Quinazolines

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  Subject Areas on Research

  • A double-blind study of prazosin in the treatment of Raynaud's phenomenon in scleroderma. 
  • A model of acquired autoresistance to a potent ErbB2 tyrosine kinase inhibitor and a therapeutic strategy to prevent its onset in breast cancer. 
  • A multi-centre randomized phase II study of nolatrexed versus doxorubicin in treatment of Chinese patients with advanced hepatocellular carcinoma. 
  • A network of substrates of the E3 ubiquitin ligases MDM2 and HUWE1 control apoptosis independently of p53. 
  • A pharmacodynamic study of the epidermal growth factor receptor tyrosine kinase inhibitor ZD1839 in metastatic colorectal cancer patients. 
  • A phase I and biology study of gefitinib and radiation in children with newly diagnosed brain stem gliomas or supratentorial malignant gliomas. 
  • A phase I and pharmacokinetic study of oral lapatinib administered once or twice daily in patients with solid malignancies. 
  • A phase I study of bevacizumab (B) in combination with everolimus (E) and erlotinib (E) in advanced cancer (BEE). 
  • A phase I/II trial of pazopanib in combination with lapatinib in adult patients with relapsed malignant glioma. 
  • A phase II study of induction chemotherapy followed by thoracic radiotherapy and erlotinib in poor-risk stage III non-small-cell lung cancer: results of CALGB 30605 (Alliance)/RTOG 0972 (NRG). 
  • A phase II study of isoflavones, erlotinib, and gemcitabine in advanced pancreatic cancer. 
  • A phase II study of lapatinib monotherapy in chemotherapy-refractory HER2-positive and HER2-negative advanced or metastatic breast cancer. 
  • A phase II study of lapatinib, a dual EGFR and HER-2 tyrosine kinase inhibitor, in patients with castration-resistant prostate cancer. 
  • A phase II study of trimetrexate therapy for metastatic colorectal carcinoma. 
  • A phase II trial of cisplatin (C), gemcitabine (G) and gefitinib for advanced urothelial tract carcinoma: results of Cancer and Leukemia Group B (CALGB) 90102. 
  • A phase II trial of cisplatin, fixed dose-rate gemcitabine and gefitinib for advanced urothelial tract carcinoma: results of the Cancer and Leukaemia Group B 90102. 
  • A randomized phase II study of lapatinib + pazopanib versus lapatinib in patients with HER2+ inflammatory breast cancer. 
  • Acquired resistance to small molecule ErbB2 tyrosine kinase inhibitors. 
  • Activation of AMP-activated protein kinase by human EGF receptor 2/EGF receptor tyrosine kinase inhibitor protects cardiac cells. 
  • Activation of EGF receptors mediates pulmonary vasoconstriction induced by residual oil fly ash. 
  • Adjuvant chemotherapy for non-small cell lung cancer. 
  • Afatinib induces apoptosis in NSCLC without EGFR mutation through Elk-1-mediated suppression of CIP2A. 
  • An heregulin-EGFR-HER3 autocrine signaling axis can mediate acquired lapatinib resistance in HER2+ breast cancer models. 
  • An improved isoprenylcysteine carboxylmethyltransferase inhibitor induces cancer cell death and attenuates tumor growth in vivo. 
  • An innovative, multi-arm, complete phase 1b study of the novel anti-cancer agent tasisulam in patients with advanced solid tumors. 
  • Analysis of dermatologic events in patients with cancer treated with lapatinib. 
  • Anti-tumor activity of GW572016: a dual tyrosine kinase inhibitor blocks EGF activation of EGFR/erbB2 and downstream Erk1/2 and AKT pathways. 
  • Beta-blockers alprenolol and carvedilol stimulate beta-arrestin-mediated EGFR transactivation. 
  • Brain tumors in mice are susceptible to blockade of epidermal growth factor receptor (EGFR) with the oral, specific, EGFR-tyrosine kinase inhibitor ZD1839 (iressa). 
  • CIP2A mediates erlotinib-induced apoptosis in non-small cell lung cancer cells without EGFR mutation. 
  • Cell signaling modifiers in prostate cancer. 
  • Chemoprevention of pancreatic cancer: ready for the clinic? 
