Search results for "Sulfonamide"

showing 10 items of 258 documents

Curcumin at Low Doses Potentiates and at High Doses Inhibits ABT-737-Induced Platelet Apoptosis

2021

Curcumin is a natural bioactive component derived from the turmeric plant Curcuma longa, which exhibits a range of beneficial activities on human cells. Previously, an inhibitory effect of curcumin on platelets was demonstrated. However, it is unknown whether this inhibitory effect is due to platelet apoptosis or procoagulant platelet formation. In this study, curcumin did not activate caspase 3-dependent apoptosis of human platelets, but rather induced the formation of procoagulant platelets. Interestingly, curcumin at low concentration (5 µM) potentiated, and at high concentration (50 µM) inhibited ABT-737-induced platelet apoptosis, which was accompanied by inhibition of ABT-737-mediated…

0301 basic medicinePharmacologyPiperazinesNitrophenolschemistry.chemical_compound0302 clinical medicinePlateletBiology (General)SpectroscopyCaspaseSulfonamidesbiologyKinaseapoptosisGeneral MedicinethrombinDrug Resistance Multipleprocoagulant activityComputer Science ApplicationsChemistry030220 oncology & carcinogenesisplateletsmedicine.drugBlood PlateletsAdenosine monophosphateautophagyCurcuminQH301-705.5ArticleCatalysisInorganic Chemistry03 medical and health sciencesCurcumaThrombinmedicineHumansATP Binding Cassette Transporter Subfamily B Member 1Physical and Theoretical ChemistryQD1-999Molecular BiologyProtein kinase BPlant ExtractsBiphenyl CompoundsOrganic ChemistryAdenosine Monophosphate030104 developmental biologychemistryApoptosisbiology.proteinCurcuminProto-Oncogene Proteins c-aktPlatelet Aggregation InhibitorsInternational Journal of Molecular Sciences
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Daclatasvir-based regimens in HCV cirrhosis: experience from the Italian early access program

2019

AbstractWe reported the efficacy and safety data for daclatasvir (DCV)-based all-oral antiviral therapy in patients treated in the Italian compassionate-use program. 275 patients were included (202 male-73.5%, mean age: 57.4 years, 62 HIV-coinfected, 94 with recurrence of hepatitis C post-OLT). Forty-nine patients (17.8%) had Child-Pugh B, Genotype(G) distribution was: G1a:72 patients (26.2%), G1b:137 (49.8%); G3:40 (14.5%) and G4:26 (9.5%). Patients received DCV with sofosbuvir(SOF) (n = 221, 129 with ribavirin(RBV) or with simeprevir (SMV) or asunaprevir (ASU) (n = 54, 19 with RBV) for up to 24 weeks. Logistic regression was used to identify baseline characteristics associated with sustai…

0301 basic medicineSimeprevirLiver CirrhosisMalePyrrolidinesSofosbuvirSustained Virologic Responselcsh:MedicineSettore MED/05Gastroenterologychemistry.chemical_compound0302 clinical medicineLiver Function TestsINFECTIONMedicinePLUS SOFOSBUVIRlcsh:ScienceSulfonamidesMultidisciplinaryImidazolesValineHepatitis CMiddle AgedTreatment OutcomeItalySAFETYHCVSUSTAINED VIROLOGICAL RESPONSEDrug Therapy CombinationFemaleRIBAVIRINSettore BIO/19 - MICROBIOLOGIA GENERALECHRONIC HEPATITIS-Cmedicine.drugAdultmedicine.medical_specialtyDaclatasvirDrug-Related Side Effects and Adverse ReactionsAntiviral AgentsArticle03 medical and health sciencesInternal medicineHumansAgedADVANCED LIVER-DISEASEbusiness.industryRibavirinVIRUS GENOTYPE 3lcsh:RHepatitis C ChronicHCV HIV Daclatasvirmedicine.diseaseIsoquinolinesEFFICACYRegimen030104 developmental biologychemistryAsunaprevirlcsh:QLiver functionCarbamatesSofosbuvirbusiness030217 neurology & neurosurgeryScientific Reports
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Loss of MCL1 function sensitizes the MDA-MB-231 breast cancer cells to rh-TRAIL by increasing DR4 levels.

2019

Triple-negative breast cancer (TNBC) is a form of BC characterized by high aggressiveness and therapy resistance probably determined by cancer stem cells. MCL1 is an antiapoptotic Bcl-2 family member that could limit the efficacy of anticancer agents as recombinant human tumor necrosis factor related apoptosis-inducing ligand (rh-TRAIL). Here, we investigated MCL1 expression in TNBC tissues and cells. We found MCL1 differentially expressed (upregulated or downregulated) in TNBC tissues. Furthermore, in comparison to the human mammary epithelial cells, we found that MDA-MB-231 cells show similar messenger RNA levels but higher MCL1 protein levels, whereas it resulted downregulated in MDA-MB-…

