cancer · doi:10.1002/ijc.31915 · Cited by 34
Targeting Epiregulin in the Treatment-Damaged Tumor Microenvironment Diminishes Therapeutic Resistance
Wang, C., Long, Q., Fu, Q., Xu, Q., Fu, D., Li, Y., Gao, L., Guo, J., Zhang, X., Lam, E. W. ‐., et al. (2021) · Oncogene · doi:10.1038/s41388-022-02476-7 · Cited by 37
Hypoxia activated HGF expression in pancreatic stellate cells confers resistance of pancreatic cancer cells to EGFR inhibition
Shi, X., Wang, M., Zhang, Y., Guo, X., Liu, M., Zhou, Z., Zhao, Y., He, R., Gao, Y., Liu, Y., et al. (2022) · EBioMedicine · doi:10.1016/j.ebiom.2022.104352 · Cited by 34
Lower gefitinib dose led to earlier resistance acquisition before emergence of T790M mutation in epidermal growth factor receptor‐mutated lung cancer model
Hayakawa, H., Ichihara, E., Ohashi, K., Ninomiya, T., Yasugi, M., Takata, S., Sakai, K., Matsumoto, K., Takigawa, N., Tanimoto, M., et al. (2013) · Cancer Science · doi:10.1111/cas.12284 · Cited by 36
Game theory in the death galaxy: interaction of cancer and stromal cells in tumour microenvironment
Wu, A. Y., Liao, D., Tlsty, T. D., Sturm, J. C., & Austin, R. H. (2014) · Interface Focus · doi:10.1098/rsfs.2014.0028 · Cited by 34
Translational PK-PD modeling analysis of MCLA-128, a HER2/HER3 bispecific monoclonal antibody, to predict clinical efficacious exposure and dose
Schultink, A. H. M. D. V., Doornbos, R. P., Bakker, A. B. H., Bol, K., Throsby, M., Geuijen, C. A. W., Maussang, D., Schellens, J. H. M., Beijnen, J. H., & Huitema, A. D. R. (2018) · Investigational New Drugs · doi:10.1007/s10637-018-0593-x · Cited by 34
HER3: Toward the Prognostic Significance, Therapeutic Potential, Current Challenges, and Future Therapeutics in Different Types of Cancer
Majumder, A. (2023) · Cells · doi:10.3390/cells12212517 · Cited by 34
MET-Mediated Resistance to EGFR Inhibitors: An Old Liaison Rooted in Colorectal Cancer Stem Cells
Boccaccio, C., Luraghi, P., & Comoglio, P. M. (2014) · Cancer Research · doi:10.1158/0008-5472.can-14-1088 · Cited by 34
Lapatinib resistance in HER2+ cancers: latest findings and new concepts on molecular mechanisms
Shi, H., Zhang, W., Zhi, Q., & Jiang, M. (2016) · Tumor Biology · doi:10.1007/s13277-016-5467-2 · Cited by 36
Strategies for Overcoming Resistance in Tumours Harboring BRAF Mutations
Obaid, N., Bedard, K., & Huang, W. (2017) · International Journal of Molecular Sciences · doi:10.3390/ijms18030585 · Cited by 37
Targeting the tumor-promoting microenvironment in MET-amplified NSCLC cells with a novel inhibitor of pro-HGF activation
Owusu, B. Y., Thomas, S., Venukadasula, P. K. M., Han, Z., Janetka, J. W., Galemmo, R. A., & Klampfer, L. (2017) · Oncotarget · doi:10.18632/oncotarget.18260 · Cited by 33
Differential expression of ABCB5 in BRAF inhibitor-resistant melanoma cell lines
Xiao, J., Egger, M. E., McMasters, K. M., & Hao, H. (2018) · BMC Cancer · doi:10.1186/s12885-018-4583-3 · Cited by 35
Phase I Study of Ficlatuzumab and Cetuximab in Cetuximab-Resistant, Recurrent/Metastatic Head and Neck Cancer
Bauman, J. E., Ohr, J. P., Gooding, W. E., Ferris, R. L., Duvvuri, U., Kim, S., Johnson, J. T., Soloff, A. C., Wallweber, G. J., Winslow, J. W., et al. (2020) · Cancers · doi:10.3390/cancers12061537 · Cited by 33