  • Chemoradiotherapy and gefitinib in stage III non-small cell lung cancer with epidermal growth factor receptor and KRAS mutation analysis: cancer and leukemia group B (CALEB) 30106, a CALGB-stratified phase II trial. 
  • Clinical evaluation of ZD6474, an orally active inhibitor of VEGF and EGF receptor signaling, in patients with solid, malignant tumors. 
  • Clonal Evolutionary Analysis during HER2 Blockade in HER2-Positive Inflammatory Breast Cancer: A Phase II Open-Label Clinical Trial of Afatinib +/- Vinorelbine. 
  • Combination testing of cediranib (AZD2171) against childhood cancer models by the pediatric preclinical testing program. 
  • Combining lapatinib (GW572016), a small molecule inhibitor of ErbB1 and ErbB2 tyrosine kinases, with therapeutic anti-ErbB2 antibodies enhances apoptosis of ErbB2-overexpressing breast cancer cells. 
  • Constitutively activated STAT3 frequently coexpresses with epidermal growth factor receptor in high-grade gliomas and targeting STAT3 sensitizes them to Iressa and alkylators. 
  • Cost-effectiveness considerations in the treatment of essential thrombocythemia. 
  • Cost-effectiveness of epidermal growth factor receptor mutation testing and first-line treatment with gefitinib for patients with advanced adenocarcinoma of the lung. 
  • Development of bilateral acquired toxoplasmic retinochoroiditis during erlotinib therapy. 
  • Differential effects of vascular endothelial growth factor receptor-2 inhibitor ZD6474 on circulating endothelial progenitors and mature circulating endothelial cells: implications for use as a surrogate marker of antiangiogenic activity. 
  • Dihydroquinazolinone inhibitors of proliferation of blood and liver stage malaria parasites. 
  • Discovery of 6-Fluoro-5-(R)-(3-(S)-(8-fluoro-1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)-2-methylphenyl)-2-(S)-(2-hydroxypropan-2-yl)-2,3,4,9-tetrahydro-1H-carbazole-8-carboxamide (BMS-986142): A Reversible Inhibitor of Bruton's Tyrosine Kinase (BTK) Conformationally Constrained by Two Locked Atropisomers. 
  • Discovery of β-Arrestin Biased, Orally Bioavailable, and CNS Penetrant Neurotensin Receptor 1 (NTR1) Allosteric Modulators. 
  • Distinct Receptor Tyrosine Kinase Subsets Mediate Anti-HER2 Drug Resistance in Breast Cancer. 
  • Downstaging in pancreatic cancer: a matched analysis of patients resected following systemic treatment of initially locally unresectable disease. 
  • Dynamic contrast-enhanced MRI in head-and-neck cancer: the impact of region of interest selection on the intra- and interpatient variability of pharmacokinetic parameters. 
  • EGF promotes mammalian cell growth by suppressing cellular senescence. 
  • EGFR and EGFRvIII interact with PUMA to inhibit mitochondrial translocalization of PUMA and PUMA-mediated apoptosis independent of EGFR kinase activity. 
  • EGFR and EGFRvIII undergo stress- and EGFR kinase inhibitor-induced mitochondrial translocalization: a potential mechanism of EGFR-driven antagonism of apoptosis. 
  • EGFR mutations and sensitivity to gefitinib. 
  • EGFRvIII and c-Met pathway inhibitors synergize against PTEN-null/EGFRvIII+ glioblastoma xenografts. 
  • Efficacy of bevacizumab plus erlotinib for advanced hepatocellular carcinoma and predictors of outcome: final results of a phase II trial. 
  • Efficacy of bevacizumab plus erlotinib versus erlotinib alone in advanced non-small-cell lung cancer after failure of standard first-line chemotherapy (BeTa): a double-blind, placebo-controlled, phase 3 trial. 
  • Endocrine therapy with or without inhibition of epidermal growth factor receptor and human epidermal growth factor receptor 2: a randomized, double-blind, placebo-controlled phase III trial of fulvestrant with or without lapatinib for postmenopausal women with hormone receptor-positive advanced breast cancer-CALGB 40302 (Alliance). 
