Factors underlying sensitivity of cancers to small-molecule kinase inhibitors.

PubWeight™: 3.64‹?› | Rank: Top 1%

🔗 View Article (PMID 19629074)

Published in Nat Rev Drug Discov on July 24, 2009

Authors

Pasi A Jänne1, Nathanael Gray, Jeff Settleman

Author Affiliations

1: Dana Farber Cancer Institute and Harvard Medical School, Boston, Massachusetts, USA.

Articles citing this

Melanomas acquire resistance to B-RAF(V600E) inhibition by RTK or N-RAS upregulation. Nature (2010) 18.69

Dissecting therapeutic resistance to RAF inhibition in melanoma by tumor genomic profiling. J Clin Oncol (2011) 8.37

Intra-tumour heterogeneity: a looking glass for cancer? Nat Rev Cancer (2012) 6.82

Activation of the AXL kinase causes resistance to EGFR-targeted therapy in lung cancer. Nat Genet (2012) 5.64

A common BIM deletion polymorphism mediates intrinsic resistance and inferior responses to tyrosine kinase inhibitors in cancer. Nat Med (2012) 4.90

KRAS and YAP1 converge to regulate EMT and tumor survival. Cell (2014) 3.06

Data mining using the Catalogue of Somatic Mutations in Cancer BioMart. Database (Oxford) (2011) 2.84

The (un)targeted cancer kinome. Nat Chem Biol (2010) 2.33

Highly multiplexed single-cell analysis of formalin-fixed, paraffin-embedded cancer tissue. Proc Natl Acad Sci U S A (2013) 2.29

Receptor tyrosine kinases exert dominant control over PI3K signaling in human KRAS mutant colorectal cancers. J Clin Invest (2011) 2.20

Harnessing synthetic lethal interactions in anticancer drug discovery. Nat Rev Drug Discov (2011) 2.01

A mechanism of resistance to gefitinib mediated by cellular reprogramming and the acquisition of an FGF2-FGFR1 autocrine growth loop. Oncogenesis (2013) 1.87

EWS-FLI-1 modulates miRNA145 and SOX2 expression to initiate mesenchymal stem cell reprogramming toward Ewing sarcoma cancer stem cells. Genes Dev (2010) 1.81

Envisioning the future of early anticancer drug development. Nat Rev Cancer (2010) 1.67

Complexity in the signaling network: insights from the use of targeted inhibitors in cancer therapy. Genes Dev (2012) 1.60

Systematic identification of molecular subtype-selective vulnerabilities in non-small-cell lung cancer. Cell (2013) 1.60

CYP3A5 mediates basal and acquired therapy resistance in different subtypes of pancreatic ductal adenocarcinoma. Nat Med (2016) 1.50

Rapid and reproducible single-stage phosphopeptide enrichment of complex peptide mixtures: application to general and phosphotyrosine-specific phosphoproteomics experiments. Anal Chem (2011) 1.40

STAT3 is activated by JAK2 independent of key oncogenic driver mutations in non-small cell lung carcinoma. PLoS One (2012) 1.33

A novel SND1-BRAF fusion confers resistance to c-Met inhibitor PF-04217903 in GTL16 cells through [corrected] MAPK activation. PLoS One (2012) 1.30

Mechanisms of drug resistance in kinases. Expert Opin Investig Drugs (2011) 1.29

Incomplete inhibition of phosphorylation of 4E-BP1 as a mechanism of primary resistance to ATP-competitive mTOR inhibitors. Oncogene (2013) 1.23

Acquired resistance to drugs targeting receptor tyrosine kinases. Biochem Pharmacol (2011) 1.23

Phase I study of vismodegib in children with recurrent or refractory medulloblastoma: a pediatric brain tumor consortium study. Clin Cancer Res (2013) 1.20

Targeting PI3K in Cancer: Any Good News? Front Oncol (2013) 1.18

PI3K/Akt-sensitive MEK-independent compensatory circuit of ERK activation in ER-positive PI3K-mutant T47D breast cancer cells. Cell Signal (2010) 1.18

Itraconazole inhibits angiogenesis and tumor growth in non-small cell lung cancer. Cancer Res (2011) 1.18

Aberrant expression of proteins involved in signal transduction and DNA repair pathways in lung cancer and their association with clinical parameters. PLoS One (2012) 1.17

Small molecule tools for functional interrogation of protein tyrosine phosphatases. FEBS J (2012) 1.17

