Search results for "Anilides"

showing 10 items of 29 documents

Kinase Inhibitors in Multitargeted Cancer Therapy

2017

The old-fashioned anticancer approaches, aiming in arresting cancer cell proliferation interfering with non-specific targets (e.g. DNA), have been replaced, in the last decades, by more specific target oriented ones. Nonetheless, single-target approaches have not always led to optimal outcomes because, for its complexity, cancer needs to be tackled at various levels by modulation of several targets. Although at present, combinations of individual single-target drugs represent the most clinically practiced therapeutic approaches, the modulation of multiple proteins by a single drug, in accordance with the polypharmacological strategy, has become more and more appealing. In the perspective of…

0301 basic medicineDrugNiacinamideIndolesPyridinesmedia_common.quotation_subjectPharmacologyBioinformaticsBiochemistryReceptor tyrosine kinase03 medical and health sciencesCrizotinibPiperidinesMultitargeted drugs anticancer agents polypharmacology tyrosine kinase receptors oncogene addiction tumor microenvironment FDA-approved drugsNeoplasmsDrug DiscoverymedicineSunitinibHumansAnilidesPyrrolesProtein Kinase Inhibitorsmedia_commonPharmacologyTumor microenvironmentbiologybusiness.industryPhenylurea CompoundsOrganic ChemistryImidazolesCancerReceptor Protein-Tyrosine KinasesSorafenibmedicine.diseaseOncogene AddictionSettore CHIM/08 - Chimica FarmaceuticaClinical trialPyridazines030104 developmental biologyMechanism of actionbiology.proteinImatinib MesylateQuinazolinesMolecular MedicinePyrazolesmedicine.symptombusinessTyrosine kinase
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Cabozantinib targets bone microenvironment modulating human osteoclast and osteoblast functions

2016

Cabozantinib, a c-MET and vascular endothelial growth factor receptor 2 inhibitor, demonstrated to prolong progression free survival and improve skeletal disease-related endpoints in castration-resistant prostate cancer and in metastatic renal carcinoma. Our purpose is to investigate the direct effect of cabozantinib on bone microenvironment using a total human model of primary osteoclasts and osteoblasts.Osteoclasts were differentiated from monocytes isolated from healthy donors; osteoblasts were derived from human mesenchymal stem cells obtained from bone fragments of orthopedic surgery patients. Osteoclast activity was evaluated by tartrate resistant acid phosphatase (TRAP) staining and …

0301 basic medicinePyridines -- pharmacologyPyridinesPyridineImmunoenzyme TechniqueOsteoclastsApoptosisRANK Ligand -- genetics -- metabolismImmunoenzyme Techniqueschemistry.chemical_compoundBone Resorption -- drug therapy -- metabolism -- pathology0302 clinical medicineOsteogenesisCathepsin KMedicineAnilidesAnilides -- pharmacologyOsteoprotegerin -- genetics -- metabolismOsteoclasts -- cytology -- drug effects -- physiologyHuman primary cellCells CulturedTartrate-resistant acid phosphataseReceptor Activator of Nuclear Factor-kappa B -- genetics -- metabolismbiologyProto-Oncogene Proteins c-met -- genetics -- metabolismReceptor Activator of Nuclear Factor-kappa BReverse Transcriptase Polymerase Chain ReactionOsteoblastOsteogenesiOsteoblastCell DifferentiationSciences bio-médicales et agricolesProto-Oncogene Proteins c-metOsteoblasts -- cytology -- drug effects -- physiologymedicine.anatomical_structureCell Differentiation -- drug effectsOncologyRANKL030220 oncology & carcinogenesishuman primary cellsOsteoclastosteoprotegerin (OPG)bone microenvironmentHumanResearch Papermusculoskeletal diseasesmedicine.medical_specialtyCabozantinibBlotting WesternOsteogenesis -- drug effects -- physiologyReal-Time Polymerase Chain ReactionBone resorption03 medical and health sciencesOsteoprotegerinOsteoclastcabozantinibInternal medicineHumansRNA MessengerBone ResorptionCell ProliferationOsteoblastsbusiness.industryRANK LigandAnilideOsteoprotegerinApoptosiBone microenvironment; Cabozantinib; Human primary cells; Osteoprotegerin (OPG); Receptor activator of nuclear factor-kb ligand (RANKL); Anilides; Apoptosis; Blotting Western; Bone Resorption; Cell Differentiation; Cell Proliferation; Cells Cultured; Humans; Immunoenzyme Techniques; Osteoblasts; Osteoclasts; Osteogenesis; Osteoprotegerin; Proto-Oncogene Proteins c-met; Pyridines; RANK Ligand; RNA Messenger; Real-Time Polymerase Chain Reaction; Receptor Activator of Nuclear Factor-kappa B; Reverse Transcriptase Polymerase Chain Reaction; Oncology030104 developmental biologyEndocrinologychemistrybiology.proteinbusinessRNA Messenger -- geneticsreceptor activator of nuclear factor-kb ligand (RANKL)
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Lorcainide. I. Saturable presystemic elimination.