  • Epidermal growth factor receptor (EGFR)-tyrosine kinase inhibitors combined with chemotherapy in first-line treatment in an advanced non-small cell lung cancer patient with EGFR sensitive mutation. 
  • Epidermal growth factor receptor inhibitor gefitinib added to chemoradiotherapy in locally advanced head and neck cancer. 
  • Epidermal growth factor receptor inhibitors and their role in non-small-cell lung cancer. 
  • Epidermal growth factor receptor mutations predict sensitivity to gefitinib in patients with non-small-cell lung cancer. 
  • Epidermal growth factor receptor trans-activation mediates the tonic and fibrogenic effects of endothelin in the aortic wall of transgenic mice. 
  • Epidermal growth factor regulates hematopoietic regeneration after radiation injury. 
  • ErbB1/2 tyrosine kinase inhibitor mediates oxidative stress-induced apoptosis in inflammatory breast cancer cells. 
  • Erlotinib in lung cancer - molecular and clinical predictors of outcome. 
  • Erlotinib-mediated inhibition of EGFR signaling induces metabolic oxidative stress through NOX4. 
  • Fibrogenesis assessed by serological type III collagen formation identifies patients with progressive liver fibrosis and responders to a potential antifibrotic therapy. 
  • Finding the optimal combination therapy for the treatment of newly diagnosed AML in older patients unfit for intensive therapy. 
  • Gefitinib (Iressa, ZD1839) and tyrosine kinase inhibitors: the wave of the future in cancer therapy. 
  • Gefitinib in patients with malignant mesothelioma: a phase II study by the Cancer and Leukemia Group B. 
  • Gefitinib therapy for non-small cell lung cancer. 
  • Genetic characterization to improve interpretation and clinical management of hepatotoxicity caused by tyrosine kinase inhibitors. 
  • Glioblastoma multiforme and the epidermal growth factor receptor. 
  • HER family kinase domain mutations promote tumor progression and can predict response to treatment in human breast cancer. 
  • Halofuginone inhibits collagen deposition in fibrous capsules around implants. 
  • Hemodynamic and metabolic responses to exercise after alpha 1-, beta 1-, and nonselective beta-adrenoceptor blockade in man. 
  • High-affinity inhibitors of dihydrofolate reductase: antimicrobial and anticancer activities of 7,8-dialkyl-1,3-diaminopyrrolo[3,2-f]quinazolines with small molecular size. 
  • Impact of lapatinib plus trastuzumab versus single-agent lapatinib on quality of life of patients with trastuzumab-refractory HER2+ metastatic breast cancer. 
  • In vitro and in vivo efficacies of the new triazole albaconazole against Cryptococcus neoformans. 
  • Increased toxicity with gefitinib, capecitabine, and radiation therapy in pancreatic and rectal cancer: phase I trial results. 
  • Inhibition of platelet production induced by an antiplatelet drug, anagrelide, in normal volunteers. 
  • Inhibition of the epidermal growth factor receptor in combined modality treatment for locally advanced non-small cell lung cancer. 
  • Inhibition of the mammalian target of rapamycin (mTOR) in advanced pancreatic cancer: results of two phase II studies. 
  • Initial testing (stage 1) of lapatinib by the pediatric preclinical testing program. 
  • Initial testing (stage 1) of the kinesin spindle protein inhibitor ispinesib by the pediatric preclinical testing program. 
  • Initial testing of the VEGFR inhibitor AZD2171 by the pediatric preclinical testing program. 
  • Lapatinib Plasma and Tumor Concentrations and Effects on HER Receptor Phosphorylation in Tumor. 
  • Lapatinib antitumor activity is not dependent upon phosphatase and tensin homologue deleted on chromosome 10 in ErbB2-overexpressing breast cancers. 
  • Lapatinib monotherapy in patients with HER2-overexpressing relapsed or refractory inflammatory breast cancer: final results and survival of the expanded HER2+ cohort in EGF103009, a phase II study. 
  • Long-term ambulatory therapy with prazosin versus placebo for chronic heart failure: relation between clinical response and left ventricular function at rest and during exercise. 