Fibroblast–tumor cell signaling limits HER2 kinase therapy response via activation of MTOR and antiapoptotic pathways
Zervantonakis, I. K., Poskus, M. D., Scott, A. L., Selfors, L. M., Lin, J., Dillon, D. A. R., Pathania, S., Sorger, P. K., Mills, G. B., & Brugge, J. S. (2020) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.2000648117 · Cited by 34
MET inhibitor, capmatinib overcomes osimertinib resistance via suppression of MET/Akt/snail signaling in non-small cell lung cancer and decreased generation of cancer-associated fibroblasts
Zhu, K., Lv, Z., Xiong, J., Zheng, H., Zhang, S., Jin, H., Yu, L., Li, Z., Zhang, J., Li, C., et al. (2021) · Aging · doi:10.18632/aging.202547 · Cited by 33
Small Molecule Inhibitors for Hepatocellular Carcinoma: Advances and Challenges
Kamal, M. A., Mandour, Y. M., El‐Aziz, M. K. A., Stein, U., & Tayebi, H. M. E. (2022) · Molecules · doi:10.3390/molecules27175537 · Cited by 35
Resistance to targeted therapies: a role for microRNAs?
Migliore, C., & Giordano, S. (2013) · Trends in Molecular Medicine · doi:10.1016/j.molmed.2013.08.002 · Cited by 33
Using Network Biology to Bridge Pharmacokinetics and Pharmacodynamics in Oncology
Kirouac, D. C., & Onsum, M. D. (2013) · CPT Pharmacometrics & Systems Pharmacology · doi:10.1038/psp.2013.38 · Cited by 32
The third dimension: new developments in cell culture models for colorectal research
Pereira, J., Awatade, N. T., Loureiro, C. A., Matos, P., Amaral, M. D., & Jordan, P. (2016) · Cellular and Molecular Life Sciences · doi:10.1007/s00018-016-2258-2 · Cited by 32
Stress responses in stromal cells and tumor homeostasis
Vitale, I., Manic, G., Galassi, C., & Galluzzi, L. (2019) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2019.04.004 · Cited by 33
The Interplay between Colon Cancer Cells and Tumour-Associated Stromal Cells Impacts the Biological Clock and Enhances Malignant Phenotypes
Fuhr, L., Abreu, M., Carbone, A., El‐Athman, R., Bianchi, F., Laukkanen, M. O., Mazzoccoli, G., & Relógio, A. (2019) · Cancers · doi:10.3390/cancers11070988 · Cited by 35
Parallels between wound healing, epimorphic regeneration and solid tumors
Wong, A. Y. L., & Whited, J. L. (2020) · Development · doi:10.1242/dev.181636 · Cited by 31
LncRNA SAMMSON Mediates Adaptive Resistance to RAF Inhibition in BRAF-Mutant Melanoma Cells
Han, S., Yan, Y., Ren, Y., Hu, Y., Wang, Y., Chen, L., Zhi, Z., Zheng, Y., Shao, Y., & Liu, J. (2021) · Cancer Research · doi:10.1158/0008-5472.can-20-3145 · Cited by 35
Microtubule-affinity regulating kinase 4: A potential drug target for cancer therapy
Anwar, S., Shahwan, M. J., Hasan, G. M., Islam, A., & Hassan, M. I. (2022) · Cellular Signalling · doi:10.1016/j.cellsig.2022.110434 · Cited by 32
Endothelial VEGFR Coreceptors Neuropilin-1 and Neuropilin-2 Are Essential for Tumor Angiogenesis
Benwell, C. J., Johnson, R., Taylor, J. A. G. E., Price, C. A., & Robinson, S. D. (2022) · Cancer Research Communications · doi:10.1158/2767-9764.crc-22-0250 · Cited by 33
Survival of HER2-Positive Breast Cancer Cells: Receptor Signaling to Apoptotic Control Centers
Fink, M. Y., & Chipuk, J. E. (2013) · Genes & Cancer · doi:10.1177/1947601913488598 · Cited by 32
High-Order Drug Combinations Are Required to Effectively Kill Colorectal Cancer Cells