0301 basic medicinecancer stem cellIndolesPhysiologyCell SurvivalClinical BiochemistryCellPopulationApoptosisTNF-Related Apoptosis-Inducing Ligand03 medical and health sciences0302 clinical medicineCancer stem cellSettore BIO/10 - BiochimicaCell Line Tumormedicinerh-TRAILBiomarkers TumorGene silencingHumansViability assayGene SilencingeducationCell ShapeCell ProliferationMembrane Potential Mitochondrialeducation.field_of_studySulfonamidesChemistryCell growthCell CycleCell BiologyCell cycleRecombinant ProteinsGene Expression Regulation NeoplasticReceptors TNF-Related Apoptosis-Inducing Ligand030104 developmental biologymedicine.anatomical_structureMCL1ApoptosisDR4 receptor030220 oncology & carcinogenesisCancer researchtriple-negative breast cancerMyeloid Cell Leukemia Sequence 1 ProteinJournal of cellular physiology
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Antiviral Properties of Chemical Inhibitors of Cellular Anti-Apoptotic Bcl-2 Proteins

2017

Viral diseases remain serious threats to public health because of the shortage of effective means of control. To combat the surge of viral diseases, new treatments are urgently needed. Here we show that small-molecules, which inhibit cellular anti-apoptotic Bcl-2 proteins (Bcl-2i), induced the premature death of cells infected with different RNA or DNA viruses, whereas, at the same concentrations, no toxicity was observed in mock-infected cells. Moreover, these compounds limited viral replication and spread. Surprisingly, Bcl-2i also induced the premature apoptosis of cells transfected with viral RNA or plasmid DNA but not of mock-transfected cells. These results suggest that Bcl-2i sensiti…

0301 basic medicinevirusesFAMILY INHIBITORSlcsh:QR1-502Virus Replicationlcsh:Microbiologychemistry.chemical_compoundTranscription (biology)SALIPHENYLHALAMIDEhost responseTRANSCRIPTIONprogrammed cell deathinnate immunity1183 Plant biology microbiology virologySulfonamidesAniline CompoundsapoptosisTransfection3. Good healthInfectious DiseasesProto-Oncogene Proteins c-bcl-2X-L INHIBITORVirus DiseasesvirustauditVirusesRNA ViralBiologyTransfectionta3111Antiviral AgentsArticleCell LineMicrobiology in the medical areaantiviral agent03 medical and health sciencesohjelmoitunut solukuolemaVirologyMikrobiologi inom det medicinska områdetHumansMetabolomicsBenzothiazolesInnate immune systemapoptosis; antiviral agent; innate immunity; host responseZIKA VIRUS-INFECTIONCHRONIC LYMPHOCYTIC-LEUKEMIAPOTENTta1183INFLUENZA-Ata1182RNAIsoquinolinesVirology030104 developmental biologyViral replicationchemistryCell cultureApoptosisCELLSREPLICATIONDNA Viral3111 BiomedicineDNA
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CCDC 1998478: Experimental Crystal Structure Determination

2021

Related Article: Lars J. Wesenberg, Erika Diehl, Till J. B. Zähringer, Carolin Dörr, Dieter Schollmeyer, Akihiro Shimizu, Jun‐ichi Yoshida, Ute A. Hellmich, Siegfried R. Waldvogel|2020|Chem.-Eur.J.|26|17574|doi:10.1002/chem.202003852

2-methoxy-N-(6-methoxy-22-dimethyl-3-oxo-34-dihydro-2H-14-benzoxazin-7-yl)-5-methylbenzene-1-sulfonamideSpace GroupCrystallographyCrystal SystemCrystal StructureCell ParametersExperimental 3D Coordinates
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CCDC 1433602: Experimental Crystal Structure Determination

2017

Related Article: H. Purandara, S. Foro, B. Thimme Gowda|2017|Acta Crystallogr.,Sect.E:Cryst.Commun.|73|1683|doi:10.1107/S2056989017014669

4-methyl-N-{2-[2-(4-nitrobenzylidene)hydrazinyl]-2-oxoethyl}benzenesulfonamide NN-dimethylformamide solvateSpace GroupCrystallographyCrystal SystemCrystal StructureCell ParametersExperimental 3D Coordinates
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CCDC 1998476: Experimental Crystal Structure Determination

2021

Related Article: Lars J. Wesenberg, Erika Diehl, Till J. B. Zähringer, Carolin Dörr, Dieter Schollmeyer, Akihiro Shimizu, Jun‐ichi Yoshida, Ute A. Hellmich, Siegfried R. Waldvogel|2020|Chem.-Eur.J.|26|17574|doi:10.1002/chem.202003852

5-bromo-2-methoxy-N-(6-methoxy-22-dimethyl-3-oxo-34-dihydro-2H-14-benzoxazin-7-yl)benzene-1-sulfonamideSpace GroupCrystallographyCrystal SystemCrystal StructureCell ParametersExperimental 3D Coordinates
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Efficacy and safety of glecaprevir/pibrentasvir in renally impaired patients with chronic HCV infection

