Published in Science on July 16, 2004
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
Chronic myeloid leukemia: an update of concepts and management recommendations of European LeukemiaNet. J Clin Oncol (2009) 9.40
Targeting cancer with small molecule kinase inhibitors. Nat Rev Cancer (2009) 9.26
Dissecting therapeutic resistance to RAF inhibition in melanoma by tumor genomic profiling. J Clin Oncol (2011) 8.37
Translating cancer research into targeted therapeutics. Nature (2010) 7.33
AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance. Cancer Cell (2009) 6.97
Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefitinib. Proc Natl Acad Sci U S A (2005) 6.82
Cancer drug resistance: an evolving paradigm. Nat Rev Cancer (2013) 6.77
Latent bone metastasis in breast cancer tied to Src-dependent survival signals. Cancer Cell (2009) 5.24
Predicting drug susceptibility of non-small cell lung cancers based on genetic lesions. J Clin Invest (2009) 5.07
Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases. Proc Natl Acad Sci U S A (2005) 4.70
Human chronic myeloid leukemia stem cells are insensitive to imatinib despite inhibition of BCR-ABL activity. J Clin Invest (2010) 4.70
Epidermal growth factor receptor activation in glioblastoma through novel missense mutations in the extracellular domain. PLoS Med (2006) 4.63
Sequential ABL kinase inhibitor therapy selects for compound drug-resistant BCR-ABL mutations with altered oncogenic potency. J Clin Invest (2007) 4.07
Factors underlying sensitivity of cancers to small-molecule kinase inhibitors. Nat Rev Drug Discov (2009) 3.64
BCL6 enables Ph+ acute lymphoblastic leukaemia cells to survive BCR-ABL1 kinase inhibition. Nature (2011) 3.63
Targeting autophagy potentiates tyrosine kinase inhibitor-induced cell death in Philadelphia chromosome-positive cells, including primary CML stem cells. J Clin Invest (2009) 3.55
Overcoming mutation-based resistance to antiandrogens with rational drug design. Elife (2013) 3.49
Conformational control inhibition of the BCR-ABL1 tyrosine kinase, including the gatekeeper T315I mutant, by the switch-control inhibitor DCC-2036. Cancer Cell (2011) 3.49
Targeting multiple kinase pathways in leukemic progenitors and stem cells is essential for improved treatment of Ph+ leukemia in mice. Proc Natl Acad Sci U S A (2006) 3.48
Targeting Bcr-Abl by combining allosteric with ATP-binding-site inhibitors. Nature (2010) 3.39
Myeloproliferative disorders. Blood (2008) 3.37
BCR-ABL1 compound mutations combining key kinase domain positions confer clinical resistance to ponatinib in Ph chromosome-positive leukemia. Cancer Cell (2014) 3.08
Results of dasatinib therapy in patients with early chronic-phase chronic myeloid leukemia. J Clin Oncol (2009) 3.07
Drug resistance in cancer: principles of emergence and prevention. Proc Natl Acad Sci U S A (2005) 3.03
Comparative analysis of two clinically active BCR-ABL kinase inhibitors reveals the role of conformation-specific binding in resistance. Proc Natl Acad Sci U S A (2005) 2.85
Oncogenic activity of epidermal growth factor receptor kinase mutant alleles is enhanced by the T790M drug resistance mutation. Cancer Res (2007) 2.78
Identifying genotype-dependent efficacy of single and combined PI3K- and MAPK-pathway inhibition in cancer. Proc Natl Acad Sci U S A (2009) 2.77
Molecular biology of bcr-abl1-positive chronic myeloid leukemia. Blood (2008) 2.76
Bead-based profiling of tyrosine kinase phosphorylation identifies SRC as a potential target for glioblastoma therapy. Nat Biotechnol (2008) 2.75
Unravelling the complexity of metastasis - molecular understanding and targeted therapies. Nat Rev Cancer (2011) 2.64
