Search results for "antineoplastic agent"

showing 10 items of 1538 documents

Reactivity of antitumor coinage metal-based N-heterocyclic carbene complexes with cysteine and selenocysteine protein sites

2021

Abstract The reaction of the antitumor M(I)-bis-N-heterocyclic carbene (M(I)-NHC) complexes, M = Cu, Ag, and Au, with their potential protein binding sites, i.e. cysteine and selenocysteine, was investigated by means of density functional theory approaches. Capped cysteine and selenocysteine were employed to better model the corresponding residues environment within peptide structures. By assuming the neutral or deprotonated form of the side chains of these amino acids and by considering the possible assistance of an external proton donor such as an adjacent acidic residue or the acidic component of the surrounding buffer environment, we devised five possible routes leading to the binding o…

SilverAnticancer; Copper(I) complexes; DFT calculations; Gold(I) complexes; N-heterocyclic carbenes; Silver(I) complexesStereochemistryCoinage metalsAntineoplastic AgentsProtonationLigandsDFT calculationsBiochemistrySilver(I) complexesInorganic Chemistrychemistry.chemical_compoundDeprotonationProtein structureCoordination ComplexesCysteineN-heterocyclic carbenesDensity Functional Theorychemistry.chemical_classificationMolecular StructureSelenocysteineCopper(I) complexesSelenocysteineAmino acidAnticancerGold(I) complexesModels ChemicalchemistryThermodynamicsGoldCarbeneCopperCysteineJournal of Inorganic Biochemistry
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Side effect management during immune checkpoint blockade using CTLA-4 and PD-1 antibodies for metastatic melanoma – an update

2020

CTLA-4 and PD-1 play a key role in tumor-induced downregulation of lymphocytic immune responses. Immune checkpoint inhibitors have been shown to alter the immune response to various cancer types. Anti-CTLA-4 and anti-PD-1 antibodies affect the interaction between tumor, antigen-presenting cells and T lymphocytes. Clinical studies of the anti-CTLA-4 antibody ipilimumab and the anti-PD-1 antibodies nivolumab and pembrolizumab have provided evidence of their positive effects on overall survival in melanoma patients. Combined treatment using ipilimumab and nivolumab has been shown to achieve five-year survival rates of 52 %. Such enhancement of the immune response is inevitably associated with …

Skin NeoplasmsDrug-Related Side Effects and Adverse ReactionsSide effectProgrammed Cell Death 1 ReceptorMedizinIpilimumabDermatologyPembrolizumabAntibodies Monoclonal Humanized030207 dermatology & venereal diseases03 medical and health sciencesAntineoplastic Agents Immunological0302 clinical medicineImmune systemmedicineHumansCTLA-4 AntigenImmune Checkpoint InhibitorsMelanomabusiness.industryMelanomamedicine.diseaseCombined Modality TherapyIpilimumabImmune checkpoint3. Good healthNivolumabCTLA-4ImmunologyImmunotherapyNivolumabbusinessmedicine.drug
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Dacarbazine-mediated upregulation of NKG2D ligands on tumor cells activates NK and CD8 T cells and restrains melanoma growth.

2013

International audience; Dacarbazine (DTIC) is a cytotoxic drug widely used for melanoma treatment. However, the putative contribution of anticancer immune responses in the efficacy of DTIC has not been evaluated. By testing how DTIC affects host immune responses to cancer in a mouse model of melanoma, we unexpectedly found that both natural killer (NK) and CD8(+) T cells were indispensable for DTIC therapeutic effect. Although DTIC did not directly affect immune cells, it triggered the upregulation of NKG2D ligands on tumor cells, leading to NK cell activation and IFNγ secretion in mice and humans. NK cell-derived IFNγ subsequently favored upregulation of major histocompatibility complex cl…

