Search results for "nitriles"

showing 10 items of 177 documents

The Clinical Efficacy of Enzalutamide in Metastatic Prostate Cancer: Prospective Single-center Study

2017

Background/Aim: To evaluate the effectiveness of enzalutamide in Italian patients with hormone-refractory metastatic castration-resistant prostate cancer, progressing after chemotherapy with docetaxel plus prednisone. Patients and Methods: A total of 60 patients were enrolled. Reduction in serum prostate-specific antigen (PSA) was assessed as the primary endpoint, while reduction in pain, safety, progression-free survival and overall survival represented secondary endpoints. Results: Enzalutamide was well tolerated, with a manageable toxicity profile and a modest objective response rate. A considerable difference in serum levels of PSA before and after treatment was observed. A significant …

Male0301 basic medicineOncologyCancer Researchmedicine.medical_treatmentDocetaxelKaplan-Meier Estimateurologic and male genital diseasesDrug resistantAntineoplastic Agentchemistry.chemical_compoundProstate cancer0302 clinical medicinePrednisoneClinical endpointProspective StudiesNeoplasm MetastasisProspective cohort studyAged 80 and overProstate cancerGeneral MedicineMiddle AgedNeoplasm MetastasiProstatic Neoplasms Castration-ResistantProstate-specific antigenTreatment OutcomeOncologyDocetaxel030220 oncology & carcinogenesisBenzamidesRegression AnalysisTaxoidsHumanmedicine.drugmedicine.medical_specialtyAntineoplastic AgentsAdenocarcinomaRegression Analysi03 medical and health sciencesTaxoidInternal medicineNitrilesPhenylthiohydantoinEnzalutamidemedicineChemotherapyHumansEnzalutamideAgedChemotherapybusiness.industryProstatic NeoplasmsProstate-Specific Antigenmedicine.diseaseProspective Studie030104 developmental biologychemistryDrug Resistance NeoplasmProstatic NeoplasmPrednisonebusinessAnticancer Research
researchProduct

Irreversible binding of acrylonitrile to nucleic acids

1983

1. [2,3-14C]Acrylonitrile was incubated with rat-liver microsomes, NADPH and either DNA, RNA or bovine serum albumin. Irreversible binding occurred to the macromolecular targets. Binding was lower when incubations were performed without microsomes. 2. Most of the 14C bound to DNA, RNA or polynucleotides (poly-A, poly-C, poly-G, poly-U) after incubation of [2,3-14C]acrylonitrile with rat-liver microsomes and 'conventional' re-isolation of the nucleic acids was removed from the macromolecular target when subsequently chromatographed on hydroxyapatite. 3. Radioactivity attached to DNA after prolonged non-enzymic incubations with [2,3-14C]acrylonitrile was also removed from the DNA by chromatog…

MaleAlkylationHealth Toxicology and MutagenesisIn Vitro TechniquesToxicologyBiochemistrychemistry.chemical_compoundNucleic AcidsNitrilesAnimalsCarbon RadioisotopesBovine serum albuminPharmacologyAcrylonitrilebiologyRNARats Inbred StrainsGeneral MedicineRatschemistryBiochemistryPolynucleotideMicrosomes Liverbiology.proteinMicrosomeNucleic acidAcrylonitrileDNAMacromoleculeXenobiotica
researchProduct

Irreversible protein binding of acrylonitrile.

1981

1. After i.p. injection of [2,3-14C]acrylonitrile to rats, a significant portion of radioactivity becomes irreversibly attached to proteins of liver, lung, spleen and other tissues. 2. When rat liver microsomes were incubated with [2,3-14C]acrylonitrile, a time-dependent irreversible binding of radioactivity occurred to microsomal proteins. This binding was not dependent on NADPH. A high extent of binding to heat-inactivated microsomes indicated that no enzymic metabolic step was involved. 3. The irreversible binding of [2,3-14C]acrylonitrile to rat liver microsomal protein in vitro was inhibited by thiols (cysteine, glutathione, mercaptoethanol). The greatest inhibitory potency was display…