The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib. Proc Natl Acad Sci U S A (2007) 2.51
An efficient rapid system for profiling the cellular activities of molecular libraries. Proc Natl Acad Sci U S A (2006) 2.51
Molecular pathogenesis and therapy of polycythemia induced in mice by JAK2 V617F. PLoS One (2006) 2.42
Pushing the limits of targeted therapy in chronic myeloid leukaemia. Nat Rev Cancer (2012) 2.35
Discovery of drug-resistant and drug-sensitizing mutations in the oncogenic PI3K isoform p110 alpha. Cancer Cell (2008) 2.32
Association between imatinib-resistant BCR-ABL mutation-negative leukemia and persistent activation of LYN kinase. J Natl Cancer Inst (2008) 2.21
BCR/ABL kinase induces self-mutagenesis via reactive oxygen species to encode imatinib resistance. Blood (2006) 2.18
A conserved protonation-dependent switch controls drug binding in the Abl kinase. Proc Natl Acad Sci U S A (2008) 2.18
The small molecule tyrosine kinase inhibitor AMN107 inhibits TEL-PDGFRbeta and FIP1L1-PDGFRalpha in vitro and in vivo. Blood (2005) 2.14
Phosphorylation of the ATP-binding loop directs oncogenicity of drug-resistant BCR-ABL mutants. Proc Natl Acad Sci U S A (2006) 2.13
Inhibition of SRC expression and activity inhibits tumor progression and metastasis of human pancreatic adenocarcinoma cells in an orthotopic nude mouse model. Am J Pathol (2006) 2.07
Novel therapies for metastatic castrate-resistant prostate cancer. J Natl Cancer Inst (2011) 1.98
Label-free detection of small-molecule-protein interactions by using nanowire nanosensors. Proc Natl Acad Sci U S A (2005) 1.95
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
Sustained regression of tumors upon MYC inactivation requires p53 or thrombospondin-1 to reverse the angiogenic switch. Proc Natl Acad Sci U S A (2006) 1.89
Protein kinases as drug targets in trypanosomes and Leishmania. Biochim Biophys Acta (2005) 1.87
Beneficial effects of combining nilotinib and imatinib in preclinical models of BCR-ABL+ leukemias. Blood (2006) 1.83
The use of nilotinib or dasatinib after failure to 2 prior tyrosine kinase inhibitors: long-term follow-up. Blood (2009) 1.82
Fyn and SRC are effectors of oncogenic epidermal growth factor receptor signaling in glioblastoma patients. Cancer Res (2009) 1.79
Dasatinib inhibits proinflammatory functions of mature human neutrophils. Blood (2012) 1.75
Critical roles for mTORC2- and rapamycin-insensitive mTORC1-complexes in growth and survival of BCR-ABL-expressing leukemic cells. Proc Natl Acad Sci U S A (2010) 1.75
Targeting primitive chronic myeloid leukemia cells by effective inhibition of a new AHI-1-BCR-ABL-JAK2 complex. J Natl Cancer Inst (2013) 1.75
A secreted tyrosine kinase acts in the extracellular environment. Cell (2014) 1.74
Anaplastic lymphoma kinase: role in cancer pathogenesis and small-molecule inhibitor development for therapy. Expert Rev Anticancer Ther (2009) 1.73
Loss of p53 impedes the antileukemic response to BCR-ABL inhibition. Proc Natl Acad Sci U S A (2006) 1.71
SGX393 inhibits the CML mutant Bcr-AblT315I and preempts in vitro resistance when combined with nilotinib or dasatinib. Proc Natl Acad Sci U S A (2008) 1.71
Leukemic stem cell persistence in chronic myeloid leukemia patients with sustained undetectable molecular residual disease. Blood (2011) 1.68
Emerging strategies for EphA2 receptor targeting for cancer therapeutics. Expert Opin Ther Targets (2011) 1.65
Stat3 contributes to resistance toward BCR-ABL inhibitors in a bone marrow microenvironment model of drug resistance. Mol Cancer Ther (2008) 1.65
