Charles L. Sawyers

TORward AKTually useful mouse models.

Overriding imatinib resistance with a novel ABL kinase inhibitor.

Rational therapeutic intervention in cancer: kinases as drug targets.

Imatinib induces durable hematologic and cytogenetic responses in patients with accelerated phase chronic myeloid leukemia: results of a phase 2 study.

NF-kappa B activates prostate-specific antigen expression and is upregulated in androgen-independent prostate cancer.

Imatinib induces hematologic and cytogenetic responses in patients with chronic myelogenous leukemia in myeloid blast crisis: results of a phase II study.

Imatinib mesylate (STI571) inhibits growth of primitive malignant progenitors in chronic myelogenous leukemia through reversal of abnormally increased proliferation.

Molecular mechanisms of resistance to STI571 in chronic myeloid leukemia.

Overview: the art of cancer drug screening: molecular target versus milieu-based screens.

Disabling Abl-perspectives on Abl kinase regulation and cancer therapeutics.

Hematopathologic and cytogenetic findings in imatinib mesylate-treated chronic myelogenous leukemia patients: 14 months' experience.

The phosphatidylinositol 3-Kinase AKT pathway in human cancer.

TMEFF2 is an androgen-regulated gene exhibiting antiproliferative effects in prostate cancer cells.

Finding the next Gleevec: FLT3 targeted kinase inhibitor therapy for acute myeloid leukemia.

Clinical resistance to the kinase inhibitor STI-571 in chronic myeloid leukemia by mutation of Tyr-253 in the Abl kinase domain P-loop.

Survival signaling mediated by c-Jun NH(2)-terminal kinase in transformed B lymphoblasts.

A phase 2 study of imatinib in patients with relapsed or refractory Philadelphia chromosome-positive acute lymphoid leukemias.

Imatinib GIST keeps finding new indications: successful treatment of dermatofibrosarcoma protuberans by targeted inhibition of the platelet-derived growth factor receptor.

Chromosomal aberrations in prostate cancer xenografts detected by comparative genomic hybridization.

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.

The emergence of resistance to targeted cancer therapeutics.

Growth inhibitory effects of the dual ErbB1/ErbB2 tyrosine kinase inhibitor PKI-166 on human prostate cancer xenografts.

BCR-ABL point mutants isolated from patients with imatinib mesylate-resistant chronic myeloid leukemia remain sensitive to inhibitors of the BCR-ABL chaperone heat shock protein 90.

Whole-body skeletal imaging in mice utilizing microPET: optimization of reproducibility and applications in animal models of bone disease.

Persistence of malignant hematopoietic progenitors in chronic myelogenous leukemia patients in complete cytogenetic remission following imatinib mesylate treatment.

MicroPET imaging of prostate cancer in LNCAP-SR39TK-GFP mouse xenografts.

A novel pyridopyrimidine inhibitor of abl kinase is a picomolar inhibitor of Bcr-abl-driven K562 cells and is effective against STI571-resistant Bcr-abl mutants.

Analysis of the phosphatidylinositol 3'-kinase signaling pathway in glioblastoma patients in vivo.

Myc-driven murine prostate cancer shares molecular features with human prostate tumors.

AKT activity determines sensitivity to mammalian target of rapamycin (mTOR) inhibitors by regulating cyclin D1 and c-myc expression.

Mechanisms of resistance to STI571 in Philadelphia chromosome-associated leukemias.

Will mTOR inhibitors make it as cancer drugs?

Opportunities and challenges in the development of kinase inhibitor therapy for cancer.

Molecular determinants of resistance to antiandrogen therapy.

Pharmacokinetics and pharmacodynamics of imatinib in a phase I trial with chronic myeloid leukemia patients.

Granulocyte-macrophage progenitors as candidate leukemic stem cells in blast-crisis CML.

Detection of BCR-ABL kinase mutations in CD34+ cells from chronic myelogenous leukemia patients in complete cytogenetic remission on imatinib mesylate treatment.

HER2/neu kinase-dependent modulation of androgen receptor function through effects on DNA binding and stability.

Antibody-based profiling of the phosphoinositide 3-kinase pathway in clinical prostate cancer.

Cross-species comparisons of cancer signaling.

Monitoring antiproliferative responses to kinase inhibitor therapy in mice with 3'-deoxy-3'-18F-fluorothymidine PET.

Comparative analysis of two clinically active BCR-ABL kinase inhibitors reveals the role of conformation-specific binding in resistance.

Transcriptional regulation of a metastasis suppressor gene by Tip60 and beta-catenin complexes.

Dynamics of chronic myeloid leukaemia.

Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases.

Calculated resistance in cancer.

Amplification and overexpression of prosaposin in prostate cancer.

Update on the use of imatinib mesylate.

Biology of progressive, castration-resistant prostate cancer: directed therapies targeting the androgen-receptor signaling axis.

Molecular determinants of the response of glioblastomas to EGFR kinase inhibitors.