  • Long-term cardiac safety and outcomes of dose-dense doxorubicin and cyclophosphamide followed by paclitaxel and trastuzumab with and without lapatinib in patients with early breast cancer. 
  • ML314: A Biased Neurotensin Receptor Ligand for Methamphetamine Abuse. 
  • Maximal beta3-adrenergic regulation of lipolysis involves Src and epidermal growth factor receptor-dependent ERK1/2 activation. 
  • Metabolic rewiring drives resistance to targeted cancer therapy. 
  • Multiple mechanisms of action of ZR2002 in human breast cancer cells: a novel combi-molecule designed to block signaling mediated by the ERB family of oncogenes and to damage genomic DNA. 
  • Mutant epidermal growth factor receptor up-regulates molecular effectors of tumor invasion. 
  • NOX4 mediates cytoprotective autophagy induced by the EGFR inhibitor erlotinib in head and neck cancer cells. 
  • Oncogenic transformation by inhibitor-sensitive and -resistant EGFR mutants. 
  • Optimization and SAR for dual ErbB-1/ErbB-2 tyrosine kinase inhibition in the 6-furanylquinazoline series. 
  • Optimization of a Novel Series of Ataxia-Telangiectasia Mutated Kinase Inhibitors as Potential Radiosensitizing Agents. 
  • Overall survival benefit with lapatinib in combination with trastuzumab for patients with human epidermal growth factor receptor 2-positive metastatic breast cancer: final results from the EGF104900 Study. 
  • PRKACA mediates resistance to HER2-targeted therapy in breast cancer cells and restores anti-apoptotic signaling. 
  • Phase 1 clinical trial of HER2-specific immunotherapy with concomitant HER2 kinase inhibition [corrected]. 
  • Phase 1 trial of dasatinib plus erlotinib in adults with recurrent malignant glioma. 
  • Phase 1 trial of gefitinib plus sirolimus in adults with recurrent malignant glioma. 
  • Phase 2 study of erlotinib in patients with unresectable hepatocellular carcinoma. 
  • Phase 2 trial of erlotinib plus sirolimus in adults with recurrent glioblastoma. 
  • Phase I and clinical pharmacology study of trimetrexate administered weekly for three weeks. 
  • Phase I and pharmacokinetic study of erlotinib for solid tumors in patients with hepatic or renal dysfunction: CALGB 60101. 
  • Phase I and pharmacokinetic study of pazopanib and lapatinib combination therapy in patients with advanced solid tumors. 
  • Phase I pharmacokinetic studies evaluating single and multiple doses of oral GW572016, a dual EGFR-ErbB2 inhibitor, in healthy subjects. 
  • Phase I safety, pharmacokinetics, and clinical activity study of lapatinib (GW572016), a reversible dual inhibitor of epidermal growth factor receptor tyrosine kinases, in heavily pretreated patients with metastatic carcinomas. 
  • Phase I safety, pharmacokinetics, and inhibition of SRC activity study of saracatinib in patients with solid tumors. 
  • Phase I study and biomarker analysis of lapatinib and concurrent radiation for locally advanced breast cancer. 
  • Phase II study of predictive biomarker profiles for response targeting human epidermal growth factor receptor 2 (HER-2) in advanced inflammatory breast cancer with lapatinib monotherapy. 
  • Phase II study of saracatinib (AZD0530) in patients with previously treated metastatic colorectal cancer. 
  • Phase II study to evaluate the efficacy and safety of neoadjuvant lapatinib plus paclitaxel in patients with inflammatory breast cancer. 
  • Phase II trial of ZD1694 (Tomudex) in patients with advanced pancreatic cancer. 
  • Phase II trial of bevacizumab and erlotinib in patients with recurrent malignant glioma. 
  • Phase II trial of erlotinib in gastroesophageal junction and gastric adenocarcinomas: SWOG 0127. 
  • Phase II trial of gefitinib in recurrent glioblastoma. 
  • Phase II trial of lapatinib for brain metastases in patients with human epidermal growth factor receptor 2-positive breast cancer. 
  • Phase II trial of the combination of bevacizumab and erlotinib in patients who have advanced hepatocellular carcinoma. 
  • Photo-activated psoralen binds the ErbB2 catalytic kinase domain, blocking ErbB2 signaling and triggering tumor cell apoptosis. 