Tyrosine kinase inhibitors as modulators of ABC transporter-mediated drug resistance. Drug Resist Updat (2012) 1.12

Allosteric interactions between the myristate- and ATP-site of the Abl kinase. PLoS One (2011) 1.12

Mechanism-based cancer therapy: resistance to therapy, therapy for resistance. Oncogene (2014) 1.10

RAF265 inhibits the growth of advanced human melanoma tumors. Clin Cancer Res (2012) 1.09

Drug synergy screen and network modeling in dedifferentiated liposarcoma identifies CDK4 and IGF1R as synergistic drug targets. Sci Signal (2013) 1.08

Coordinated effects of microRNA-494 induce G₂/M arrest in human cholangiocarcinoma. Cell Cycle (2012) 1.08

Ten things you should know about protein kinases: IUPHAR Review 14. Br J Pharmacol (2015) 1.06

Genomic Determinants of PI3K Pathway Inhibitor Response in Cancer. Front Oncol (2012) 1.05

PI3K therapy reprograms mitochondrial trafficking to fuel tumor cell invasion. Proc Natl Acad Sci U S A (2015) 1.05

Minnelide: a novel therapeutic that promotes apoptosis in non-small cell lung carcinoma in vivo. PLoS One (2013) 1.02

New strategies for treatment of ALK-rearranged non-small cell lung cancers. Clin Cancer Res (2011) 1.01

Adaptive mitochondrial reprogramming and resistance to PI3K therapy. J Natl Cancer Inst (2015) 1.00

Akt/mTOR counteract the antitumor activities of cixutumumab, an anti-insulin-like growth factor I receptor monoclonal antibody. Mol Cancer Ther (2011) 1.00

Discovery and evaluation of novel inhibitors of mycobacterium protein tyrosine phosphatase B from the 6-Hydroxy-benzofuran-5-carboxylic acid scaffold. J Med Chem (2013) 1.00

The road to resistance: EGFR mutation and cetuximab. Nat Med (2012) 0.98

Hsp90 as a gatekeeper of tumor angiogenesis: clinical promise and potential pitfalls. J Oncol (2010) 0.97

Erlotinib binds both inactive and active conformations of the EGFR tyrosine kinase domain. Biochem J (2012) 0.95

Target enzyme mutations are the molecular basis for resistance towards pharmacological inhibition of nicotinamide phosphoribosyltransferase. BMC Cancer (2010) 0.92

Metabolism of the EGFR tyrosin kinase inhibitor gefitinib by cytochrome P450 1A1 enzyme in EGFR-wild type non small cell lung cancer cell lines. Mol Cancer (2011) 0.91

Systems pharmacology. Mt Sinai J Med (2010) 0.90

Responsiveness to PI3K and MEK inhibitors in breast cancer. Use of a 3D culture system to study pathways related to hormone independence in mice. PLoS One (2010) 0.89

Resistance of Cancer Cells to Targeted Therapies Through the Activation of Compensating Signaling Loops. Curr Signal Transduct Ther (2013) 0.88

Attacking a nexus of the oncogenic circuitry by reversing aberrant eIF4F-mediated translation. Mol Cancer Ther (2012) 0.87

A highly selective and potent PTP-MEG2 inhibitor with therapeutic potential for type 2 diabetes. J Am Chem Soc (2012) 0.86

Putting together structures of epidermal growth factor receptors. Curr Opin Struct Biol (2014) 0.86

Personalizing Medicine in Head and Neck Squamous Cell Carcinoma: The Rationale for Combination Therapies. Med Res Arch (2016) 0.86

Drug resistance missense mutations in cancer are subject to evolutionary constraints. PLoS One (2013) 0.85

Identification of PLX4032-resistance mechanisms and implications for novel RAF inhibitors. Pigment Cell Melanoma Res (2014) 0.84

Tumour heterogeneity and immune-modulation. Curr Opin Pharmacol (2013) 0.84

A loss-of-function genetic screening identifies novel mediators of thyroid cancer cell viability. Oncotarget (2016) 0.84

Flavopiridol synergizes with sorafenib to induce cytotoxicity and potentiate antitumorigenic activity in EGFR/HER-2 and mutant RAS/RAF breast cancer model systems. Neoplasia (2013) 0.83

Synthetic lethal screening reveals FGFR as one of the combinatorial targets to overcome resistance to Met-targeted therapy. Oncogene (2014) 0.83