Skin NeoplasmsMelanoma ExperimentalCD8-Positive T-LymphocytesPharmacologyMESH: Antineoplastic Agents AlkylatingLigandsBiochemistryMiceInterleukin 210302 clinical medicineMESH: Up-RegulationMESH: LigandsCytotoxic T cell[ SDV.IMM ] Life Sciences [q-bio]/ImmunologyMESH: AnimalsMESH : Up-RegulationMESH : LigandsMESH : Melanoma ExperimentalMelanomaMESH : Mice NudeMESH : CD8-Positive T-LymphocytesMESH: CD8-Positive T-LymphocytesUp-Regulation3. Good healthDacarbazineKiller Cells NaturalMESH: Melanoma ExperimentalNK Cell Lectin-Like Receptor Subfamily K030220 oncology & carcinogenesisMESH: NK Cell Lectin-Like Receptor Subfamily K[SDV.IMM]Life Sciences [q-bio]/ImmunologyMESH : Killer Cells Naturalmedicine.drugMESH: Killer Cells NaturalMESH: Cell Line Tumor[SDV.IMM] Life Sciences [q-bio]/ImmunologyMESH: Interferon-gammaDacarbazineMESH : Antineoplastic Agents AlkylatingMice NudeMESH : Mice Inbred C57BLDermatologyBiologyMajor histocompatibility complexMESH: DacarbazineInterferon-gamma03 medical and health sciencesImmune systemDownregulation and upregulationMESH: Mice Inbred C57BLCell Line TumorMESH : MicemedicineMESH : NK Cell Lectin-Like Receptor Subfamily KMESH: Mice NudeAnimalsHumansMESH : DacarbazineAntineoplastic Agents AlkylatingMolecular BiologyMESH: MiceMESH : Interferon-gammaMESH: HumansMESH : Cell Line TumorMESH: Skin NeoplasmsMESH : Skin NeoplasmsMESH : HumansCell Biologymedicine.diseaseMESH : Disease Models AnimalMice Inbred C57BLDisease Models Animalbiology.proteinMESH : AnimalsMESH: Disease Models AnimalCD8030215 immunology
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UV Exposure Boosts Transcutaneous Immunization and Improves Tumor Immunity: Cytotoxic T-Cell Priming through the Skin

2010

Immunologic approaches to combat cancer aim at the induction of tumor-reactive immune responses to achieve long-term protection. In this context, we recently developed a transcutaneous immunization (TCI) method using the Toll-like receptor (TLR) 7 agonist imiquimod and a peptide epitope. Application onto intact skin induces potent cytotoxic T lymphocyte (CTL) responses and protection against transplanted tumors. The purpose of this study was to explore the effects of UV irradiation on imiquimod-based TCI. Here we show that skin exposure to low-dose UV light before TCI with imiquimod strongly boosts specific CTL responses leading to memory formation and enhanced tumor protection. Toward the …

Skin NeoplasmsUltraviolet RaysPriming (immunology)ImiquimodAntineoplastic AgentsDermatologyBiochemistryEpitopeMiceImmune systemImmune ToleranceCytotoxic T cellMedicineAnimalsReceptorMolecular BiologySkinImiquimodMembrane GlycoproteinsDose-Response Relationship Drugbusiness.industryDose-Response Relationship RadiationCell BiologyMice Mutant StrainsVaccinationMice Inbred C57BLCTL*Toll-Like Receptor 7Langerhans CellsImmunologyAminoquinolinesbusinessImmunologic Memorymedicine.drugT-Lymphocytes CytotoxicJournal of Investigative Dermatology
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Sunitinib in patients with advanced hepatocellular carcinoma after progression under sorafenib treatment.

2010

<i>Objective:</i> To evaluate the safety and efficacy of sunitinib in patients with advanced hepatocellular carcinoma (HCC) after progression under sorafenib treatment. <i>Methods:</i> Sunitinib was administered at 37.5 mg daily (4-weeks-on/2-weeks-off schedule) after progression under sorafenib treatment. Adverse events (AEs) were assessed using NCI-CTCAE v3.0, and tumor response was evaluated according to RECIST. Data were analyzed retrospectively. <i>Results:</i> Eleven patients with metastatic disease were treated. Seven patients (64%) presented with no liver cirrhosis, including 3 patients with a history of liver transplantation. The first radiologic…