Antitumor activity of targeting SRC kinases in endothelial and myeloid cell compartments of the tumor microenvironment. Clin Cancer Res (2010) 1.64
Equally potent inhibition of c-Src and Abl by compounds that recognize inactive kinase conformations. Cancer Res (2009) 1.64
Protein kinase inhibitors substantially improve the physical detection of T-cells with peptide-MHC tetramers. J Immunol Methods (2008) 1.62
Resistance to chemotherapy: new treatments and novel insights into an old problem. Br J Cancer (2008) 1.62
Inhibition of heat shock protein 90 prolongs survival of mice with BCR-ABL-T315I-induced leukemia and suppresses leukemic stem cells. Blood (2007) 1.61
Combination of hyper-CVAD with ponatinib as first-line therapy for patients with Philadelphia chromosome-positive acute lymphoblastic leukaemia: a single-centre, phase 2 study. Lancet Oncol (2015) 1.61
Therapeutic options for chronic myeloid leukemia: focus on imatinib (Glivec, Gleevectrade mark). Ther Clin Risk Manag (2008) 1.59
Activation of the p38 Map kinase pathway is essential for the antileukemic effects of dasatinib. Leuk Lymphoma (2009) 1.53
Inhibition of Src family kinases with dasatinib blocks migration and invasion of human melanoma cells. Mol Cancer Res (2008) 1.52
The evolution of two mutations during clonal expansion. Genetics (2007) 1.52
ATRA-induced cellular differentiation and CD38 expression inhibits acquisition of BCR-ABL mutations for CML acquired resistance. PLoS Genet (2014) 1.48
Applying the discovery of the Philadelphia chromosome. J Clin Invest (2007) 1.46
Phase II study of dasatinib in relapsed or refractory chronic lymphocytic leukemia. Clin Cancer Res (2011) 1.46
HIV-1 protease inhibitors from inverse design in the substrate envelope exhibit subnanomolar binding to drug-resistant variants. J Am Chem Soc (2008) 1.43
Identification of candidate predictive and surrogate molecular markers for dasatinib in prostate cancer: rationale for patient selection and efficacy monitoring. Genome Biol (2007) 1.43
The challenge of developing robust drugs to overcome resistance. Drug Discov Today (2011) 1.43
Identification of a Tumor Specific, Active-Site Mutation in Casein Kinase 1α by Chemical Proteomics. PLoS One (2016) 1.40
Multifaceted actions of 8-amino-adenosine kill BCR-ABL positive cells. Leuk Lymphoma (2012) 1.40
Sole BCR-ABL inhibition is insufficient to eliminate all myeloproliferative disorder cell populations. Proc Natl Acad Sci U S A (2004) 1.39
CREB is a critical regulator of normal hematopoiesis and leukemogenesis. Blood (2007) 1.39
Shifting paradigms: the seeds of oncogene addiction. Nat Med (2009) 1.37
C-KIT mutation cooperates with full-length AML1-ETO to induce acute myeloid leukemia in mice. Proc Natl Acad Sci U S A (2011) 1.36
Dasatinib in the treatment of chronic myeloid leukemia in accelerated phase after imatinib failure: the START a trial. J Clin Oncol (2009) 1.35
Chaperones as thermodynamic sensors of drug-target interactions reveal kinase inhibitor specificities in living cells. Nat Biotechnol (2013) 1.33
Failure of CDKN2A/B (INK4A/B-ARF)-mediated tumor suppression and resistance to targeted therapy in acute lymphoblastic leukemia induced by BCR-ABL. Genes Dev (2008) 1.33
Overlooking evolution: a systematic analysis of cancer relapse and therapeutic resistance research. PLoS One (2011) 1.32
Efficacy of imatinib dose escalation in patients with chronic myeloid leukemia in chronic phase. Cancer (2009) 1.32
Effects of dasatinib on SRC kinase activity and downstream intracellular signaling in primitive chronic myelogenous leukemia hematopoietic cells. Cancer Res (2008) 1.30