  • Photoaffinity cross-linking of a radioiodinated probe, 125I-A55453, into alpha 1-adrenergic receptors. 
  • Pleiotropic coupling of G protein-coupled receptors to the mitogen-activated protein kinase cascade. Role of focal adhesions and receptor tyrosine kinases. 
  • Polyclonal immune responses to antigens associated with cancer signaling pathways and new strategies to enhance cancer vaccines. 
  • Potentiation of the effect of erlotinib by genistein in pancreatic cancer: the role of Akt and nuclear factor-kappaB. 
  • Prevention of Barrett esophagus and esophageal adenocarcinoma by smoothened inhibitor in a rat model of gastroesophageal reflux disease. 
  • Primary systemic therapy in HER2-amplified breast cancer: a clinical review. 
  • Proceedings of the 99th meeting of the Food and Drug Administration Cardiovascular and Renal Drugs Advisory Committee. May 29th and 30th, 2003. 
  • Prospective trial of synchronous bevacizumab, erlotinib, and concurrent chemoradiation in locally advanced head and neck cancer. 
  • Protein kinase B controls transcriptional programs that direct cytotoxic T cell fate but is dispensable for T cell metabolism. 
  • Quantitative high-throughput efficacy profiling of approved oncology drugs in inflammatory breast cancer models of acquired drug resistance and re-sensitization. 
  • Randomized phase II multicenter trial of two schedules of lapatinib as first- or second-line monotherapy in patients with advanced or metastatic non-small cell lung cancer. 
  • Randomized phase II study of gefitinib versus erlotinib in patients with advanced non-small cell lung cancer who failed previous chemotherapy. 
  • Randomized phase II trial of erlotinib alone or with carboplatin and paclitaxel in patients who were never or light former smokers with advanced lung adenocarcinoma: CALGB 30406 trial. 
  • Randomized study of Lapatinib alone or in combination with trastuzumab in women with ErbB2-positive, trastuzumab-refractory metastatic breast cancer. 
  • Regulation of survivin by ErbB2 signaling: therapeutic implications for ErbB2-overexpressing breast cancers. 
  • Reply to Frange and Leruez-Ville, "Caution Is Required before Recommending Wide Use of Letermovir as Salvage Therapy for Cytomegalovirus Diseases". 
  • Resistance to ErbB2 tyrosine kinase inhibitors in breast cancer is mediated by calcium-dependent activation of RelA. 
  • Resistance to tyrosine kinase inhibition by mutant epidermal growth factor receptor variant III contributes to the neoplastic phenotype of glioblastoma multiforme. 
  • Role of endocytosis in the activation of the extracellular signal-regulated kinase cascade by sequestering and nonsequestering G protein-coupled receptors. 
  • Selection bias, phase II trials, and the FDA accelerated approval process. 
  • Signal transduction through substance P receptor in human glioblastoma cells: roles for Src and PKCdelta. 
  • Single-agent lapatinib for HER2-overexpressing advanced or metastatic breast cancer that progressed on first- or second-line trastuzumab-containing regimens. 
  • Spectrum of ocular toxicities from epidermal growth factor receptor inhibitors and their intermediate-term follow-up: a five-year review. 
  • Stereoselective synthesis of 2,6-cis- and 2,6-trans-piperidines through organocatalytic aza-Michael reactions: a facile synthesis of (+)-myrtine and (-)-epimyrtine. 
  • Study of the biologic effects of lapatinib, a reversible inhibitor of ErbB1 and ErbB2 tyrosine kinases, on tumor growth and survival pathways in patients with advanced malignancies. 
  • Suppression of lipopolysaccharide-stimulated release of tumor necrosis factor by adenosine: evidence for A2 receptors on rat Kupffer cells. 
  • Synergism from combined immunologic and pharmacologic inhibition of HER2 in vivo. 
  • Synthesis and biological evaluation of 4-amino derivatives of benzimidazoquinoxaline, benzimidazoquinoline, and benzopyrazoloquinazoline as potent IKK inhibitors. 
  • TD-19, an erlotinib derivative, induces epidermal growth factor receptor wild-type nonsmall-cell lung cancer apoptosis through CIP2A-mediated pathway. 