Structural basis and distal effects of Gag substrate coevolution in drug resistance to HIV-1 protease. Proc Natl Acad Sci U S A (2014) 0.82

Accurate calculation of mutational effects on the thermodynamics of inhibitor binding to p38α MAP kinase: a combined computational and experimental study. J Chem Theory Comput (2013) 0.82

Nonamplified FGFR1 is a growth driver in malignant pleural mesothelioma. Mol Cancer Res (2014) 0.81

Receptor tyrosine kinase gene expression profiles of Ewing sarcomas reveal ROR1 as a potential therapeutic target in metastatic disease. Mol Oncol (2015) 0.80

Prediction of signaling cross-talks contributing to acquired drug resistance in breast cancer cells by Bayesian statistical modeling. BMC Syst Biol (2015) 0.80

Post-transcriptional controls by ribonucleoprotein complexes in the acquisition of drug resistance. Int J Mol Sci (2013) 0.80

Evaluation of a multi-kinase inhibitor KRC-108 as an anti-tumor agent in vitro and in vivo. Invest New Drugs (2010) 0.80

Crosstalk with cancer-associated fibroblasts induces resistance of non-small cell lung cancer cells to epidermal growth factor receptor tyrosine kinase inhibition. Onco Targets Ther (2015) 0.79

Targeting GTPases in Parkinson's disease: comparison to the historic path of kinase drug discovery and perspectives. Front Mol Neurosci (2014) 0.79

Integrating complex genomic datasets and tumour cell sensitivity profiles to address a 'simple' question: which patients should get this drug? BMC Med (2009) 0.79

Pre-clinical drug prioritization via prognosis-guided genetic interaction networks. PLoS One (2010) 0.78

Tyrosine phosphatase inhibitor-3 sensitizes melanoma and colon cancer to biotherapeutics and chemotherapeutics. Mol Cancer Ther (2010) 0.78

Kinase inhibition by deoxy analogues of the resorcylic lactone L-783277. ACS Med Chem Lett (2010) 0.77

Chiral kinase inhibitors. Curr Top Med Chem (2011) 0.77

Simultaneous perturbation of the MAPK and the PI3K/mTOR pathways does not lead to increased radiosensitization. Radiat Oncol (2015) 0.77

Overexpression of FGFR2 contributes to inherent resistance to MET inhibitors in MET-amplified patient-derived gastric cancer xenografts. Oncol Lett (2015) 0.77

The Aurora kinase inhibitors in cancer research and therapy. J Cancer Res Clin Oncol (2016) 0.76

Model-Based Design of a Decision Tree for Treating HER2+ Cancers Based on Genetic and Protein Biomarkers. CPT Pharmacometrics Syst Pharmacol (2015) 0.76

An inhibitor's-eye view of the ATP-binding site of CDKs in different regulatory states. ACS Chem Biol (2014) 0.76

Future directions in the evaluation of c-MET-driven malignancies. Ther Adv Med Oncol (2011) 0.76

Assessing Combinational Drug Efficacy in Cancer Cells by Using Image-based Dynamic Response Analysis. Cancer Inform (2016) 0.75

Cellular biochemistry methods for investigating protein tyrosine phosphatases. Antioxid Redox Signal (2014) 0.75

Synthesis and cytotoxicity evaluation of novel pyrido[3,4-d]pyrimidine derivatives as potential anticancer agents. Medchemcomm (2012) 0.75

Tracking the evolution of cancer cell populations through the mathematical lens of phenotype-structured equations. Biol Direct (2016) 0.75

The escalating role of epidermal growth factor receptor inhibitors in cancer management: clinical considerations for the health system pharmacist. P T (2010) 0.75

A Novel Inhibitor of Topoisomerase I Is Selectively Toxic for a Subset of Non-Small Cell Lung Cancer Cell Lines. Mol Cancer Ther (2015) 0.75

Targeted Therapy Database (TTD): a model to match patient's molecular profile with current knowledge on cancer biology. PLoS One (2010) 0.75

Mycobacterial Protein Tyrosine Phosphatases A and B Inhibitors Augment the Bactericidal Activity of the Standard Anti-tuberculosis Regimen. ACS Infect Dis (2015) 0.75

Activation Status of Receptor Tyrosine Kinases as an Early Predictive Marker of Response to Chemotherapy in Osteosarcoma. Transl Oncol (2017) 0.75

Integrated analysis profiles of long non-coding RNAs reveal potential biomarkers of drug resistance in lung cancer. Oncotarget (2017) 0.75