1979

AdultMaleBenzeneacetamidesAdministration OralPharmacologyHepatic VeinsIn Vitro TechniquesPulmonary ArteryLorcainidePiperidinesMedicineHumansPharmacology (medical)Aorta AbdominalAortaAgedPharmacologybusiness.industryArrhythmias CardiacBlood ProteinsMiddle AgedBloodInjections IntravenousAcetanilidesFemalebusinessAnti-Arrhythmia Agentsmedicine.drugProtein BindingClinical pharmacology and therapeutics
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Lorcainide; II. Plasma concentration-effect relationship

1979

AdultMalePharmacologyChromatographybusiness.industryBenzeneacetamidesAdministration OralArrhythmias CardiacIn Vitro TechniquesMiddle AgedLorcainideElectrocardiographyPiperidinesInjections IntravenousPlasma concentrationmedicineHumansAcetanilidesFemaleInfusions ParenteralPharmacology (medical)businessAnti-Arrhythmia AgentsAgedmedicine.drugClinical Pharmacology & Therapeutics
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Cemiplimab in locally advanced basal cell carcinoma after hedgehog inhibitor therapy: an open-label, multi-centre, single-arm, phase 2 trial.

2021

Summary Background Before February, 2021, there was no standard treatment regimen for locally advanced basal cell carcinoma after first-line hedgehog inhibitor (HHI) therapy. Cemiplimab, a PD-1 antibody, is approved for treatment of advanced cutaneous squamous cell carcinoma and has shown clinical activity as monotherapy in first-line non-small-cell lung cancer. Here, we present the primary analysis data of cemiplimab in patients with locally advanced basal cell carcinoma after HHI therapy. Methods We did an open-label, multicentre, single-arm, phase 2 trial across 38 outpatient clinics, primarily at academic medical centres, in Canada, Europe, and the USA. Eligible patients (aged ≥18 years…

AdultMalemedicine.medical_specialtySkin NeoplasmsPyridinesProgrammed Cell Death 1 ReceptorVismodegibAntibodies Monoclonal Humanized030207 dermatology & venereal diseases03 medical and health sciences0302 clinical medicineInternal medicineAntineoplastic Combined Chemotherapy ProtocolsmedicineCarcinomaClinical endpointOutpatient clinicHumansBasal cell carcinomaAnilidesHedgehog ProteinsLung cancerImmune Checkpoint InhibitorsAgedbusiness.industryStandard treatmentMiddle Agedmedicine.diseaseRegimenOncologyCarcinoma Basal CellDrug Resistance Neoplasm030220 oncology & carcinogenesisFemaleNeoplasm Recurrence LocalSettore MED/35 - MALATTIE CUTANEE E VENEREEbusinessmedicine.drugThe Lancet. Oncology
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Involvement of cholinergic nicotinic receptors in the menthol-induced gastric relaxation.

