Thiazoles

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  Subject Areas on Research

  • A Systematic Analysis of Mosquito-Microbiome Biosynthetic Gene Clusters Reveals Antimalarial Siderophores that Reduce Mosquito Reproduction Capacity. 
  • A futile metabolic cycle activated in adipocytes by antidiabetic agents. 
  • A novel N-aryl tyrosine activator of peroxisome proliferator-activated receptor-gamma reverses the diabetic phenotype of the Zucker diabetic fatty rat. 
  • A phase I trial of dasatinib, an SRC-family kinase inhibitor, in combination with paclitaxel and carboplatin in patients with advanced or recurrent ovarian cancer. 
  • A phase II study of dasatinib in patients with chemosensitive relapsed small cell lung cancer (Cancer and Leukemia Group B 30602). 
  • A small-molecule antagonist of the hedgehog signaling pathway. 
  • A sphingosine kinase inhibitor induces cell death in temozolomide resistant glioblastoma cells. 
  • A study of the binding of thiamine diphosphate and thiochrome diphosphate to the pyruvate dehydrogenase multienzyme complex. 
  • Activity and distribution of the cysteine prodrug activating enzyme, 5-oxo-L-prolinase, in human normal and tumor tissues. 
  • Acto-myosin drug effects and aqueous outflow function. 
  • Acute dystonic reaction with moderate-dose ziprasidone. 
  • Acute management of stroke patients taking non-vitamin K antagonist oral anticoagulants Addressing Real-world Anticoagulant Management Issues in Stroke (ARAMIS) Registry: Design and rationale. 
  • Agonist-stimulated beta-adrenergic receptor internalization requires dynamic cytoskeletal actin turnover. 
  • Alternatives to warfarin for stroke prevention in patients with nonvalvular atrial fibrillation: a look back at the state of the field in 2012. 
  • Anticolon cancer activity of largazole, a marine-derived tunable histone deacetylase inhibitor. 
  • Antifungal resistance: the clinical front. 
  • Antithrombotic therapy for patients with atrial fibrillation undergoing percutaneous coronary intervention: balance best with double antithrombotic therapy. 
  • Antithrombotic treatment strategies after PCI. 
  • Atypical antipsychotic drugs and diabetes mellitus in a large outpatient population: a retrospective cohort study. 
  • Atypical antipsychotics and pituitary tumors: a pharmacovigilance study. 
  • Atypical antipsychotics rapidly and inappropriately switch peripheral fuel utilization to lipids, impairing metabolic flexibility in rodents. 
  • Can binimetinib, encorafenib and masitinib be more efficacious than currently available mutation-based targeted therapies for melanoma treatment? 
  • Caveats to the use of MTT, neutral red, Hoechst and Resazurin to measure silver nanoparticle cytotoxicity. 
  • Changes in Aβ biomarkers and associations with APOE genotype in 2 longitudinal cohorts. 
  • Changing practice of anticoagulation: will target-specific anticoagulants replace warfarin? 
  • Characteristics of the MATRICS Consensus Cognitive Battery in a 29-site antipsychotic schizophrenia clinical trial. 
  • Comparative toxicities of selected compounds to nauplii of Balanus amphitrite amphitrite Darwin and Artemia sp. 
  • Comparison of outcomes for African Americans, Hispanics, and Non-Hispanic Whites in the CATIE study. 
  • Constitutive salicylic acid-dependent signaling in cpr1 and cpr6 mutants requires PAD4. 
  • Continuous anticoagulation with catheter ablation: answers and questions. 
  • Correspondence between in vivo (11)C-PiB-PET amyloid imaging and postmortem, region-matched assessment of plaques. 
  • Cryptosporidium-malnutrition interactions: mucosal disruption, cytokines, and TLR signaling in a weaned murine model. 
  • Dasatinib (BMS-35482) has synergistic activity with paclitaxel and carboplatin in ovarian cancer cells. 
  • Dasatinib (BMS-35482) interacts synergistically with docetaxel, gemcitabine, topotecan, and doxorubicin in ovarian cancer cells with high SRC pathway activation and protein expression. 
  • Dasatinib combined with docetaxel for castration-resistant prostate cancer: results from a phase 1-2 study. 
  • Decreased synthesis of matrix metalloproteinase-7 and adhesion to the extracellular matrix proteins of human colon cancer cells treated with troglitazone. 
  • Dendritic macromers as in situ polymerizing biomaterials for securing cataract incisions. 