The PI3Kδ Inhibitor Idelalisib Inhibits Homing in an in Vitro and in Vivo Model of B ALL. Cancers (Basel) (2017) 0.75

Articles cited by this

(truncated to the top 100)

Activating mutations in the epidermal growth factor receptor underlying responsiveness of non-small-cell lung cancer to gefitinib. N Engl J Med (2004) 71.08

Mutations of the BRAF gene in human cancer. Nature (2002) 65.42

EGFR mutations in lung cancer: correlation with clinical response to gefitinib therapy. Science (2004) 61.56

Identification of the transforming EML4-ALK fusion gene in non-small-cell lung cancer. Nature (2007) 37.09

A census of human cancer genes. Nat Rev Cancer (2004) 36.20

EGF receptor gene mutations are common in lung cancers from "never smokers" and are associated with sensitivity of tumors to gefitinib and erlotinib. Proc Natl Acad Sci U S A (2004) 33.85

MET amplification leads to gefitinib resistance in lung cancer by activating ERBB3 signaling. Science (2007) 32.68

Erlotinib in previously treated non-small-cell lung cancer. N Engl J Med (2005) 31.48

EGFR mutation and resistance of non-small-cell lung cancer to gefitinib. N Engl J Med (2005) 26.35

Acquired resistance of lung adenocarcinomas to gefitinib or erlotinib is associated with a second mutation in the EGFR kinase domain. PLoS Med (2005) 25.93

Efficacy and safety of imatinib mesylate in advanced gastrointestinal stromal tumors. N Engl J Med (2002) 24.88

Efficacy and safety of a specific inhibitor of the BCR-ABL tyrosine kinase in chronic myeloid leukemia. N Engl J Med (2001) 24.51

mTOR inhibition induces upstream receptor tyrosine kinase signaling and activates Akt. Cancer Res (2006) 18.44

Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity. Proc Natl Acad Sci U S A (2008) 17.41

Imatinib compared with interferon and low-dose cytarabine for newly diagnosed chronic-phase chronic myeloid leukemia. N Engl J Med (2003) 17.23

The evolution of phosphatidylinositol 3-kinases as regulators of growth and metabolism. Nat Rev Genet (2006) 17.19

Molecular determinants of the response of glioblastomas to EGFR kinase inhibitors. N Engl J Med (2005) 15.42

A quantitative analysis of kinase inhibitor selectivity. Nat Biotechnol (2008) 14.74

Effective use of PI3K and MEK inhibitors to treat mutant Kras G12D and PIK3CA H1047R murine lung cancers. Nat Med (2008) 14.47

Cancer. Addiction to oncogenes--the Achilles heal of cancer. Science (2002) 14.20

Multiple BCR-ABL kinase domain mutations confer polyclonal resistance to the tyrosine kinase inhibitor imatinib (STI571) in chronic phase and blast crisis chronic myeloid leukemia. Cancer Cell (2002) 13.03

High-throughput oncogene mutation profiling in human cancer. Nat Genet (2007) 12.68

Gefitinib plus best supportive care in previously treated patients with refractory advanced non-small-cell lung cancer: results from a randomised, placebo-controlled, multicentre study (Iressa Survival Evaluation in Lung Cancer). Lancet (2005) 12.30

MET amplification occurs with or without T790M mutations in EGFR mutant lung tumors with acquired resistance to gefitinib or erlotinib. Proc Natl Acad Sci U S A (2007) 11.85

Overriding imatinib resistance with a novel ABL kinase inhibitor. Science (2004) 11.83

Gefitinib-sensitizing EGFR mutations in lung cancer activate anti-apoptotic pathways. Science (2004) 11.58

Kinase mutations and imatinib response in patients with metastatic gastrointestinal stromal tumor. J Clin Oncol (2003) 11.33

A functional genetic approach identifies the PI3K pathway as a major determinant of trastuzumab resistance in breast cancer. Cancer Cell (2007) 11.21

PTEN activation contributes to tumor inhibition by trastuzumab, and loss of PTEN predicts trastuzumab resistance in patients. Cancer Cell (2004) 10.89

Fusion of a kinase gene, ALK, to a nucleolar protein gene, NPM, in non-Hodgkin's lymphoma. Science (1994) 10.45

Phase II trial of cetuximab in patients with refractory colorectal cancer that expresses the epidermal growth factor receptor. J Clin Oncol (2004) 9.73