2019

Background and aims Chronic hepatitis C virus (HCV) infection increases the risk of incident chronic kidney disease (CKD) and progression to end-stage renal disease (ESRD). Previously available direct-acting antiviral regimens are not approved for patients with advanced CKD across all HCV genotypes. Methods EXPEDITION-5 is a phase 3 study to evaluate efficacy and safety of the fixed-dose combination of glecaprevir and pibrentasvir (G/P) for chronic HCV infection (genotype 1 through 6) in adults without cirrhosis or with compensated cirrhosis and with stage 3b, 4 or 5 CKD. Patients received approved duration of G/P according to HCV genotype, cirrhosis status and prior HCV treatment experienc…

AdultCyclopropaneshepatitis C virusmedicine.medical_specialtyAminoisobutyric AcidsPyrrolidinesCirrhosisProlineLactams Macrocyclicmedicine.medical_treatmentAntiviral Agents03 medical and health sciences0302 clinical medicineLeucineQuinoxalinesInternal medicineGenotypeHumansMedicineAdverse effectDialysisSulfonamidesdirect-acting antiviralpangenotypicHepatologychronic kidney disease; cirrhosis; direct-acting antiviral; hepatitis C virus; pangenotypicbusiness.industrycirrhosisGlecaprevirHepatitis C Chronicmedicine.diseasePibrentasvirDrug Combinations030220 oncology & carcinogenesisBronchitisBenzimidazoles030211 gastroenterology & hepatologybusinesschronic kidney diseaseKidney disease
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Raltegravir Pharmacokinetics in Patients on Asunaprevir-Daclatasvir.

2015

ABSTRACT Raltegravir pharmacokinetics was studied in 20 patients included in the ANRS HC30 QUADRIH Study before and after addition of anti-hepatitis C virus (anti-HCV) quadritherapy, including pegylated-interferon–ribavirin and asunaprevir plus daclatasvir. Raltegravir pharmacokinetic parameters remained unchanged whether administered on or off anti-HCV therapy. In addition, concentrations of raltegravir, asunaprevir, and daclatasvir were not affected by liver cirrhosis. These data suggest that in human immunodeficiency virus (HIV)-HCV-coinfected patients, whether cirrhotic or not, asunaprevir and daclatasvir could be administered safely with raltegravir.

AdultLiver CirrhosisMaleDaclatasvirPyrrolidinesAlpha interferonHIV InfectionsHepacivirusPharmacologyAntiviral AgentsRaltegravir PotassiumPolyethylene Glycolschemistry.chemical_compoundPharmacokineticsRaltegravir PotassiumRibavirinMedicineHumansPharmacology (medical)PharmacologySulfonamidesbusiness.industryCoinfectionRibavirinImidazolesvirus diseasesInterferon-alphaValineHepatitis CHepatitis C ChronicMiddle AgedRaltegravirmedicine.diseaseIsoquinolinesdigestive system diseasesRecombinant ProteinsInfectious DiseaseschemistryLiverHIV-1AsunaprevirDrug Therapy CombinationFemaleCarbamatesbusinessmedicine.drugAntimicrobial agents and chemotherapy
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Rosuvastatin Prevents Conduit Artery Endothelial Dysfunction Induced by Ischemia and Reperfusion by a Cyclooxygenase-2–Dependent Mechanism

2010

ObjectivesThe purpose of this study was to determine whether single-dose rosuvastatin (40 mg) protects against ischemia and reperfusion (IR)–induced endothelial dysfunction in humans and whether this effect is cyclooxygenase (COX)-2 dependent.BackgroundAnimal studies have demonstrated that rosuvastatin can limit damage and improve recovery after IR.MethodsIn a double-blind, parallel design, 20 volunteers were randomized to a single dose of oral rosuvastatin (40 mg) or placebo. Twenty-four hours later, endothelium-dependent, flow-mediated dilation (FMD) of the radial artery was measured before and after IR (15 min of upper arm ischemia followed by 15 min of reperfusion). In a separate protoc…

AdultMaleEndotheliumendotheliumAdolescentPremedicationIschemiaMyocardial Reperfusion InjuryPharmacologyPlaceboYoung AdultDouble-Blind Methodmedicineischemia reperfusionHumansRosuvastatinEndothelial dysfunctionRosuvastatin CalciumSulfonamidesCyclooxygenase 2 Inhibitorsbusiness.industryModels Cardiovascularnutritional and metabolic diseases3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitormedicine.diseaseFluorobenzenesVasodilationRosuvastatin Calciummedicine.anatomical_structurePyrimidinesCelecoxibCyclooxygenase 2AnesthesiaIschemic Preconditioning MyocardialRadial ArteryCelecoxibIschemic preconditioningPyrazolesFemaleEndothelium VascularHydroxymethylglutaryl-CoA Reductase InhibitorsbusinessCardiology and Cardiovascular Medicinerosuvastatinmedicine.drugJournal of the American College of Cardiology
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