MaleHot TemperatureHealth Toxicology and MutagenesisSpleenPlasma protein bindingToxicologyBiochemistryDithiocarbchemistry.chemical_compoundNitrilesmedicineAnimalsSulfhydryl CompoundsPharmacologyAcrylonitrileChemistryGeneral MedicineGlutathioneIn vitroRatsmedicine.anatomical_structureBiochemistryLiverMicrosomeMicrosomes LiverAcrylonitrileDitiocarbSpleenCysteineProtein BindingXenobiotica; the fate of foreign compounds in biological systems
researchProduct

Transmission of HIV Drug Resistance and the Predicted Effect on Current First-line Regimens in Europe

2016

Transmitted human immunodeficiency virus drug resistance in Europe is stable at around 8%. The impact of baseline mutation patterns on susceptibility to antiretroviral drugs should be addressed using clinical guidelines. The impact on baseline susceptibility is largest for nonnucleoside reverse transcriptase inhibitors.

MaleHuman immunodeficiency virus 1EtravirineRNA directed DNA polymerase inhibitordarunavirHIV InfectionsSettore MED/42 - Igiene Generale E Applicata:Disciplines and Occupations::Health Occupations::Medicine::Public Health [Medical Subject Headings]:Organisms::Eukaryota::Animals::Chordata::Vertebrates::Mammals::Primates::Haplorhini::Catarrhini::Hominidae::Humans [Medical Subject Headings]Salud públicageneticsInhibidores de proteasas:Analytical Diagnostic and Therapeutic Techniques and Equipment::Investigative Techniques::Epidemiologic Methods::Data Collection::Vital Statistics::Morbidity::Prevalence [Medical Subject Headings]atazanavirmedia_commontransmission:Geographicals::Geographic Locations::Europe [Medical Subject Headings]3. Good healthmicrobial sensitivity testpriority journalEurope ; HIV-1 ; antiretroviral therapy ; drug resistance ; transmissionHIV/AIDSlamivudineReverse Transcriptase Inhibitors/pharmacologyanti human immunodeficiency virus agentDrugMicrobiology (medical)medicine.medical_specialtyantiviral susceptibility:Phenomena and Processes::Genetic Phenomena::Genetic Variation::Mutation [Medical Subject Headings]media_common.quotation_subjectantiretroviral therapy030106 microbiologyHIV Infections/drug therapy:Chemicals and Drugs::Chemical Actions and Uses::Pharmacologic Actions::Therapeutic Uses::Anti-Infective Agents::Antiviral Agents::Anti-Retroviral Agents::Reverse Transcriptase Inhibitors [Medical Subject Headings]Microbial Sensitivity TestsRILPIVIRINEArticleEFAVIRENZ03 medical and health sciencestransmitted drug resistanceSDG 3 - Good Health and Well-beingHumansTransmissionhuman:Phenomena and Processes::Physiological Phenomena::Pharmacological Phenomena::Drug Resistance [Medical Subject Headings]REVERSE-TRANSCRIPTASE INHIBITORSRilpivirinaINTEGRASEMUTATIONSabacavirmajor clinical studyVirologyInfecciones por VIHRegimenAntiretroviral therapy; Drug resistance; Europe; HIV-1; Transmission; Medicine (all); Microbiology (medical); Infectious DiseaseschemistryDrug resistance:Chemicals and Drugs::Heterocyclic Compounds::Heterocyclic Compounds 1-Ring::Oxazines::Benzoxazines [Medical Subject Headings]MutationHIV-10301 basic medicinenevirapineDrug resistanceCommunicable diseases:Analytical Diagnostic and Therapeutic Techniques and Equipment::Investigative Techniques::Epidemiologic Methods::Statistics as Topic::Confidence Intervals [Medical Subject Headings]chemistry.chemical_compoundantiviral therapyINFECTIONMedicine and Health SciencesPrevalence:Analytical Diagnostic and Therapeutic Techniques and Equipment::Investigative Techniques::Epidemiologic Methods::Data Collection::Surveys and Questionnaires [Medical Subject Headings]ViralNon-U.S. Gov'tReverse-transcriptase inhibitorantiretrovirus agentResearch Support Non-U.S. Gov'tMedicine (all)Human immunodeficiency virus infected patientMiddle AgedvirologyPREVALENCEAntiretroviral therapyEncuestas y CuestionariosANTIRETROVIRAL TREATMENTEuropeInfectious DiseasesHIV-1/drug effectsHIV Protease Inhibitors/pharmacologyRilpivirineReverse Transcriptase Inhibitors:Diseases::Immune System Diseases::Immunologic Deficiency Syndromes::HIV Infections [Medical Subject Headings]FemaleHIV drug resistancemedicine.drugAdultHuman immunodeficiency virus proteinase inhibitor:Chemicals and Drugs::Organic Chemicals::Nitriles::Rilpivirine [Medical Subject Headings]EfavirenzAnti-HIV AgentsResearch SupportResistencia a medicamentosSettore MED/17 - MALATTIE INFETTIVEantiviral resistanceInternal medicineAnti-HIV Agents/pharmacologyDrug Resistance ViralJournal Articlemedicine:Chemicals and Drugs::Chemical Actions and Uses::Pharmacologic Actions::Molecular Mechanisms of Pharmacological Action::Enzyme Inhibitors::Protease Inhibitors [Medical Subject Headings]abacavir plus lamivudineEuropa (Continente)Antiretroviral therapy; Drug resistance; Europe; HIV-1; Transmission; Adult; Anti-HIV Agents; Drug Resistance Viral; Europe; Female; HIV Infections; HIV Protease Inhibitors; HIV-1; Humans; Male; Microbial Sensitivity Tests; Middle Aged; Mutation; Prevalence; Reverse Transcriptase Inhibitors; Microbiology (medical); Infectious DiseasesemtricitabinenonhumanIntervalos de confianzadrug resistanceMutaciónAntiretroviral therapy; Drug resistance; Europe; HIV-1; Transmissionbusiness.industryHIVpredictionInhibidores de la transcriptasa inversaHIV Protease InhibitorsHuman immunodeficiency virus 1 infectiontenofovirINDIVIDUALSDrug Resistance Viral/geneticsBenzoxazinasETRAVIRINEdrug effects3121 General medicine internal medicine and other clinical medicinePrevalenciabusiness
researchProduct