SorafenibAdultMaleNiacinamideCancer Researchmedicine.medical_specialtyCirrhosisCarcinoma HepatocellularIndolesPyridinesmedicine.medical_treatmentAntineoplastic AgentsLiver transplantationGastroenterologySeverity of Illness IndexDrug Administration ScheduleInternal medicinemedicineSunitinibHumansPyrrolesTreatment FailureAgedRetrospective StudiesSunitinibbusiness.industryPhenylurea CompoundsBenzenesulfonatesLiver NeoplasmsGeneral MedicineMiddle AgedSorafenibmedicine.diseasedigestive system diseasesSurgeryRadiographyTreatment OutcomeOncologyTumor progressionDrug Resistance NeoplasmHepatocellular carcinomaDisease ProgressionFemaleLiver functionLiver cancerbusinessmedicine.drugOncology
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TRAIL-induced apoptosis of hepatocellular carcinoma cells is augmented by targeted therapies

2009

AIM: To analyze the effect of chemotherapeutic drugs and specific kinase inhibitors, in combination with the death receptor ligand tumor necrosis factor-related apoptosis inducing ligand (TRAIL), on overcoming TRAIL resistance in hepatocellular carcinoma (HCC) and to study the efficacy of agonistic TRAIL antibodies, as well as the commitment of antiapoptotic BCL-2 proteins, in TRAIL-induced apoptosis. METHODS: Surface expression of TRAIL receptors (TRAIL-R1-4) and expression levels of the antiapoptotic BCL-2 proteins MCL-1 and BCL-xL were analyzed by flow cytometry and Western blotting, respectively. Knock-down of MCL-1 and BCL-xL was performed by transfecting specific small interfering RNA…

SorafenibCarcinoma Hepatocellularbcl-X ProteinBcl-xLAntineoplastic AgentsApoptosisTNF-Related Apoptosis-Inducing Ligandchemistry.chemical_compoundCell Line TumormedicineAnimalsHumansLY294002Viability assayEnzyme InhibitorsPI3K/AKT/mTOR pathwaybiologyKinaseLiver NeoplasmsGastroenterologyGeneral Medicinedigestive system diseasesReceptors TNF-Related Apoptosis-Inducing LigandchemistryProto-Oncogene Proteins c-bcl-2ApoptosisDoxorubicinCancer researchbiology.proteinMyeloid Cell Leukemia Sequence 1 ProteinTumor necrosis factor alphaOriginal ArticleFluorouracilmedicine.drug
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A systems biology perspective on cholangiocellular carcinoma development: focus on MAPK-signaling and the extracellular environment.

2008

Background/Aims Multiple genes have been implicated in cholangiocellular carcinoma (CCC) development. However, the overall neoplastic risk is likely associated with a much lower number of critical physiological pathways. Methods To investigate this hypothesis, we extracted all published genetic associations for the development of CCC from PubMed (genetic association studies, but also studies associating genes and CCC in general, i.e. functional studies in cell lines, genetic studies in humans, knockout mice etc.) and integrated CCC microarray data. Results We demonstrated the MAPK pathway was consistently enriched in CCC. Comparing our data to genetic associations in HCC often successfully …

SorafenibMAPK/ERK pathwayNiacinamideMAP Kinase Signaling SystemPyridinesSystems biologyAntineoplastic AgentsOncogenomicsBiologyCholangiocarcinomaMiceDatabases GeneticmedicineAnimalsHumansGeneOligonucleotide Array Sequence AnalysisHepatologyMicroarray analysis techniquesKinasePhenylurea CompoundsSystems BiologyBenzenesulfonatesComputational BiologySorafenibBiological EvolutionBile Ducts IntrahepaticBile Duct NeoplasmsMultigene FamilyImmunologyKnockout mouseCancer researchExtracellular Spacemedicine.drugJournal of hepatology
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Curative therapies are superior to standard of care (transarterial chemoembolization) for intermediate stage hepatocellular carcinoma.