  • Diatom gliding is the result of an actin-myosin motility system. 
  • Differentiation- and stress-dependent nuclear cytoplasmic redistribution of myopodin, a novel actin-bundling protein. 
  • Docetaxel and dasatinib or placebo in men with metastatic castration-resistant prostate cancer (READY): a randomised, double-blind phase 3 trial. 
  • Dopamine D2 receptor occupancy and cognition in schizophrenia: analysis of the CATIE data. 
  • Drug rash with eosinophilia and systemic symptoms (DRESS syndrome). 
  • Dual inhibition of αV integrins and Src kinase activity as a combination therapy strategy for colorectal cancer. 
  • Edoxaban and the need for outcomes-based NOAC dosing. 
  • Edoxaban in the secondary prevention of VTE. 
  • Edoxaban versus warfarin in patients with atrial fibrillation. 
  • Effect of metabotropic glutamate 5 receptor antagonists on morphine efficacy and tolerance in rats with neuropathic pain. 
  • Effect of pain management on immunization efficacy in mice. 
  • Effectiveness of antipsychotic drugs in patients with chronic schizophrenia. 
  • Effectiveness of clozapine versus olanzapine, quetiapine, and risperidone in patients with chronic schizophrenia who did not respond to prior atypical antipsychotic treatment. 
  • Effectiveness of lurasidone in patients with schizophrenia or schizoaffective disorder switched from other antipsychotics: a randomized, 6-week, open-label study. 
  • Effectiveness of olanzapine, quetiapine, risperidone, and ziprasidone in patients with chronic schizophrenia following discontinuation of a previous atypical antipsychotic. 
  • Effects of antipsychotic medications on psychosocial functioning in patients with chronic schizophrenia: findings from the NIMH CATIE study. 
  • Efficacy and safety of reduced-dose non-vitamin K antagonist oral anticoagulants in patients with atrial fibrillation: a meta-analysis of randomized controlled trials. 
  • Enhanced catalytic DNAzyme for label-free colorimetric detection of DNA. 
  • Environmental factors influence the production of enterobactin, salmochelin, aerobactin, and yersiniabactin in Escherichia coli strain Nissle 1917. 
  • Evaluation of class I HDAC isoform selectivity of largazole analogues. 
  • Fatty acid elongase-5 (Elovl5) regulates hepatic triglyceride catabolism in obese C57BL/6J mice. 
  • Fatty acid homeostasis and induction of lipid regulatory genes in skeletal muscles of peroxisome proliferator-activated receptor (PPAR) alpha knock-out mice. Evidence for compensatory regulation by PPAR delta. 
  • Fluorescence energy transfer between the thiamine diphosphate and flavine adenine dinucleotide binding sites on the pyruvate dehydrogenase multienzyme complex. 
  • Fluorescent derivatives of the pyruvate dehydrogenase component of the Escherichia coli pyruvate dehydrogenase complex. 
  • Glucose intolerance, insulin resistance, and pathological features of Alzheimer disease in the Baltimore Longitudinal Study of Aging. 
  • High-dose oral ziprasidone versus conventional dosing in schizophrenia patients with residual symptoms: the ZEBRAS study. 
  • Hypoxia-independent activation of HIF-1 by enterobacteriaceae and their siderophores. 
  • Imidazo[4,5-d]thiazolo[5,4-b]pyridine based inhibitors of IKK2: synthesis, SAR, PK/PD and activity in a preclinical model of rheumatoid arthritis. 
  • Impact of antipsychotic treatment on nonfasting triglycerides in the CATIE Schizophrenia Trial phase 1. 
  • Implications of atypical antipsychotic prescribing in the intensive care unit. 
  • Improving frontline treatment for chronic myeloid leukemia: emerging evidence for use of nilotinib and dasatinib. 
  • In vivo dynamics of clathrin and its adaptor-dependent recruitment to the actin-based endocytic machinery in yeast. 
  • Increased Metabotropic Glutamate Receptor 5 Signaling Underlies Obsessive-Compulsive Disorder-like Behavioral and Striatal Circuit Abnormalities in Mice. 
  • Increased resistance of tumor cells to hyperthermia mediated by integrin-linked kinase. 
  • Influence of Kidney Function Estimation Methods on Eligibility for Edoxaban Population Impact of the US Food and Drug Administration's Approach for Its Product Labeling. 
  • Inhibition of SRC expression and activity inhibits tumor progression and metastasis of human pancreatic adenocarcinoma cells in an orthotopic nude mouse model. 