Phosphorylation of extracellular signal-related protein kinase is required for rapid facilitation of heat-induced currents in rat dorsal root ganglio…

2005

A subgroup of dorsal root ganglion (DRG) neurons responds to noxious heat with an influx of cations carried by specific ion channels such as the transient receptor potential channel of the vanilloid receptor type, subtype 1 (TRPV1). Application of capsaicin induces a reversible facilitation of these currents. This facilitation could be an interaction of two agonists at their common receptor or be caused by an influx of calcium ions into the cell. Calcium influx into the cell can activate protein kinases such as the extracellular signal-related protein kinase (ERK) pathway. This study explored the kinetics, calcium-dependency and intracellular signals following application of capsaicin and l…

MaleMAPK/ERK pathwayHot TemperaturePatch-Clamp TechniquesStatistics as TopicTRPV1BiologyMembrane PotentialsRats Sprague-Dawleychemistry.chemical_compoundBAPTAGanglia SpinalNitrilesButadienesAnimalsDrug InteractionsEnzyme InhibitorsPhosphorylationExtracellular Signal-Regulated MAP KinasesProtein kinase AProtein kinase CNeuronsAnalysis of VarianceDose-Response Relationship DrugGeneral NeuroscienceMEK inhibitorRatsCell biologychemistryBiochemistryCapsaicinMitogen-activated protein kinasebiology.proteinCalciumFemaleCapsaicinNeuroscience
researchProduct

Inactivation of glycogen synthase kinase-3β protects against kainic acid-induced neurotoxicity in vivo