2014

We have previously demonstrated that menthol reduces murine gastric tone in part through a neural mechanism, involving adrenergic pathways and reduction of ongoing release of acetylcholine from enteric nerves. In the present study we aimed to verify whether the gastric relaxation to menthol may be triggered by interaction with neural receptors or ionic channels proteins, such as transient receptor potential (TRP)-melastatin8 (TRPM8), TRP-ankyrin 1 (TRPA1), 5-hydroxytriptamine 3 (5-HT3) receptor or cholinergic nicotinic receptors. Spontaneous mechanical activity was detected in vitro as changes in intraluminal pressure from isolated mouse stomach. Menthol (0.3-30 mM) induced gastric relaxati…

AgonistMalemedicine.medical_specialtySerotoninmedicine.drug_classDimethylphenylpiperaziniumMuscle RelaxationTRPM Cation ChannelsPharmacologyReceptors NicotinicSettore BIO/09 - Fisiologiachemistry.chemical_compoundMiceGanglion type nicotinic receptorTransient Receptor Potential ChannelsIsothiocyanatesInternal medicinemedicineTRPM8AnimalsSerotonin 5-HT3 Receptor AntagonistsRNA MessengerTRPA1 Cation ChannelPharmacologyStomachmenthol gastric relaxation TRPM8 TRPA1 nicotinic receptorsReceptor antagonistOndansetronMice Inbred C57BLMentholEndocrinologyNicotinic agonistchemistryPurinesHexamethoniumAcetanilidesAlpha-4 beta-2 nicotinic receptorGastrointestinal Motilitymedicine.drugEuropean journal of pharmacology
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Apoptosis induced in HepG2 cells by the synthetic cannabinoid WIN: involvement of the transcription factor PPARgamma.

2008

It has recently been shown that cannabinoids induce growth inhibition and apoptosis in different tumour cell lines. In the current study, the effects of WIN 55,212-2 (WIN), a synthetic and potent cannabinoid receptor agonist, are investigated in hepatoma HepG2 cells and a possible signal transduction pathway is proposed. In these cells, WIN induces a clear apoptotic effect which was accompanied by up-regulation of the death-signalling factors Bax, Bcl-X(S), t-Bid and down-regulation of the survival factors survivin, phospho-AKT, Hsp72 and Bcl-2. Moreover, WIN-induced apoptosis is associated with JNK/p38 MAPK pathway activation and mitochondrial depolarisation demonstrated by a cytofluorimet…

Cannabinoid receptorCarcinoma HepatocellularCell SurvivalPyridinesmedicine.medical_treatmentp38 mitogen-activated protein kinasesMorpholinesApoptosisBiologyNaphthalenesBiochemistryReceptor Cannabinoid CB2Membrane Microdomainscannabinoids PPARgamma factor apoptosis cancer cellsSettore BIO/10 - BiochimicaCell Line TumorSurvivinmedicineHumansAnilidesViability assayCannabinoidsLiver NeoplasmsGeneral MedicineCell biologyBenzoxazinesPPAR gammaApoptosisCancer cellBenzamidesCannabinoidSignal transductionApoptosis Regulatory ProteinsProtein KinasesSignal TransductionBiochimie
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Genetic instability in calamondin (Citrus madurensis Lour.) plants derived from somatic embryogenesis induced by diphenylurea derivative

2007

Somatic embryos were regenerated in vitro from calamondin style-stigma explants cultured in the presence of N (6)-benzylaminopurine (BAP) cytokinin and three synthetic phenylurea derivatives, N-(2-chloro-4-pyridyl)-N-phenylurea (4-CPPU), N-phenyl-N'-benzothiazol-6-ylurea (PBU) and N,N'-bis-(2,3-methilendioxyphenyl)urea (2,3-MDPU). The phenylurea derivative compounds tested at micromolar level (12 muM) were able to induce a percentage of responsive explants significantly higher from that obtained with BAP and hormone-free (HF) conditions. In order to verify the genetic stability of the regenerants, 27 plants coming from different embryogenic events were randomly selected from each different …

