Search results for "COMB"

showing 10 items of 7115 documents

Pyrrolo[3',2':6,7]cyclohepta[1,2-b]pyridines with potent photo-antiproliferative activity.

2017

Abstract Pyrrolo[3′,2′:6,7]cyclohepta[1,2-b]pyridines were synthesized as a new class of tricyclic system in which the pyridine ring is annelated to a cycloheptapyrrole scaffold, with the aim of obtaining new photosensitizing agents with improved antiproliferative activity and lower undesired toxic effects. A versatile synthetic pathway was approached, which allowed the isolation of derivatives of the title ring system with a good substitution pattern on the pyrrole moiety. Photobiological studies revealed that the majority of the new compounds showed a potent cytotoxic effect upon photoactivation with light of the proper wavelength, especially when decorated with a 2-ethoxycabonyl group an…

0301 basic medicineLightPyridines01 natural sciencesAntioxidantschemistry.chemical_compound7]cyclohepta[1NeoplasmsDrug DiscoveryTumor Cells CulturedMoietyPyrrolechemistry.chemical_classificationPhotosensitizing AgentsGeneral MedicinePhotosensitizing AgentPyrrolo[3′2′:67]cyclohepta[12-b]pyridine-9(1H)-oneReactive oxygen speciemedicine.symptomPhototoxicity2-b]pyridine-9(1H)-onesStereochemistryBlotting WesternPhoto-antiproliferative activityAntineoplastic AgentsRing (chemistry)Phototoxicity03 medical and health sciencesStructure-Activity RelationshipPyridinemedicineHumansPyrrolo[3′PyrrolesCell ProliferationPharmacologyPhotosensitizing agent010405 organic chemistry2′:6Drug Discovery3003 Pharmaceutical ScienceOrganic ChemistryPhoto-antiproliferative activity; Photosensitizing agents; Phototoxicity; Pyrrolo[3′2′:67]cyclohepta[12-b]pyridine-9(1H)-ones; Reactive oxygen species; Pharmacology; Drug Discovery3003 Pharmaceutical Science; Organic ChemistryCombinatorial chemistry0104 chemical sciences030104 developmental biologychemistryMechanism of actionPhoto-antiproliferative activity; Photosensitizing agents; Phototoxicity; Pyrrolo[3′; 2′:6; 7]cyclohepta[1; 2-b]pyridine-9(1H)-ones; Reactive oxygen species; Pharmacology; Drug Discovery3003 Pharmaceutical Science; Organic ChemistryDrug Screening Assays AntitumorReactive Oxygen SpeciesTricyclicEuropean journal of medicinal chemistry
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Potential Therapeutic Applications of MDA-9/Syntenin-NF-κB-RKIP Loop in Human Liver Carcinoma

2019

Background Overexpression of MDA-9/Syntenin occurs in multiple human cancer cell lines and is associated with higher grade of tumor classification, invasiveness and metastasis. In some cases, its role in cancer biology depends on relationships between MDA-9/Syntenin and NF-κB. Objective This study aims to analyze the presence of a regulation loop like that between MDA-9/Syntenin - NF-κB - RKIP in human liver carcinoma. Methods Transient transfection was performed with siRNA anti-MDA-9/Syntenin. Expression of different factors was evaluated by Real time-PCR and Western blotting, while NF-κB activation by TransAM assay. Invasion capacity was analyzed by Matrigel Invasion Assay and the effects…

0301 basic medicineMDA-9/Syntenin NF-κB RKIP drug targets HA22T/VGH Hep3B HepG2Carcinoma HepatocellularCurcuminSynteninsPhosphatidylethanolamine Binding ProteinBiochemistry03 medical and health scienceschemistry.chemical_compound0302 clinical medicineDownregulation and upregulationAntineoplastic Combined Chemotherapy ProtocolsHumansGene silencingNeoplasm InvasivenessViability assayMolecular BiologyCell growthMatrigel Invasion AssayLiver NeoplasmsNF-kappa BNF-κBHep G2 CellsGeneral MedicineNeoplasm ProteinsBlot030104 developmental biologychemistryDoxorubicinCell cultureSettore BIO/14 - FarmacologiaCancer researchMolecular MedicineSignal Transduction030215 immunologyCurrent Molecular Medicine
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Impact of NADPH oxidase functional polymorphisms in acute myeloid leukemia induction chemotherapy.

2016

Efficacy and toxicity of anthracycline treatment in acute myeloid leukemia (AML) is mediated by reactive oxygen species (ROS). NADPH oxidase is the major endogenous source of ROS and a key mediator of oxidative cardiac damage. The impact of NADPH oxidase polymorphisms (CYBA:rs4673, NCF4:rs1883112, RAC2:rs13058338) was evaluated in 225 adult de novo AML patients. Variant alleles of NCF4 and RAC2 were related to higher complete remission (P=0.035, P=0.016), and CYBA homozygous variant showed lower overall survival with recessive model (P=0.045). Anthracycline-induced cardiotoxicity was associated to NCF4 homozygous variant (P=0.012) and CYBA heterozygous genotype (P=0.027). Novel associations…

0301 basic medicineMaleAnthracyclinePharmacologyBiologyPolymorphism Single NucleotideNephrotoxicity03 medical and health sciences0302 clinical medicineAntineoplastic Combined Chemotherapy ProtocolsGeneticsHumansAgedRetrospective StudiesPharmacologychemistry.chemical_classificationReactive oxygen speciesCardiotoxicityNADPH oxidaseRemission InductionMyeloid leukemiaNADPH OxidasesInduction ChemotherapyMiddle Agedrac GTP-Binding ProteinsRac GTP-Binding ProteinsLeukemia Myeloid Acute030104 developmental biologychemistry030220 oncology & carcinogenesisToxicitybiology.proteinMolecular MedicineFemaleReactive Oxygen SpeciesThe pharmacogenomics journal
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Threshold Effects of Circulating Angiopoietin-Like 3 Levels on Plasma Lipoproteins.