2017

Background and aims the Barcelona Clinic Liver Cancer intermediate stage (BCLC-B) of hepatocellular carcinoma (HCC) includes extremely heterogeneous patients in terms of tumor burden and liver function. Transarterial-chemoembolization (TACE) is the first-line treatment for these patients although it may be risky/useless for someone, while others could undergo curative treatments. This study assesses the treatment type performed in a large cohort of BCLC-B patients and its outcome. Methods retrospective analysis of 485 consecutive BCLC-B patients from the ITA.LI.CA database diagnosed with naive HCC after 1999. Patients were stratified by treatment. Results 29 patients (6%) were lost to follo…

SorafenibMaleNiacinamidemedicine.medical_specialtyStandard of careCarcinoma HepatocellularAntineoplastic AgentsGastroenterologyIntermediate stage03 medical and health sciences0302 clinical medicineHCC; BCLC-B; Intermediate stage; Treatment; HepatologyInternal medicinemedicineHumansChemoembolization TherapeuticHCCPropensity ScoreAgedNeoplasm StagingRetrospective Studiesintermediate stageHepatologytreatmentbusiness.industryPatient SelectionPhenylurea CompoundsLiver NeoplasmsSettore MED/09 - MEDICINA INTERNAStandard of CareHepatologyMiddle AgedSorafenibmedicine.diseaseSurvival AnalysisTreatment OutcomeItaly030220 oncology & carcinogenesisHepatocellular carcinomaPropensity score matchingMultivariate Analysis030211 gastroenterology & hepatologyFemaleLiver functionLiver cancerbusinessBCLC-Bmedicine.drug
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Sorafenib perpetuates cellular anti-cancer effector functions by modulating the cross talk between macrophages and natural killer cells.

2012

Alternatively polarized macrophages (Mϕ) shape the microenvironment of hepatocellular carcinoma (HCC) and temper anticancer immune responses. We investigated if sorafenib alters the HCC microenvironment by restoring classical macrophage polarization and triggering tumor-directed natural killer (NK) cell responses. In vivo experiments were conducted with sorafenib (25 mg/kg)-treated C57BL/6 wildtype as well as hepatitis B virus (HBV) and lymphotoxin transgenic mice with and without HCC. Monocyte-derived Mϕ or tumor-associated macrophages (TAM) isolated from HCC tissue were treated with sorafenib (0.07-5.0 μg/mL) and cocultured with autologous NK cells. Mϕ and NK cell activation was analyzed …

SorafenibNiacinamideCarcinoma Hepatocellularmedicine.medical_treatmentMacrophage polarizationDrug Evaluation PreclinicalAntineoplastic AgentsApoptosisBiologyMiceliver cancer; therapy; microenvironment; immunology; HCCmedicineAnimalsHumansneoplasmsHepatologyMacrophagesPhenylurea CompoundsLiver NeoplasmsDegranulationNF-kappa BInterleukinMacrophage ActivationSorafenibdigestive system diseasesKiller Cells NaturalMice Inbred C57BLCytokineLymphotoxinImmunologyCancer researchInterleukin 12CytokinesInterleukin 18medicine.drug
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Field-practice study of sorafenib therapy for hepatocellular carcinoma: a prospective multicenter study in Italy

2011

A multicenter randomized controlled trial established sorafenib as a standard of care for patients with advanced hepatocellular carcinoma (HCC). Because the study was prematurely interrupted due to survival benefits in the sorafenib arm, we conducted an observational study to adequately assess risks and benefits of this regimen in field practice. Starting in 2008, all clinically compensated patients with advanced HCC and those with an intermediate HCC who were unfit or failed to respond to ablative therapies were consecutively evaluated in six liver centers in Italy, for tolerability as well as radiologic and survival response to 800-mg/d sorafenib therapy. Treatment was down-dosed or inter…

SorafenibNiacinamideMalemedicine.medical_specialtyCarcinoma HepatocellularDrug-Related Side Effects and Adverse ReactionsPyridinesAntineoplastic AgentsEPATOCARCINOMAlaw.inventionRandomized controlled triallawDrug ToxicityInternal medicinemedicineHumansProspective StudiesHCCProspective cohort studySurvival analysisAgedHCC; sorafenibHepatologybusiness.industryPhenylurea CompoundsBenzenesulfonatesLiver NeoplasmsCarcinomaSettore MED/09 - MEDICINA INTERNAHepatocellularSorafenibMiddle Agedmedicine.diseaseSurvival Analysisdigestive system diseasesSurgeryHepatocellular carcinoma sorafenibRegimenTUMORI DEL FEGATOTolerabilityItalyHepatocellular carcinomaDisease ProgressionsorafenibFemaleLiver cancerbusinessmedicine.drug
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