A non-ATP-competitive inhibitor of BCR-ABL overrides imatinib resistance. Proc Natl Acad Sci U S A (2005) 1.30
Activity of dual SRC-ABL inhibitors highlights the role of BCR/ABL kinase dynamics in drug resistance. Proc Natl Acad Sci U S A (2006) 1.30
Acute dasatinib exposure commits Bcr-Abl-dependent cells to apoptosis. Blood (2009) 1.29
Mechanisms of drug resistance in kinases. Expert Opin Investig Drugs (2011) 1.29
The phosphatidylinositol 3-Kinase AKT pathway in human cancer. Nat Rev Cancer (2002) 28.11
Integrative genomic profiling of human prostate cancer. Cancer Cell (2010) 23.61
Molecular determinants of resistance to antiandrogen therapy. Nat Med (2003) 18.90
Molecular determinants of the response of glioblastomas to EGFR kinase inhibitors. N Engl J Med (2005) 15.42
Development of a second-generation antiandrogen for treatment of advanced prostate cancer. Science (2009) 13.87
Dasatinib in imatinib-resistant Philadelphia chromosome-positive leukemias. N Engl J Med (2006) 13.54
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
Granulocyte-macrophage progenitors as candidate leukemic stem cells in blast-crisis CML. N Engl J Med (2004) 11.29
Antitumour activity of MDV3100 in castration-resistant prostate cancer: a phase 1-2 study. Lancet (2010) 10.79
Biology of progressive, castration-resistant prostate cancer: directed therapies targeting the androgen-receptor signaling axis. J Clin Oncol (2005) 10.48
Reciprocal feedback regulation of PI3K and androgen receptor signaling in PTEN-deficient prostate cancer. Cancer Cell (2011) 7.32
Dynamics of chronic myeloid leukaemia. Nature (2005) 6.63
Myc-driven murine prostate cancer shares molecular features with human prostate tumors. Cancer Cell (2003) 6.38
In vitro activity of Bcr-Abl inhibitors AMN107 and BMS-354825 against clinically relevant imatinib-resistant Abl kinase domain mutants. Cancer Res (2005) 5.98
Constitutively active androgen receptor splice variants expressed in castration-resistant prostate cancer require full-length androgen receptor. Proc Natl Acad Sci U S A (2010) 5.59
Antitumor activity of rapamycin in a Phase I trial for patients with recurrent PTEN-deficient glioblastoma. PLoS Med (2008) 5.54
Cooperativity of TMPRSS2-ERG with PI3-kinase pathway activation in prostate oncogenesis. Nat Genet (2009) 5.31
Prevalence of chronic obstructive pulmonary disease in China: a large, population-based survey. Am J Respir Crit Care Med (2007) 4.82
Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases. Proc Natl Acad Sci U S A (2005) 4.70
Epidermal growth factor receptor activation in glioblastoma through novel missense mutations in the extracellular domain. PLoS Med (2006) 4.63
Evolutionary dynamics of gene and isoform regulation in Mammalian tissues. Science (2012) 4.52
Hypoxia-inducible factor determines sensitivity to inhibitors of mTOR in kidney cancer. Nat Med (2005) 4.44
Sequential ABL kinase inhibitor therapy selects for compound drug-resistant BCR-ABL mutations with altered oncogenic potency. J Clin Invest (2007) 4.07
HER2/neu kinase-dependent modulation of androgen receptor function through effects on DNA binding and stability. Cancer Cell (2004) 3.79
Ciliary proteins link basal body polarization to planar cell polarity regulation. Nat Genet (2007) 3.79
Identification of new diamine scaffolds with activity against Mycobacterium tuberculosis. J Med Chem (2006) 3.75
Quantitative 3D video microscopy of HIV transfer across T cell virological synapses. Science (2009) 3.69
Transient potent BCR-ABL inhibition is sufficient to commit chronic myeloid leukemia cells irreversibly to apoptosis. Cancer Cell (2008) 3.68