First-line gefitinib in patients with advanced non-small-cell lung cancer harboring somatic EGFR mutations. J Clin Oncol (2008) 9.43

EML4-ALK fusion gene and efficacy of an ALK kinase inhibitor in lung cancer. Clin Cancer Res (2008) 9.29

Targeting cancer with small molecule kinase inhibitors. Nat Rev Cancer (2009) 9.26

Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling. Proc Natl Acad Sci U S A (2007) 8.23

The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP. Proc Natl Acad Sci U S A (2008) 8.08

Activation of Akt and eIF4E survival pathways by rapamycin-mediated mammalian target of rapamycin inhibition. Cancer Res (2005) 7.34

Cytoreductive antitumor activity of PF-2341066, a novel inhibitor of anaplastic lymphoma kinase and c-Met, in experimental models of anaplastic large-cell lymphoma. Mol Cancer Ther (2007) 7.08

BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models. Oncogene (2008) 6.82

Activating mutations in ALK provide a therapeutic target in neuroblastoma. Nature (2008) 6.80

Genomic alterations of anaplastic lymphoma kinase may sensitize tumors to anaplastic lymphoma kinase inhibitors. Cancer Res (2008) 6.71

Escape from HER-family tyrosine kinase inhibitor therapy by the kinase-inactive HER3. Nature (2007) 6.56

Prospective phase II study of gefitinib for chemotherapy-naive patients with advanced non-small-cell lung cancer with epidermal growth factor receptor gene mutations. J Clin Oncol (2006) 6.55

A dual PI3 kinase/mTOR inhibitor reveals emergent efficacy in glioma. Cancer Cell (2006) 6.15

Modeling genomic diversity and tumor dependency in malignant melanoma. Cancer Res (2008) 5.95

Oncogenic mutations of ALK kinase in neuroblastoma. Nature (2008) 5.80

Allelic dilution obscures detection of a biologically significant resistance mutation in EGFR-amplified lung cancer. J Clin Invest (2006) 5.73

Somatic and germline activating mutations of the ALK kinase receptor in neuroblastoma. Nature (2008) 5.32

Amplification of MET may identify a subset of cancers with extreme sensitivity to the selective tyrosine kinase inhibitor PHA-665752. Proc Natl Acad Sci U S A (2006) 5.23

Acquired resistance to EGFR tyrosine kinase inhibitors in cancer cells is mediated by loss of IGF-binding proteins. J Clin Invest (2008) 4.95

Bronchial and peripheral murine lung carcinomas induced by T790M-L858R mutant EGFR respond to HKI-272 and rapamycin combination therapy. Cancer Cell (2007) 4.85

Phase I pharmacokinetic and pharmacodynamic study of the oral, small-molecule mitogen-activated protein kinase kinase 1/2 inhibitor AZD6244 (ARRY-142886) in patients with advanced cancers. J Clin Oncol (2008) 4.82

A phase II trial of gefitinib as first-line therapy for advanced non-small cell lung cancer with epidermal growth factor receptor mutations. Br J Cancer (2006) 4.46

Hepatocyte growth factor induces gefitinib resistance of lung adenocarcinoma with epidermal growth factor receptor-activating mutations. Cancer Res (2008) 4.30

c-Src and cooperating partners in human cancer. Cancer Cell (2004) 4.22

Oncogene addiction: setting the stage for molecularly targeted cancer therapy. Genes Dev (2007) 4.11

Efficacy and safety of lapatinib as first-line therapy for ErbB2-amplified locally advanced or metastatic breast cancer. J Clin Oncol (2008) 3.83

Dasatinib, an orally active small molecule inhibitor of both the src and abl kinases, selectively inhibits growth of basal-type/"triple-negative" breast cancer cell lines growing in vitro. Breast Cancer Res Treat (2007) 3.83

A common signaling cascade may underlie "addiction" to the Src, BCR-ABL, and EGF receptor oncogenes. Cancer Cell (2006) 3.78

Phosphatidylinositol 3-kinase hyperactivation results in lapatinib resistance that is reversed by the mTOR/phosphatidylinositol 3-kinase inhibitor NVP-BEZ235. Cancer Res (2008) 3.70

Transient potent BCR-ABL inhibition is sufficient to commit chronic myeloid leukemia cells irreversibly to apoptosis. Cancer Cell (2008) 3.68

Acquired resistance to tyrosine kinase inhibitors during cancer therapy. Curr Opin Genet Dev (2008) 3.67