  • Targeted therapies for cancer 2004. 
  • Targeted therapy in rectal cancer. 
  • Targeting ABL1-mediated oxidative stress adaptation in fumarate hydratase-deficient cancer. 
  • Targeting HER2 in brain metastases from breast cancer. 
  • Targeting the future in head and neck cancer. 
  • Targeting the histone methyltransferase G9a activates imprinted genes and improves survival of a mouse model of Prader-Willi syndrome. 
  • The addition of erlotinib to gemcitabine and cisplatin does not appear to improve median survival in metastatic pancreatic cancer. 
  • The combined effect of prazosin and autogenic training on cold reactivity in Raynaud's phenomenon. 
  • The cytoplasmic prolyl-tRNA synthetase of the malaria parasite is a dual-stage target of febrifugine and its analogs. 
  • The dual ErbB1/ErbB2 inhibitor, lapatinib (GW572016), cooperates with tamoxifen to inhibit both cell proliferation- and estrogen-dependent gene expression in antiestrogen-resistant breast cancer. 
  • The effects of ZD6474, an inhibitor of VEGF signaling, on cutaneous wound healing in mice. 
  • The rexinoid LG100268 and the synthetic triterpenoid CDDO-methyl amide are more potent than erlotinib for prevention of mouse lung carcinogenesis. 
  • Transactivation of the epidermal growth factor receptor mediates parathyroid hormone and prostaglandin F2 alpha-stimulated mitogen-activated protein kinase activation in cultured transgenic murine osteoblasts. 
  • Transforming growth factor alpha expression drives constitutive epidermal growth factor receptor pathway activation and sensitivity to gefitinib (Iressa) in human pancreatic cancer cell lines. 
  • Transient inhibition of ATM kinase is sufficient to enhance cellular sensitivity to ionizing radiation. 
  • Trastuzumab emtansine (T-DM1) versus lapatinib plus capecitabine in patients with HER2-positive metastatic breast cancer and central nervous system metastases: a retrospective, exploratory analysis in EMILIA. 
  • Trastuzumab emtansine for HER2-positive advanced breast cancer. 
  • Trastuzumab emtansine versus capecitabine plus lapatinib in patients with previously treated HER2-positive advanced breast cancer (EMILIA): a descriptive analysis of final overall survival results from a randomised, open-label, phase 3 trial. 
  • Truncated ErbB2 expressed in tumor cell nuclei contributes to acquired therapeutic resistance to ErbB2 kinase inhibitors. 
  • Truncated ErbB2 receptor (p95ErbB2) is regulated by heregulin through heterodimer formation with ErbB3 yet remains sensitive to the dual EGFR/ErbB2 kinase inhibitor GW572016. 
  • Tyrosine phosphorylation of the human glutathione S-transferase P1 by epidermal growth factor receptor. 
  • Use of Letermovir as Salvage Therapy for Drug-Resistant Cytomegalovirus Retinitis. 
  • Vandetanib for the treatment of patients with locally advanced or metastatic hereditary medullary thyroid cancer. 
  • Vandetanib, a novel multitargeted kinase inhibitor, in cancer therapy. 
  • Vascular endothelial growth factor signaling is necessary for expansion of medullary microvessels during postnatal kidney development. 
  • X-linked inhibitor of apoptosis protein inhibits apoptosis in inflammatory breast cancer cells with acquired resistance to an ErbB1/2 tyrosine kinase inhibitor. 
  • ZD6474, a novel tyrosine kinase inhibitor of vascular endothelial growth factor receptor and epidermal growth factor receptor, inhibits tumor growth of multiple nervous system tumors. 
  • beta-Arrestin 2 expression determines the transcriptional response to lysophosphatidic acid stimulation in murine embryo fibroblasts. 
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  Keywords of People

  • Abbruzzese, James, D. C. I. Distinguished Professor of Medical Oncology, Medicine, Medical Oncology
  • Craciunescu, Oana, Professor of Radiation Oncology, Radiation Oncology
  • Sampson, John Howard, Robert H., M.D. and Gloria Wilkins Professor of Neurosurgery, in the School of Medicine, Immunology