Effect of carbocisteine on acute exacerbation of chronic obstructive pulmonary disease (PEACE Study): a randomised placebo-controlled study. Lancet (2008) 3.62
Imatinib induces durable hematologic and cytogenetic responses in patients with accelerated phase chronic myeloid leukemia: results of a phase 2 study. Blood (2002) 3.60
Glucocorticoid receptor confers resistance to antiandrogens by bypassing androgen receptor blockade. Cell (2013) 3.59
Targeting the androgen receptor pathway in prostate cancer. Curr Opin Pharmacol (2008) 3.56
Impact of animal handling on the results of 18F-FDG PET studies in mice. J Nucl Med (2006) 3.52
Pharmacokinetics and pharmacodynamics of imatinib in a phase I trial with chronic myeloid leukemia patients. J Clin Oncol (2004) 3.51
Overcoming mutation-based resistance to antiandrogens with rational drug design. Elife (2013) 3.49
Targeting multiple kinase pathways in leukemic progenitors and stem cells is essential for improved treatment of Ph+ leukemia in mice. Proc Natl Acad Sci U S A (2006) 3.48
Math1-driven GFP expression in the developing nervous system of transgenic mice. Gene Expr Patterns (2003) 3.42
Analysis of the phosphatidylinositol 3'-kinase signaling pathway in glioblastoma patients in vivo. Cancer Res (2003) 3.36
Mammalian target of rapamycin inhibition promotes response to epidermal growth factor receptor kinase inhibitors in PTEN-deficient and PTEN-intact glioblastoma cells. Cancer Res (2006) 3.31
FAS and NF-κB signalling modulate dependence of lung cancers on mutant EGFR. Nature (2011) 3.18
Pretreatment EGFR T790M mutation and BRCA1 mRNA expression in erlotinib-treated advanced non-small-cell lung cancer patients with EGFR mutations. Clin Cancer Res (2011) 3.15
Distinct microRNA expression profiles in acute myeloid leukemia with common translocations. Proc Natl Acad Sci U S A (2008) 3.13
Action of the Src family kinase inhibitor, dasatinib (BMS-354825), on human prostate cancer cells. Cancer Res (2005) 3.08
Dishevelled genes mediate a conserved mammalian PCP pathway to regulate convergent extension during neurulation. Development (2006) 2.96
AKT activity determines sensitivity to mammalian target of rapamycin (mTOR) inhibitors by regulating cyclin D1 and c-myc expression. J Biol Chem (2003) 2.88
miR-21 plays a pivotal role in gastric cancer pathogenesis and progression. Lab Invest (2008) 2.87
Comparative analysis of two clinically active BCR-ABL kinase inhibitors reveals the role of conformation-specific binding in resistance. Proc Natl Acad Sci U S A (2005) 2.85
Wnt5a functions in planar cell polarity regulation in mice. Dev Biol (2007) 2.85
Proteasomal and genetic inactivation of the NF1 tumor suppressor in gliomagenesis. Cancer Cell (2009) 2.73
ETV1 is a lineage survival factor that cooperates with KIT in gastrointestinal stromal tumours. Nature (2010) 2.65
Dasatinib (BMS-354825), a dual SRC/ABL kinase inhibitor, inhibits the kinase activity of wild-type, juxtamembrane, and activation loop mutant KIT isoforms associated with human malignancies. Cancer Res (2006) 2.61
Detection of BCR-ABL kinase mutations in CD34+ cells from chronic myelogenous leukemia patients in complete cytogenetic remission on imatinib mesylate treatment. Blood (2004) 2.57
ARN-509: a novel antiandrogen for prostate cancer treatment. Cancer Res (2012) 2.51
A prostatic intraepithelial neoplasia-dependent p27 Kip1 checkpoint induces senescence and inhibits cell proliferation and cancer progression. Cancer Cell (2008) 2.48
Identification of the immunodominant protein and other proteins of the Bacillus anthracis exosporium. J Bacteriol (2003) 2.48