Horn, T. L., Ferretti, S., Ebel, N., Tam, A., Ho, S. B., Harbinski, F., Farsidjani, A., Zubrowski, M. J., Sellers, W. R., Schlegel, R., et al. (2016) · Cancer Research · doi:10.1158/0008-5472.can-15-3425 · Cited by 33
Adaptive Responses as Mechanisms of Resistance to BRAF Inhibitors in Melanoma
Saei, A., & Eichhorn, P. J. A. (2019) · Cancers · doi:10.3390/cancers11081176 · Cited by 33
Mécanismes de résistance aux inhibiteurs de BRAF
Charles, J., Martel, C., de Fraipont, F., Leccia, M. ‐., Robert, C., & Busser, B. (2014) · Annales de Dermatologie et de Vénéréologie · doi:10.1016/j.annder.2014.06.021 · Cited by 36
Amplified Ras-MAPK signal states correlate with accelerated EGFR internalization, cytostasis and delayed HER2 tumor onset in Fer-deficient model systems
Sangrar, W., Shi, C., Mullins, G., LeBrun, D. P., Ingalls, B., & Greer, P. A. (2014) · Oncogene · doi:10.1038/onc.2014.340 · Cited by 31
Distinct Receptor Tyrosine Kinase Subsets Mediate Anti-HER2 Drug Resistance in Breast Cancer
Alexander, P. B., Chen, R., Gong, C., Yuan, L., Jasper, J. S., Ding, Y., Markowitz, G. J., Yang, P., Xu, X., McDonnell, D. P., et al. (2016) · Journal of Biological Chemistry · doi:10.1074/jbc.m116.754960 · Cited by 33
The protein kinase MAP3K19 phosphorylates MAP2Ks and thereby activates ERK and JNK kinases and increases viability of KRAS-mutant lung cancer cells
Hoang, V. T., Nyswaner, K. M., Torres‐Ayuso, P., & Brognard, J. (2020) · Journal of Biological Chemistry · doi:10.1074/jbc.ra119.012365 · Cited by 31
Tumour Progression Stage-Dependent Secretion of YB-1 Stimulates Melanoma Cell Migration and Invasion
Kosnopfel, C., Sinnberg, T., Sauer, B., Niessner, H., Muenchow, A., Fehrenbacher, B., Schaller, M., Mertens, P. R., Garbe, C., Thakur, B. K., et al. (2020) · Cancers · doi:10.3390/cancers12082328 · Cited by 31
Presence and utility of intrinsically disordered regions in kinases
Kathiriya, J. J., Pathak, R. R., Clayman, E., Xue, B., Uversky, V. N., & Davé, V. (2014) · Molecular BioSystems · doi:10.1039/c4mb00224e · Cited by 30
Melanoma: oncogenic drivers and the immune system.
Karachaliou, N., Pilotto, S., Teixidó, C., Viteri, S., González‐Cao, M., Riso, A. A., Morales-Espinosa, D., Molina‐Vila, M. Á., CHAIB-OUKADOUR, I., Santarpía, M., et al. (2015) · Europe PMC (PubMed Central) · doi:10.3978/j.issn.2305-5839.2015.08.06 · Cited by 30
Priming cancer cells for drug resistance: role of the fibroblast niche
Fang, W. B., Yao, M., & Cheng, N. (2014) · Frontiers in Biology · doi:10.1007/s11515-014-1300-8 · Cited by 31
Antibody targeting of HER 2/ HER 3 signaling overcomes heregulin‐induced resistance to PI 3 K inhibition in prostate cancer
Poovassery, J. S., Kang, J. C., Kim, D., Ober, R. J., & Ward, E. S. (2014) · International Journal of Cancer · doi:10.1002/ijc.29378 · Cited by 30
The Role of MET in Melanoma and Melanocytic Lesions
Zhou, Y., Song, K. Y., & Giubellino, A. (2019) · American Journal Of Pathology · doi:10.1016/j.ajpath.2019.08.002 · Cited by 30
Neuropilin: Handyman and Power Broker in the Tumor Microenvironment
Niland, S., & Eble, J. A. (2020) · Advances in experimental medicine and biology · doi:10.1007/978-3-030-35582-1_3 · Cited by 30
The IGF-II–Insulin Receptor Isoform-A Autocrine Signal in Cancer: Actionable Perspectives