Hypoxia-inducible factor determines sensitivity to inhibitors of mTOR in kidney cancer.

Context-dependent hormone-refractory progression revealed through characterization of a novel murine prostate cancer cell line.

Structure of the kinase domain of an imatinib-resistant Abl mutant in complex with the Aurora kinase inhibitor VX-680.

Ligand-specific allosteric regulation of coactivator functions of androgen receptor in prostate cancer cells.

Dasatinib in imatinib-resistant Philadelphia chromosome-positive leukemias.

Will kinase inhibitors have a dark side?

Treating imatinib-resistant leukemia: the next generation targeted therapies.

Mammalian target of rapamycin inhibition promotes response to epidermal growth factor receptor kinase inhibitors in PTEN-deficient and PTEN-intact glioblastoma cells.

Phosphorylation of the ATP-binding loop directs oncogenicity of drug-resistant BCR-ABL mutants.

Epidermal growth factor receptor activation in glioblastoma through novel missense mutations in the extracellular domain.

Identification of the JNK signaling pathway as a functional target of the tumor suppressor PTEN.

Murine cell lines derived from Pten null prostate cancer show the critical role of PTEN in hormone refractory prostate cancer development.

Sequential ABL kinase inhibitor therapy selects for compound drug-resistant BCR-ABL mutations with altered oncogenic potency.

Where lies the blame for resistance--tumor or host?

Cancer: mixing cocktails.

Nineteenth Annual Pezcoller Symposium: hypothesis-driven clinical investigation in cancer.

Antitumor activity of rapamycin in a Phase I trial for patients with recurrent PTEN-deficient glioblastoma.

IkappaB kinase beta inhibition induces cell death in Imatinib-resistant and T315I Dasatinib-resistant BCR-ABL+ cells.

Something lost--something gained: the ASCI begins its second century.

The cancer biomarker problem.

Targeting the androgen receptor pathway in prostate cancer.

A prostatic intraepithelial neoplasia-dependent p27 Kip1 checkpoint induces senescence and inhibits cell proliferation and cancer progression.

The nuclear factor-kappaB pathway controls the progression of prostate cancer to androgen-independent growth.

Translational research: are we on the right track? 2008 American Society for Clinical Investigation Presidential Address.

Transient potent BCR-ABL inhibition is sufficient to commit chronic myeloid leukemia cells irreversibly to apoptosis.

Comprehensive mutational analysis and mRNA isoform quantification of TP63 in normal and neoplastic human prostate cells.

Histone deacetylases are required for androgen receptor function in hormone-sensitive and castrate-resistant prostate cancer.

Development of a second-generation antiandrogen for treatment of advanced prostate cancer.

Cooperativity of TMPRSS2-ERG with PI3-kinase pathway activation in prostate oncogenesis.

Finding and drugging the vulnerabilities of RAS-dependent cancers.

Proteasomal and genetic inactivation of the NF1 tumor suppressor in gliomagenesis.

Clonal hematopoiesis in Philadelphia chromosome-negative bone marrow cells of chronic myeloid leukemia patients receiving dasatinib.

Shifting paradigms: the seeds of oncogene addiction.

Lessons learned from the development of kinase inhibitors.

Structure-activity relationship for thiohydantoin androgen receptor antagonists for castration-resistant prostate cancer (CRPC).

Antitumour activity of MDV3100 in castration-resistant prostate cancer: a phase 1-2 study.

Coordinate transcriptional regulation by ERG and androgen receptor in fusion-positive prostate cancers.

Even better kinase inhibitors for chronic myeloid leukemia.

Integrative genomic profiling of human prostate cancer.

Constitutively active androgen receptor splice variants expressed in castration-resistant prostate cancer require full-length androgen receptor.

ETV1 is a lineage survival factor that cooperates with KIT in gastrointestinal stromal tumours.

Drug discovery: How melanomas bypass new therapy.

Pretreatment EGFR T790M mutation and BRCA1 mRNA expression in erlotinib-treated advanced non-small-cell lung cancer patients with EGFR mutations.

MYC cooperates with AKT in prostate tumorigenesis and alters sensitivity to mTOR inhibitors.

FAS and NF-κB signalling modulate dependence of lung cancers on mutant EGFR.

Reciprocal feedback regulation of PI3K and androgen receptor signaling in PTEN-deficient prostate cancer.

Noninvasive measurement of androgen receptor signaling with a positron-emitting radiopharmaceutical that targets prostate-specific membrane antigen.

A HIF-regulated VHL-PTP1B-Src signaling axis identifies a therapeutic target in renal cell carcinoma.

TMPRSS2-ERG status in circulating tumor cells as a predictive biomarker of sensitivity in castration-resistant prostate cancer patients treated with abiraterone acetate.

Fitness conferred by BCR-ABL kinase domain mutations determines the risk of pre-existing resistance in chronic myeloid leukemia.

ARN-509: a novel anti-androgen for prostate cancer treatment.