  • Inhibition of corneal neovascularization in the rat by SK&F 86002, a dual inhibitor of arachidonic acid metabolism. 
  • Initial testing of dasatinib by the pediatric preclinical testing program. 
  • Internalization is essential for the antiapoptotic effects of exogenous thymosin beta-4 on human corneal epithelial cells. 
  • Intravenous ziprasidone for treatment of delirium in the intensive care unit. 
  • Invasive prostate carcinoma driven by c-Src and androgen receptor synergy. 
  • Involvement of the mt1 melatonin receptor in human breast cancer. 
  • Largazole pharmacokinetics in rats by LC-MS/MS. 
  • Largazole: from discovery to broad-spectrum therapy. 
  • Masitinib is a broad coronavirus 3CL inhibitor that blocks replication of SARS-CoV-2. 
  • Mechanism of action of the pyruvate dehydrogenase multienzyme complex from Escherichia coli. 
  • Metabolic network failures in Alzheimer's disease: A biochemical road map. 
  • Neurocognitive effects of antipsychotic medications in patients with chronic schizophrenia in the CATIE Trial. 
  • Nonvitamin K Anticoagulant Agents in Patients With Advanced Chronic Kidney Disease or on Dialysis With AF. 
  • Novel thiazole based heterocycles as inhibitors of LFA-1/ICAM-1 mediated cell adhesion. 
  • Open-label pilot study of ziprasidone for refractory generalized anxiety disorder. 
  • Optimization of a polyglutamine aggregation inhibitor peptide (QBP1) using a thioflavin T fluorescence assay. 
  • Oral factor Xa inhibitors for the prevention of stroke in atrial fibrillation. 
  • Orbital fibroblast heterogeneity may determine the clinical presentation of thyroid-associated ophthalmopathy. 
  • PGC-1alpha regulates a HIF2alpha-dependent switch in skeletal muscle fiber types. 
  • PPARβ/δ selectively regulates phenotypic features of age-related macular degeneration. 
  • Pancreatic expression and secretion of human islet amyloid polypeptide in a transgenic mouse. 
  • Performance and interview-based assessments of cognitive change in a randomized, double-blind comparison of lurasidone vs. ziprasidone. 
  • Periprocedural antithrombotic and bridging therapy: recommendations for standardized reporting in patients with arterial indications for chronic oral anticoagulant therapy. 
  • Pharmacological activation of PPARbeta/delta stimulates utrophin A expression in skeletal muscle fibers and restores sarcolemmal integrity in mature mdx mice. 
  • Pharmacological targeting of GLI1 inhibits proliferation, tumor emboli formation and in vivo tumor growth of inflammatory breast cancer cells. 
  • Phase 1 trial of dasatinib plus erlotinib in adults with recurrent malignant glioma. 
  • Phase I study of dasatinib in combination with capecitabine, oxaliplatin and bevacizumab followed by an expanded cohort in previously untreated metastatic colorectal cancer. 
  • Phase II multicenter trial of voreloxin as second-line therapy in chemotherapy-sensitive or refractory small cell lung cancer. 
  • Phase II study of dasatinib in patients with previously treated malignant mesothelioma (cancer and leukemia group B 30601): a brief report. 
  • Phase II trial of dasatinib in patients with metastatic breast cancer using real-time pharmacodynamic tissue biomarkers of Src inhibition to escalate dosing. 
  • Pseudomonas invasion of type I pneumocytes is dependent on the expression and phosphorylation of caveolin-2. 
  • Quantification and time course of microvascular obstruction by contrast-enhanced echocardiography and magnetic resonance imaging following acute myocardial infarction and reperfusion. 
  • Randomized Trial of the Effect of Four Second-Generation Antipsychotics and One First-Generation Antipsychotic on Cigarette Smoking, Alcohol, and Drug Use in Chronic Schizophrenia. 
  • Reduction of spinal PGE2 concentrations prevents swim stress-induced thermal hyperalgesia. 
  • Retinal microvasculature changes in amyloid-negative subcortical vascular cognitive impairment compared to amyloid-positive Alzheimer's disease. 
  • Revealing the macromolecular targets of complex natural products. 
  • Role of platelet activating factor in the inflammatory and secretory effects of Clostridium difficile toxin A. 
  • Role of platelet activating factor in the intestinal epithelial secretory and Chinese hamster ovary cell cytoskeletal responses to cholera toxin. 