Mutations in the phosphatidylinositol-3-kinase pathway predict for antitumor activity of the inhibitor PX-866 whereas oncogenic Ras is a dominant predictor for resistance. Cancer Res (2009) 3.59

PDGFRs are critical for PI3K/Akt activation and negatively regulated by mTOR. J Clin Invest (2007) 3.54

Phase II study of receptor-enhanced chemosensitivity using recombinant humanized anti-p185HER2/neu monoclonal antibody plus cisplatin in patients with HER2/neu-overexpressing metastatic breast cancer refractory to chemotherapy treatment. J Clin Oncol (1998) 3.40

STI571 inactivation of the gastrointestinal stromal tumor c-KIT oncoprotein: biological and clinical implications. Oncogene (2001) 3.36

EWS/FLI-1 silencing and gene profiling of Ewing cells reveal downstream oncogenic pathways and a crucial role for repression of insulin-like growth factor binding protein 3. Mol Cell Biol (2004) 3.33

Drug-sensitive FGFR2 mutations in endometrial carcinoma. Proc Natl Acad Sci U S A (2008) 3.30

Characterization of a conserved structural determinant controlling protein kinase sensitivity to selective inhibitors. Chem Biol (2004) 3.30

The structure of Dasatinib (BMS-354825) bound to activated ABL kinase domain elucidates its inhibitory activity against imatinib-resistant ABL mutants. Cancer Res (2006) 3.28

Lung cancer cell lines harboring MET gene amplification are dependent on Met for growth and survival. Cancer Res (2007) 3.20

Impact of Fc{gamma}RIIa-Fc{gamma}RIIIa polymorphisms and KRAS mutations on the clinical outcome of patients with metastatic colorectal cancer treated with cetuximab plus irinotecan. J Clin Oncol (2009) 3.20

Targeting the RAF-MEK-ERK pathway in cancer therapy. Cancer Lett (2009) 3.19

Major response to imatinib mesylate in KIT-mutated melanoma. J Clin Oncol (2008) 3.16

A germline JAK2 SNP is associated with predisposition to the development of JAK2(V617F)-positive myeloproliferative neoplasms. Nat Genet (2009) 3.10

BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. Cancer Res (2008) 2.76

An alternative inhibitor overcomes resistance caused by a mutation of the epidermal growth factor receptor. Cancer Res (2005) 2.72

Genetic predictors of MEK dependence in non-small cell lung cancer. Cancer Res (2008) 2.71

Targeting mammalian target of rapamycin (mTOR) for health and diseases. Drug Discov Today (2006) 2.59

The T790M "gatekeeper" mutation in EGFR mediates resistance to low concentrations of an irreversible EGFR inhibitor. Mol Cancer Ther (2008) 2.58

KIT gene mutations and copy number in melanoma subtypes. Clin Cancer Res (2008) 2.57

FGFR3 activates RSK2 to mediate hematopoietic transformation through tyrosine phosphorylation of RSK2 and activation of the MEK/ERK pathway. Cancer Cell (2007) 2.56

FGFR2-amplified gastric cancer cell lines require FGFR2 and Erbb3 signaling for growth and survival. Cancer Res (2008) 2.46

Mutations in BRAF and KRAS converge on activation of the mitogen-activated protein kinase pathway in lung cancer mouse models. Cancer Res (2007) 2.45

Human cancer, PTEN and the PI-3 kinase pathway. Semin Cell Dev Biol (2004) 2.42

Dasatinib (BMS-354825) selectively induces apoptosis in lung cancer cells dependent on epidermal growth factor receptor signaling for survival. Cancer Res (2006) 2.41

Phase I and pharmacodynamic study of the oral MEK inhibitor CI-1040 in patients with advanced malignancies. J Clin Oncol (2005) 2.32

"Oncogenic shock": explaining oncogene addiction through differential signal attenuation. Clin Cancer Res (2006) 2.30

Multicentre prospective phase II trial of gefitinib for advanced non-small cell lung cancer with epidermal growth factor receptor mutations: results of the West Japan Thoracic Oncology Group trial (WJTOG0403). Br J Cancer (2008) 2.19

Antitumor activity of the insulin-like growth factor-I receptor kinase inhibitor NVP-AEW541 in musculoskeletal tumors. Cancer Res (2005) 2.09

Differential metabolism of gefitinib and erlotinib by human cytochrome P450 enzymes. Clin Cancer Res (2007) 2.07