2004

Many neurodegenerative diseases involve oxidative stress and excitotoxic cell death. In an attempt to further elucidate the signal transduction pathways involved in the cell death/cell survival associated with excitotoxicity, we have used an in vivo model of excitotoxicity employing kainic acid (KA)-induced neurotoxicity. Here, we show that extracellular signal-related kinase (ERK) 2, but not ERK 1, is phosphorylated and thereby activated in the hippocampus and cerebellum of kainic acid-treated mice. Phosphorylation and hence inactivation of glycogen synthase kinase 3beta (GSK-3beta), a general survival factor, is often a downstream consequence of mitogen-activated protein kinase pathway ac…

MaleMAPK/ERK pathwayKainic acidProgrammed cell deathTime FactorsCell SurvivalBlotting WesternExcitotoxicityTetrazolium Saltsmacromolecular substancesBiologymedicine.disease_causeHippocampusGlycogen Synthase Kinase 3Micechemistry.chemical_compoundOrgan Culture TechniquesGSK-3CerebellumNitrilesButadienesSerinemedicineAnimalsEnzyme InhibitorsPhosphorylationProtein kinase AMolecular BiologyMitogen-Activated Protein Kinase 1Glycogen Synthase Kinase 3 betaKainic AcidBehavior AnimalCell DeathKinaseGeneral NeuroscienceImmunohistochemistryCell biologyEnzyme ActivationThiazolesBiochemistrychemistryTyrosineNeurotoxicity SyndromesNeurology (clinical)Signal transductionLithium ChlorideDevelopmental BiologyBrain Research
researchProduct

Intraspecific Communication Through Chemical Signals in Female Mice: Reinforcing Properties of Involatile Male Sexual Pheromones

2006

In rodents, social and reproductive behaviors critically depend on chemical signals, including sexual pheromones that have been suggested (but not demonstrated) to be rewarding. In this work, we analyze this issue by studying the chemoinvestigatory behavior of adult female mice (without experience with male-derived chemicals) toward 1) the synthetic odorant citralva, 2) bedding soiled by different conspecifics (females, males, and castrated males), and 3) volatiles derived from bedding soiled by males and castrated males (confronted in 2-choice tests). We also study whether these chemical signals are able to induce conditioned place preference, a reliable test for rewarding properties of st…

MaleOlfactory systemVomeronasal organPhysiologyZoologyolfactory systemplace preferenceBiologyIntraspecific competitionvomeronasal systemMiceBehavioral Neurosciencesexual behaviorPhysiology (medical)Conditioning PsychologicalNitrilesAnimalsAnimal communicationSex AttractantsHabituationrewardCommunicationbusiness.industryBedding and LinensStimulation ChemicalSensory SystemsConditioned place preferenceAnimal CommunicationSex pheromoneOdorantsPheromoneFemaleVolatilizationbusinessChemical Senses
researchProduct

Disseminated tuberculosis in a patient treated with a JAK2 selective inhibitor: a case report

2012

Abstract Background Primary myelofibrosis is a myeloproliferative disorder characterized by bone marrow fibrosis, abnormal cytokine expression, splenomegaly and anemia. The activation of JAK2 and the increased levels of circulating proinflammatory cytokines seem to play an important role in the pathogenesis of myelofibrosis. Novel therapeutic agents targeting JAKs have been developed for the treatment of myeloproliferative disorders. Ruxolitinib (INCB018424) is the most recent among them. Case presentation To our knowledge, there is no evidence from clinical trials of an increased risk of tuberculosis during treatment with JAK inhibitors. Here we describe the first case of tuberculosis in a…