  • Role of platelet-activating factor in Chinese hamster ovary cell responses to cholera toxin. 
  • SRC family kinase inhibition as a novel strategy to augment melphalan-based regional chemotherapy of advanced extremity melanoma. 
  • Saccharomyces cerevisiae Bzz1p is implicated with type I myosins in actin patch polarization and is able to recruit actin-polymerizing machinery in vitro. 
  • Severity of renal impairment in patients with heart failure and atrial fibrillation: implications for non-vitamin K antagonist oral anticoagulant dose adjustment. 
  • Should patients on vitamin K antagonists be treated differently? 
  • Small molecule dual-inhibitors of TRPV4 and TRPA1 for attenuation of inflammation and pain. 
  • Stroke prevention in atrial fibrillation: Closing the gap. 
  • Structural Insights into Electrophile Irritant Sensing by the Human TRPA1 Channel. 
  • Substance use in persons with schizophrenia: baseline prevalence and correlates from the NIMH CATIE study. 
  • Synergistic activity of the SRC family kinase inhibitor dasatinib and oxaliplatin in colon carcinoma cells is mediated by oxidative stress. 
  • Synthesis and activity of largazole analogues with linker and macrocycle modification 
  • Synthesis and biological evaluation of largazole zinc-binding group analogs. 
  • Tenofovir alafenamide for HIV infection: is less more? 
  • Tetomilast: new promise for phosphodiesterase-4 inhibitors? 
  • The Texas Medication Algorithm Project antipsychotic algorithm for schizophrenia: 2003 update. 
  • The current state of care in gout: Addressing the need for better understanding of an ancient disease. 
  • The metabolic regulator ERRα, a downstream target of HER2/IGF-1R, as a therapeutic target in breast cancer. 
  • The neuroprotective agent riluzole inhibits release of glutamate and aspartate from slices of hippocampal area CA1. 
  • The posttranslational modification cascade to the thiopeptide berninamycin generates linear forms and altered macrocyclic scaffolds. 
  • The unanticipated loss of SO2 from sulfonamides in collision-induced dissociation. 
  • Three ring posttranslational circuses: insertion of oxazoles, thiazoles, and pyridines into protein-derived frameworks. 
  • Total synthesis and molecular target of largazole, a histone deacetylase inhibitor. 
  • Trans-arachidonic acids generated during nitrative stress induce a thrombospondin-1-dependent microvascular degeneration. 
  • Treatment outcomes of patients with tardive dyskinesia and chronic schizophrenia. 
  • Troglitazone-associated hepatotoxicity treated successfully with steroids. 
  • Up-regulation of UCP-2 gene expression by PPAR agonists in preadipose and adipose cells. 
  • Uricase and other novel agents for the management of patients with treatment-failure gout. 
  • Voreloxin, a first-in-class anticancer quinolone derivative, in relapsed/refractory solid tumors: a report on two dosing schedules. 
  • Vosaroxin plus cytarabine versus placebo plus cytarabine in patients with first relapsed or refractory acute myeloid leukaemia (VALOR): a randomised, controlled, double-blind, multinational, phase 3 study. 
  • WNT11 expression is induced by estrogen-related receptor alpha and beta-catenin and acts in an autocrine manner to increase cancer cell migration. 
  • What CATIE found: results from the schizophrenia trial. 
  • When evaluating parameter uncertainty is not enough: the case of dasatinib and nilotinib for imatinib-resistant chronic myeloid leukemia. 
  • XBP1 (X-Box-Binding Protein-1)-Dependent O-GlcNAcylation Is Neuroprotective in Ischemic Stroke in Young Mice and Its Impairment in Aged Mice Is Rescued by Thiamet-G. 
  • Ziprasidone-associated mania: a case series and review of the mechanism. 
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  Keywords of People

  • Abbruzzese, James, D. C. I. Distinguished Professor of Medical Oncology, Medicine, Medical Oncology
  • Berchuck, Andrew, James M. Ingram Distinguished Professor of Gynecologic Oncology, Obstetrics and Gynecology, Gynecologic Oncology
  • McCall, Shannon Jones, Associate Professor of Pathology, Pathology
  • Sampson, John Howard, Robert H., M.D. and Gloria Wilkins Professor of Neurosurgery, in the School of Medicine, Biomedical Engineering
  • Uronis, Hope Elizabeth, Associate Professor of Medicine, Medicine, Medical Oncology
  • Zafar, Syed Yousuf, Adjunct Professor in the Department of Medicine, Duke Science & Society