Enhancing mammalian target of rapamycin (mTOR)-targeted cancer therapy by preventing mTOR/raptor inhibition-initiated, mTOR/rictor-independent Akt activation. Cancer Res (2008) 2.01

Pharmacogenomic and pharmacokinetic determinants of erlotinib toxicity. J Clin Oncol (2008) 1.91

Phase I study of anti--epidermal growth factor receptor antibody cetuximab in combination with radiation therapy in patients with advanced head and neck cancer. J Clin Oncol (2001) 1.87

Prediction of resistance to small molecule FLT3 inhibitors: implications for molecularly targeted therapy of acute leukemia. Cancer Res (2004) 1.79

Epidermal growth factor receptor kinase domain mutations in esophageal and pancreatic adenocarcinomas. Clin Cancer Res (2006) 1.75

Effects of smoking on the pharmacokinetics of erlotinib. Clin Cancer Res (2006) 1.74

The role of Src in prostate cancer. Ann Oncol (2007) 1.71

Tumor endothelial cells express epidermal growth factor receptor (EGFR) but not ErbB3 and are responsive to EGF and to EGFR kinase inhibitors. Cancer Res (2006) 1.67

ZD1839 (Iressa) induces antiangiogenic effects through inhibition of epidermal growth factor receptor tyrosine kinase. Cancer Res (2002) 1.67

Articles by these authors

Activating mutations in the epidermal growth factor receptor underlying responsiveness of non-small-cell lung cancer to gefitinib. N Engl J Med (2004) 71.08

A chromatin-mediated reversible drug-tolerant state in cancer cell subpopulations. Cell (2010) 11.20

Widespread potential for growth-factor-driven resistance to anticancer kinase inhibitors. Nature (2012) 8.13

A gene expression signature associated with "K-Ras addiction" reveals regulators of EMT and tumor cell survival. Cancer Cell (2009) 6.23

Inherited susceptibility to lung cancer may be associated with the T790M drug resistance mutation in EGFR. Nat Genet (2005) 4.00

Sphingosine 1-phosphate (S1P) receptor subtypes S1P1 and S1P3, respectively, regulate lymphocyte recirculation and heart rate. J Biol Chem (2004) 3.57

Identification of a mutation in the extracellular domain of the Epidermal Growth Factor Receptor conferring cetuximab resistance in colorectal cancer. Nat Med (2012) 3.44

Cell line-based platforms to evaluate the therapeutic efficacy of candidate anticancer agents. Nat Rev Cancer (2010) 3.33

Gene expression signatures and small-molecule compounds link a protein kinase to Plasmodium falciparum motility. Nat Chem Biol (2008) 3.23

Targeting the RAF-MEK-ERK pathway in cancer therapy. Cancer Lett (2009) 3.19

Functional characterization of an isoform-selective inhibitor of PI3K-p110β as a potential anticancer agent. Cancer Discov (2012) 2.35

Roscovitine targets, protein kinases and pyridoxal kinase. J Biol Chem (2005) 2.31

Personalized cancer therapy with selective kinase inhibitors: an emerging paradigm in medical oncology. J Clin Oncol (2009) 2.27

Cancer: drivers and passengers. Nature (2007) 2.11

Response and acquired resistance to everolimus in anaplastic thyroid cancer. N Engl J Med (2014) 2.09

TAK1 inhibition promotes apoptosis in KRAS-dependent colon cancers. Cell (2012) 2.08

DOCK4, a GTPase activator, is disrupted during tumorigenesis. Cell (2003) 1.94

Acquired resistance of non-small cell lung cancer cells to MET kinase inhibition is mediated by a switch to epidermal growth factor receptor dependency. Cancer Res (2010) 1.94

Neuregulin-1-mediated autocrine signaling underlies sensitivity to HER2 kinase inhibitors in a subset of human cancers. Cancer Cell (2011) 1.92

Noncovalent wild-type-sparing inhibitors of EGFR T790M. Cancer Discov (2012) 1.86

Epidermal growth factor receptor kinase domain mutations in esophageal and pancreatic adenocarcinomas. Clin Cancer Res (2006) 1.75

Identification of human kinases involved in hepatitis C virus replication by small interference RNA library screening. J Biol Chem (2007) 1.65

FLT3 inhibition and mechanisms of drug resistance in mutant FLT3-positive AML. Drug Resist Updat (2009) 1.47