CitrusSomatic embryogenesisMutantPlant ScienceBiologyGenetic polymorphismsSomaclonal variationTissue Culture Techniqueschemistry.chemical_compoundGene Expression Regulation PlantBotanygenetic polymorphismmolecular markerPolymorphism GeneticMolecular markersGeneral MedicineSomaclonal variabilitybiology.organism_classificationMolecular biologyIn vitroCulture MediaRutaceaechemistryMutagenesisCytokininmutationAgronomy and Crop ScienceCarbanilidesDNAMutationsExplant culturePlant regeneration
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Ombitasvir, paritaprevir, and ritonavir, with or without dasabuvir, plus ribavirin for patients with hepatitis C virus genotype 1 or 4 infection with…

2017

Summary Background We ran a compassionate use nationwide programme (ABACUS) to provide access to ombitasvir, paritaprevir, and ritonavir, with dasabuvir, plus ribavirin for hepatitis C virus (HCV) genotype 1 infection and ombitasvir, paritaprevir, and ritonavir, plus ribavirin for HCV genotype 4 infection in patients with cirrhosis at high risk of decompensation while approval of these regimens was pending in Italy. Methods In this prospective observational study, we collected data from a compassionate use nationwide programme from March 17, 2014, to May 28, 2015. Patients with HCV genotype 1 infection and cirrhosis at high risk of decompensation were given coformulated ombitasvir (25 mg), …

CyclopropanesCompassionate Use TrialsLiver CirrhosisMalechemistry.chemical_compound0302 clinical medicine2-NaphthylamineHCV direct-acting antiviral mixed cryoglobulinemia RBVAnilides030212 general & internal medicineLongitudinal StudiesProspective StudiesChronicAdult; Aged; Anilides; Antiviral Agents; Carbamates; Compassionate Use Trials; Drug Therapy Combination; Female; Genotype; Hepatitis C Chronic; Humans; Liver Cirrhosis; Longitudinal Studies; Macrocyclic Compounds; Male; Middle Aged; Prospective Studies; Ribavirin; Ritonavir; Sulfonamides; Treatment Outcome; UracilSettore MED/12 - GastroenterologiaSulfonamidesDasabuvirHCV DAAGastroenterologyvirus diseasesValineMiddle AgedSettore MED/07 - Microbiologia e Microbiologia ClinicaHepatitis CTreatment OutcomeGastroenterology; HepatologyCombinationDrug Therapy Combination030211 gastroenterology & hepatologyFemalemedicine.drugAdultmedicine.medical_specialtyMacrocyclic CompoundsProlineGenotypeLactams MacrocyclicAdult; Aged; Anilides; Antiviral Agents; Carbamates; Compassionate Use Trials; Drug Therapy Combination; Female; Genotype; Hepatitis C Chronic; Humans; Liver Cirrhosis; Longitudinal Studies; Macrocyclic Compounds; Male; Middle Aged; Prospective Studies; Ribavirin; Ritonavir; Sulfonamides; Treatment Outcome; Uracil; Hepatology; GastroenterologyHepatitis C virus genotype 1 Hepatitis C virus genotype 4 decompensated liver cirrhosis antiviral therapy dasabuvir ombitasvir paritaprevirHepatology; GastroenterologyAntiviral Agents03 medical and health sciencesDrug TherapyInternal medicineRibavirinmedicineHumansDecompensationAdverse effectUracilAgedRitonavirHepatologybusiness.industryRibavirinHepatitis C ChronicVirologyOmbitasvirClinical trialchemistryParitaprevirRitonavirCarbamatesbusiness
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Safety and efficacy of ombitasvir/paritaprevir/ritonavir/dasabuvir plus ribavirin in patients over 65 years with HCV genotype 1 cirrhosis