Scalia, P., Giordano, A., & Williams, S. J. (2020) · Cancers · doi:10.3390/cancers12020366 · Cited by 30
AKT inactivation causes persistent drug tolerance to EGFR inhibitors
Tetsu, O., Phuchareon, J., Eisele, D. W., Hangauer, M. J., & McCormick, F. P. (2015) · Pharmacological Research · doi:10.1016/j.phrs.2015.09.022 · Cited by 31
Novel ATP-Competitive MEK Inhibitor E6201 Is Effective against Vemurafenib-Resistant Melanoma Harboring the MEK1-C121S Mutation in a Preclinical Model
Narita, Y., Okamoto, K., Kawada, M. I., Takase, K., Minoshima, Y., Kodama, K., Iwata, M., Miyamoto, N., & Sawada, K. (2014) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-13-0667 · Cited by 31
Characterization of In Vivo Resistance to Osimertinib and JNJ-61186372, an EGFR/Met Bispecific Antibody, Reveals Unique and Consensus Mechanisms of Resistance
Emdal, K. B., Dittmann, A., Reddy, R. J., Lescarbeau, R. S., Moores, S. L., Laquerre, S. G., & White, F. M. (2017) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-17-0413 · Cited by 33
BRAF inhibition causes resilience of melanoma cell lines by inducing the secretion of FGF1
Grimm, J., Hufnagel, A., Wobser, M., Borst, A., Haferkamp, S., Houben, R., & Meierjohann, S. (2018) · Oncogenesis · doi:10.1038/s41389-018-0082-2 · Cited by 31
What general conclusions can we draw from kinase profiling data sets?
Sutherland, J. J., Gao, C., Cahya, S., & Vieth, M. (2013) · Biochimica et Biophysica Acta (BBA) - Proteins and Proteomics · doi:10.1016/j.bbapap.2012.12.023 · Cited by 29
Ganglioside GD 3 induces convergence and synergism of adhesion and hepatocyte growth factor/Met signals in melanomas
Furukawa, K., Kambe, M., Miyata, M., Ohkawa, Y., Tajima, O., & Furukawa, K. (2013) · Cancer Science · doi:10.1111/cas.12310 · Cited by 29
Microfluidic co-cultures with hydrogel-based ligand trap to study paracrine signals giving rise to cancer drug resistance
Patel, D., Gao, Y., Son, K., Siltanen, C. A., Neve, R. M., Ferrara, K. W., & Revzin, A. (2015) · Lab on a Chip · doi:10.1039/c5lc00948k · Cited by 29
Identification of short-form RON as a novel intrinsic resistance mechanism for anti-MET therapy in MET-positive gastric cancer
Wu, Z., Zhang, Z., Ge, X., Lin, Y., Dai, C., Chang, J., Liu, X., Geng, R., Wang, C., Chen, H., et al. (2015) · Oncotarget · doi:10.18632/oncotarget.5816 · Cited by 29
microRNAs Tune Oxidative Stress in Cancer Therapeutic Tolerance and Resistance
Zhang, W. C. (2019) · International Journal of Molecular Sciences · doi:10.3390/ijms20236094 · Cited by 29
Early Steps of Resistance to Targeted Therapies in Non-Small-Cell Lung Cancer
Delahaye, C., Figarol, S., Pradines, A., Favre, G., Mazières, J., & Calvayrac, O. (2022) · Cancers · doi:10.3390/cancers14112613 · Cited by 32
Intrinsic Resistance to Cixutumumab Is Conferred by Distinct Isoforms of the Insulin Receptor
Forest, A., Amatulli, M., Ludwig, D. L., Damoci, C. B., Wang, Y., Burns, C. A., Donoho, G. P., Zanella, N., Fiebig, H., Prewett, M. C., et al. (2015) · Molecular Cancer Research · doi:10.1158/1541-7786.mcr-15-0279 · Cited by 31
Valproic acid-induced amphiregulin secretion confers resistance to temozolomide treatment in human glioma cells
Chen, J., Lee, I., Huang, C., Wu, Y., Chung, C., Lee, M., Lin, M. H., & Yang, J. (2019) · BMC Cancer · doi:10.1186/s12885-019-5843-6 · Cited by 29