A monoselective sphingosine-1-phosphate receptor-1 agonist prevents allograft rejection in a stringent rat heart transplantation model. Chem Biol (2006) 1.47

Genome and transcriptome sequencing of lung cancers reveal diverse mutational and splicing events. Genome Res (2012) 1.47

A mutation in MYD88 (L265P) supports the survival of lymphoplasmacytic cells by activation of Bruton tyrosine kinase in Waldenström macroglobulinemia. Blood (2013) 1.44

Mechanisms of acquired resistance to targeted cancer therapies. Future Oncol (2012) 1.33

Discovery of a small-molecule type II inhibitor of wild-type and gatekeeper mutants of BCR-ABL, PDGFRalpha, Kit, and Src kinases: novel type II inhibitor of gatekeeper mutants. Blood (2010) 1.32

p190 Rho-GTPase activating protein associates with plexins and it is required for semaphorin signalling. J Cell Sci (2005) 1.31

Lkb1 inactivation is sufficient to drive endometrial cancers that are aggressive yet highly responsive to mTOR inhibitor monotherapy. Dis Model Mech (2010) 1.27

The IkappaB kinase family phosphorylates the Parkinson's disease kinase LRRK2 at Ser935 and Ser910 during Toll-like receptor signaling. PLoS One (2012) 1.27

Exploiting the balance between life and death: targeted cancer therapy and "oncogenic shock". Biochem Pharmacol (2010) 1.13

Increased prevalence of EGFR-mutant lung cancer in women and in East Asian populations: analysis of estrogen-related polymorphisms. Clin Cancer Res (2008) 1.12

Targeting the cyclin E-Cdk-2 complex represses lung cancer growth by triggering anaphase catastrophe. Clin Cancer Res (2009) 1.10

p42/p44 MAPKs are intracellular targets of the CDK inhibitor purvalanol. Oncogene (2002) 1.10

Oncogenic K-ras "addiction" and synthetic lethality. Cell Cycle (2009) 1.08

High heregulin expression is associated with activated HER3 and may define an actionable biomarker in patients with squamous cell carcinomas of the head and neck. PLoS One (2013) 1.05

SRC family kinases: potential targets for the treatment of human cancer and leukemia. Curr Pharm Des (2003) 1.05

Recent advances in pathway-targeted cancer drug therapies emerging from cancer genome analysis. Curr Opin Genet Dev (2012) 0.97

Discovery of EGFR selective 4,6-disubstituted pyrimidines from a combinatorial kinase-directed heterocycle library. J Am Chem Soc (2006) 0.96

PIM kinases are essential for chronic lymphocytic leukemia cell survival (PIM2/3) and CXCR4-mediated microenvironmental interactions (PIM1). Mol Cancer Ther (2014) 0.95

Identification of coumarin derivatives as a novel class of allosteric MEK1 inhibitors. Bioorg Med Chem Lett (2005) 0.94

Crystal structure of pyridoxal kinase in complex with roscovitine and derivatives. J Biol Chem (2005) 0.93

Selective Akt inhibitors synergize with tyrosine kinase inhibitors and effectively override stroma-associated cytoprotection of mutant FLT3-positive AML cells. PLoS One (2013) 0.88

Selective aurora kinase inhibitors identified using a taxol-induced checkpoint sensitivity screen. ACS Chem Biol (2011) 0.87

Design and synthesis of 7H-pyrrolo[2,3-d]pyrimidines as focal adhesion kinase inhibitors. Part 2. Bioorg Med Chem Lett (2006) 0.86

Design and synthesis of 7H-pyrrolo[2,3-d]pyrimidines as focal adhesion kinase inhibitors. Part 1. Bioorg Med Chem Lett (2006) 0.85

Discovering tumor suppressor genes through genome-wide copy number analysis. Curr Genomics (2010) 0.83

Response to inhibition of smoothened in diverse epithelial cancer cells that lack smoothened or patched 1 mutations. Int J Oncol (2012) 0.80

Dissecting cancer heterogeneity. Nat Biotechnol (2011) 0.80

Corrigendum: The promise and peril of chemical probes. Nat Chem Biol (2015) 0.79

Cancer: miRNA addiction - depending on life's little things. Curr Biol (2010) 0.79

Integrating complex genomic datasets and tumour cell sensitivity profiles to address a 'simple' question: which patients should get this drug? BMC Med (2009) 0.79

Chemical and biological profile of dual Cdk1 and Cdk2 inhibitors. Curr Med Chem Anticancer Agents (2003) 0.75