MaleOncologymedicine.medical_specialtyRuxolitinibTuberculosisSettore MED/17 - Malattie InfettiveAnemiaAntitubercular AgentsMyelofibrosislcsh:MedicineCase ReportGeneral Biochemistry Genetics and Molecular BiologyProinflammatory cytokineMyeloproliferative DisordersInternal medicineNitrilesmedicineHumansTuberculosisMyelofibrosislcsh:Science (General)lcsh:QH301-705.5Medicine(all)Janus kinase 2biologyLatent tuberculosisBiochemistry Genetics and Molecular Biology(all)business.industryTuberculosis Myelofibrosis Ruxolitiniblcsh:RGeneral MedicineJanus Kinase 2medicine.diseasePyrimidinesRuxolitiniblcsh:Biology (General)Primary MyelofibrosisImmunologybiology.proteinPyrazolesbusinessmedicine.druglcsh:Q1-390BMC Research Notes
researchProduct

Effects of Vildagliptin/Metformin Therapy on Patient-Reported Outcomes: Work Productivity, Patient Satisfaction, and Resource Utilization

2013

Introduction: Type 2 diabetes mellitus (T2DM) is associated not only with high direct healthcare costs, but also with indirect costs, as diabetic complications and the disease itself result in loss of productivity. Vildagliptin is a novel dipeptidyl peptidase-4 inhibitor that is given either alone or in combination with oral hypoglycemic drugs, including metformin. The study was designed to assess the hypothesis that fixed-combination vildagliptin/metformin improves work productivity measured as Work Productivity and Activity Impairment (WPAI) scores. Secondary objectives were the assessment of patient satisfaction by means of the Diabetes Treatment Satisfaction Questionnaire (DTSQs), the c…

MalePyrrolidinesSettore MED/09 - Medicina Internaendocrine system diseasesAdamantaneEfficiencyoutcomeschemistry.chemical_compoundIndirect costsDiabetes mellitusVildagliptinPharmacology (medical)Prospective StudiesPatient-reported outcomeProductivityAged 80 and overVildagliptinMedicine(all)Health Care CostsGeneral MedicineHealth ServicesMiddle AgedMetforminMetforminType 2 diabetes mellituDrug CombinationsTreatment OutcomeItalyPatient SatisfactionFemalemedicine.drugAdultEmploymentResourcemedicine.medical_specialtyDiabetes mellitus; oral antidiabetics; vildagliptin; outcomesoral antidiabeticsPatient satisfactionInternal medicineDiabetes mellitusNitrilesmedicineHumansHypoglycemic AgentsHealthcare costFixed combinationAgedbusiness.industryType 2 Diabetes Mellitusnutritional and metabolic diseasesmedicine.diseaseEndocrinologyDiabetes Mellitus Type 2chemistryEmergency medicineObservational studyGlycated hemoglobinbusinessAdvances in Therapy
researchProduct

Cytostatic Activity of Aeroplysinin-1 against Lymphoma and Epithelioma Cells

1989

(±)-Aeroplysinin-1, an optically active 1.2-dihydroarene-1.2-diol. was isolated from the marine sponges Verongia aerophoba (+-isomer) and lanthella ardis (--isomer). For the experiments presented we used the +-isomer from Verongia aerophoba. Here we describe the hitherto unknown biological and pharmacological property of this compound to display pronounced anticancer activity against L5178y mouse lymphoma cells (ED50: 0.5 μm). Friend erythroleukemia cells (ED50: 0.7μm) , human mamma carcinoma cells (ED50: 0.3μm) and human colon carcinoma cells (ED50: 3.0 μm) in vitro. Furthermore, aeroplysinin caused a preferential inhibition of [3H]thymidine (dThd) incorporation rates in L5178y mouse lymph…

MaleSalmonella typhimuriumAcetonitrilesCell SurvivalCellAntineoplastic AgentsMice Inbred StrainsBiologyGeneral Biochemistry Genetics and Molecular BiologyCell LineMicechemistry.chemical_compoundIn vivoCyclohexenesTumor Cells CulturedmedicineCarcinomaAnimalsHumansLeukemia L5178ED50Leukemia ExperimentalMutagenicity TestsMelanomaCarcinomamedicine.diseaseVirologyMolecular biologyIn vitroLymphomamedicine.anatomical_structurechemistryDrug Screening Assays AntitumorThymidineZeitschrift für Naturforschung C
researchProduct