Authors: Wilson, T. R., Fridlyand, J., Yan, Y., Penuel, E., Burton, L., Chan, E., Peng, J., Lin, E., Wang, Y., Sosman, J., Ribas, A., Li, J., Moffat, J., Sutherlin, D. P., Koeppen, H., Merchant, M., Neve, R., & Settleman, J.
Affiliations: Genentech (US)
Vanderbilt University Medical Center (US)
University of California, Los Angeles (US)
Corresponding author: Settleman, Jeff
ORCID: Wilson, Timothy R.
Penuel, Elicia
Chan, Emily
Peng, Jing
Lin, Eva
Wang, Yulei
Ribas, Antoni
Koeppen, Hartmut
Merchant, Mark
Neve, Richard
Venue: Nature
Publisher: Springer Science and Business Media LLC
Published: 2012-07
Volume: 487
Issue: 7408
Pages: 505-509
ISSN: 0028-0836 (ISSN-L)
1476-4687
DOI: 10.1038/nature11249
PMC: PMC3724525
OpenAlex: W1999025555
Cited by: 1,134
References: 29
Citations by year: 2026: 23 · 2025: 16 · 2024: 31 · 2023: 46 · 2022: 47 · 2021: 51 · 2020: 65 · 2019: 70 · 2018: 85 · 2017: 87 · 2016: 125 · 2015: 137 · 2014: 166 · 2013: 150 · 2012: 34
FWCI: 62.91
Type: journal article
Language: en
Open access: green
www.ncbi.nlm.nih.gov
Licence: www.springer.com/tdm (tdm)
Locations: Nature (publishedVersion)
PubMed (publishedVersion)
Europe PMC (PubMed Central) (acceptedVersion)
PubMed Central (acceptedVersion)
RePEc: Research Papers in Economics (submittedVersion)
Funders: National Cancer Institute (K24CA097588)
Topics: Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Melanoma and MAPK Pathways
Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Lung Cancer Treatments and Mutations
Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › Cancer Mechanisms and Therapy
Keywords: drug resistance, kinase inhibitors, receptor tyrosine kinase, growth factors, hepatocyte growth factor, BRAF inhibitors, vemurafenib, melanoma, tumor microenvironment, phosphatidylinositol 3-kinase, mitogen-activated protein kinase, combination therapy
MeSH terms: Lapatinib, Vemurafenib, Antineoplastic Agents, Breast Neoplasms, Cell Survival, Female, Humans, Indoles, Ligands, Melanoma, Quinazolines, Sulfonamides, Signal Transduction, Hepatocyte Growth Factor, Erb-b2 Receptor Tyrosine Kinases, Receptor, ErbB-2, Drug Resistance, Neoplasm, Phosphatidylinositol 3-Kinases, Receptor Protein-Tyrosine Kinases, Mitogen-Activated Protein Kinases, Cell Line, Tumor, Protein Kinase Inhibitors, Proto-Oncogene Proteins B-raf

About these checks

Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.

Statistics and arithmetic are recomputed, not judged.

Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.

What counts as a claim ›How we measure confidence ›How we check this ›

Are you an author, or do you see a problem with this page? Request a review

Widespread potential for growth-factor-driven resistance to anticancer kinase inhibitors

Abstract

Overview

Integrity signals

Verification

Claims the paper makes

Claims other papers make about this one

Self-check

Citations

Cites

Cited by

Related

Metadata

Record

About these checks