Identification of the JNK signaling pathway as a functional target of the tumor suppressor PTEN. Cancer Cell (2007) 2.43
Transcriptional regulation of a metastasis suppressor gene by Tip60 and beta-catenin complexes. Nature (2005) 2.43
Dasatinib (BMS-354825) selectively induces apoptosis in lung cancer cells dependent on epidermal growth factor receptor signaling for survival. Cancer Res (2006) 2.41
Cryo-EM study of the chromatin fiber reveals a double helix twisted by tetranucleosomal units. Science (2014) 2.37
Neuregulin-1/erbB-activation improves cardiac function and survival in models of ischemic, dilated, and viral cardiomyopathy. J Am Coll Cardiol (2006) 2.37
Regulation of polarized extension and planar cell polarity in the cochlea by the vertebrate PCP pathway. Nat Genet (2005) 2.36
A phase 2 study of imatinib in patients with relapsed or refractory Philadelphia chromosome-positive acute lymphoid leukemias. Blood (2002) 2.33
Murine dishevelled 3 functions in redundant pathways with dishevelled 1 and 2 in normal cardiac outflow tract, cochlea, and neural tube development. PLoS Genet (2008) 2.29
ETS factors reprogram the androgen receptor cistrome and prime prostate tumorigenesis in response to PTEN loss. Nat Med (2013) 2.26
Androgen receptor signaling regulates DNA repair in prostate cancers. Cancer Discov (2013) 2.15
TMPRSS2-ERG status in circulating tumor cells as a predictive biomarker of sensitivity in castration-resistant prostate cancer patients treated with abiraterone acetate. Eur Urol (2011) 2.14
Clinical resistance to the kinase inhibitor STI-571 in chronic myeloid leukemia by mutation of Tyr-253 in the Abl kinase domain P-loop. Proc Natl Acad Sci U S A (2002) 2.13
Phosphorylation of the ATP-binding loop directs oncogenicity of drug-resistant BCR-ABL mutants. Proc Natl Acad Sci U S A (2006) 2.13
Identification of a new antitubercular drug candidate, SQ109, from a combinatorial library of 1,2-ethylenediamines. J Antimicrob Chemother (2005) 2.08
Inhibition of SRC expression and activity inhibits tumor progression and metastasis of human pancreatic adenocarcinoma cells in an orthotopic nude mouse model. Am J Pathol (2006) 2.07
Determination of substrate motifs for human Chk1 and hCds1/Chk2 by the oriented peptide library approach. J Biol Chem (2002) 2.06
Murine cell lines derived from Pten null prostate cancer show the critical role of PTEN in hormone refractory prostate cancer development. Cancer Res (2007) 2.04
Breaching the DNA damage checkpoint via PF-00477736, a novel small-molecule inhibitor of checkpoint kinase 1. Mol Cancer Ther (2008) 2.04
Molecular mechanisms of resistance to STI571 in chronic myeloid leukemia. Curr Opin Hematol (2002) 2.02
Structure of the kinase domain of an imatinib-resistant Abl mutant in complex with the Aurora kinase inhibitor VX-680. Cancer Res (2006) 1.98
Mechanisms of resistance to STI571 in Philadelphia chromosome-associated leukemias. Oncogene (2003) 1.96
Dasatinib inhibits migration and invasion in diverse human sarcoma cell lines and induces apoptosis in bone sarcoma cells dependent on SRC kinase for survival. Cancer Res (2007) 1.96
Potent inhibition of platelet-derived growth factor-induced responses in vascular smooth muscle cells by BMS-354825 (dasatinib). Mol Pharmacol (2006) 1.95
Large-scale data integration framework provides a comprehensive view on glioblastoma multiforme. Genome Med (2010) 1.94
Novel oligosaccharide side chains of the collagen-like region of BclA, the major glycoprotein of the Bacillus anthracis exosporium. J Biol Chem (2004) 1.92
JNK and PTEN cooperatively control the development of invasive adenocarcinoma of the prostate. Proc Natl Acad Sci U S A (2012) 1.88