2018

Purpose: To analyse safety and efficacy of treatment based on ombitasvir/paritaprevir/ritonavir/dasabuvir plus ribavirin in the sub-group of GT1 patients older than 65 years. Methods: We collected data extracted from the ABACUS compassionate-use nationwide Italian programme, in patients with cirrhosis due to hepatitis C virus (HCV) Genotype-1 (GT1) or 4 and at high risk of decompensation. GT1-HCV-infected patients received once-daily ombitasvir/paritaprevir, with the pharmacokinetic enhancer ritonavir (25/150/100 mg) and twice-daily dasabuvir (250 mg) plus Ribavirin (RBV) (OBV/PTV/r + DSV + RBV) for 12 (GT1b) or 24 (GT1a) weeks. Endpoints were to evaluate safety and efficacy, the latter def…

CyclopropanesLiver CirrhosisMaleCirrhosis;Dasabuvir;Elderly;Ombitasvir;ParitaprevirCirrhosis; Dasabuvir; Elderly; Ombitasvir; Paritaprevir; Aged; Aged; 80 and over; Anilides; Antiviral Agents; Biomarkers; Carbamates; Female; Hepacivirus; Hepatitis C; Chronic; Humans; Liver Cirrhosis; Macrocyclic Compounds; Male; Ribavirin; Ritonavir; Sulfonamides; Treatment Outcome; Uracil; Drug Therapy; Combination; GenotypeParitaprevirCirrhosis Dasabuvir Elderly Ombitasvir Paritaprevir Microbiology (medical) Infectious DiseasesCirrhosis; Dasabuvir; Elderly; Ombitasvir; Paritaprevir; Aged; Aged 80 and over; Anilides; Antiviral Agents; Biomarkers; Carbamates; Female; Hepacivirus; Hepatitis C Chronic; Humans; Liver Cirrhosis; Macrocyclic Compounds; Male; Ribavirin; Ritonavir; Sulfonamides; Treatment Outcome; Uracil; Drug Therapy Combination; Genotype; Microbiology (medical); Infectious DiseasesHepacivirusGastroenterologychemistry.chemical_compound0302 clinical medicineElderly2-Naphthylamine80 and overMedicineAnilides030212 general & internal medicineChronicAged 80 and overSulfonamidesDasabuvirValineGeneral MedicineHepatitis CHepatitis CTreatment OutcomeInfectious DiseasesCirrhosisCombination030211 gastroenterology & hepatologyDrug Therapy CombinationFemaleDasabuvirMacrocyclic CompoundCirrhosis; Dasabuvir; Elderly; Ombitasvir; Paritaprevir; Microbiology (medical); Infectious Diseasesmedicine.drugHumanMicrobiology (medical)medicine.medical_specialtyMacrocyclic CompoundsProlineGenotypeLactams MacrocyclicSettore MED/12 - GASTROENTEROLOGIALiver CirrhosiSulfonamideAntiviral Agents03 medical and health sciencesDrug TherapyInternal medicineRibavirinHumansDecompensationUracilAgedHepatitisAntiviral AgentCirrhosiHepaciviruRitonavirbusiness.industryRibavirinSettore MED/09 - MEDICINA INTERNAAnilideBiomarkerHepatitis C Chronicmedicine.diseaseCirrhosis; Dasabuvir; Elderly; Ombitasvir; Paritaprevir; Aged; Aged 80 and over; Anilides; Antiviral Agents; Biomarkers; Carbamates; Female; Hepacivirus; Hepatitis C Chronic; Humans; Liver Cirrhosis; Macrocyclic Compounds; Male; Ribavirin; Ritonavir; Sulfonamides; Treatment Outcome; Uracil; Drug Therapy Combination; GenotypeOmbitasvirOmbitasvirchemistryParitaprevirCarbamateRitonavirCarbamatesbusinessBiomarkers
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