2017

Abstract Context Angiopoietin-like 3 (ANGPTL3) deficiency in plasma due to loss-of-function gene mutations results in familial combined hypobetalipoproteinemia type 2 (FHBL2) in homozygotes. However, the lipid phenotype in heterozygotes is much milder and does not appear to relate directly to ANGPTL3 levels. Furthermore, the low-density lipoprotein (LDL) phenotype in carriers of ANGPTL3 mutations is unexplained. Objective To determine whether reduction below a critical threshold in plasma ANGPTL3 levels is a determinant of lipoprotein metabolism in FHBL2, and to determine whether proprotein convertase subtilisin kexin type 9 (PCSK9) is involved in determining low LDL levels in this conditio…

0301 basic medicineMaleApolipoprotein BEndocrinology Diabetes and MetabolismClinical BiochemistryBiochemistryLipoprotein particlePCSK9Cohort StudiesHypobetalipoproteinemiaschemistry.chemical_compoundEndocrinologyANGPTL3biologyChemistryMiddle AgedPedigreeLipoproteins LDLPhenotypeKexinlipids (amino acids peptides and proteins)FemaleANGPTL3; familial combined hypolipidemia; PCSK9Lipoproteins HDLAdultmedicine.medical_specialtyHeterozygoteBlotting Western03 medical and health sciencesInternal medicinemedicineHumansGenetic Predisposition to DiseaseClinical Research ArticlesAgedAngiopoietin-Like Protein 3Apolipoproteins BCholesterolPCSK9Biochemistry (medical)medicine.disease030104 developmental biologyEndocrinologyAngiopoietin-like ProteinsLDL receptorMultivariate AnalysisMutationbiology.proteinLinear Modelsfamilial combined hypobetalipoproteinemiaHypobetalipoproteinemiaAngiopoietinsLipoprotein
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Muscle and serum metabolomes are dysregulated in colon-26 tumor-bearing mice despite amelioration of cachexia with activin receptor type 2B ligand bl…

2019

Cancer-associated cachexia reduces survival, which has been attenuated by blocking the activin receptor type 2B (ACVR2B) ligands in mice. The purpose of this study was to unravel the underlying physiology and novel cachexia biomarkers by use of the colon-26 (C26) carcinoma model of cancer cachexia. Male BALB/c mice were subcutaneously inoculated with C26 cancer cells or vehicle control. Tumor-bearing mice were treated with vehicle (C26+PBS) or soluble ACVR2B either before (C26+sACVR/b) or before and after (C26+sACVR/c) tumor formation. Skeletal muscle and serum metabolomics analysis was conducted by gas chromatography-mass spectrometry. Cancer altered various biologically functional groups …

0301 basic medicineMaleCachexiaPhysiologyEndocrinology Diabetes and MetabolismActivin Receptors Type IIlihaksetMyostatinMice0302 clinical medicineAmino Acidsta315Activin Receptor Type-2BbiologyOrganophosphatesRecombinant Proteins3. Good healthmedicine.anatomical_structureribosome030220 oncology & carcinogenesismyostatinColonic NeoplasmsMetabolomesyöpätauditC26Metabolic Networks and Pathwaysmedicine.medical_specialtyPhenylalanineCachexia03 medical and health sciencesribosomitPhysiology (medical)Internal medicineCell Line TumormedicineAnimalsskeletal muscleMuscle SkeletalPI3K/AKT/mTOR pathwaybusiness.industrySkeletal muscleCancermedicine.diseaseta3122BlockadeImmunoglobulin Fc Fragments030104 developmental biologyEndocrinologyProtein Biosynthesisbiology.proteinaineenvaihduntatuotteetPyrimidine NucleotidesproteiinitbusinesslihassurkastumasairaudetACVR2BAmerican journal of physiology. Endocrinology and metabolism
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Treatment patterns for metastatic colorectal cancer in Spain

2020

Abstract Purpose The primary aim of this retrospective study was to describe the treatment patterns according to the type of treatment received by patients with metastatic colorectal cancer (mCRC) in Spain. Methods This was a retrospective, observational, multicenter study performed by 33 sites throughout Spain that included consecutive patients aged 18 years or older who had received or were receiving treatment for mCRC. Results At the time of inclusion, of the 873 evaluable patients, 507 (58%) had received two lines, 235 (27%) had received three lines, 106 (12%) had received four lines, and the remaining patients had received up to ten lines. The most frequent chemotherapy schemes were th…

0301 basic medicineMaleCancer ResearchColorectal cancermedicine.medical_treatmentmedicine.disease_causeTargeted therapy0302 clinical medicineFOLFOXAntineoplastic Combined Chemotherapy ProtocolsKRAS/BRAF mutation statusMolecular Targeted TherapyNeoplasm MetastasisCàncerTreatment patternsGeneral MedicineMiddle AgedTreatment OutcomeOncology030220 oncology & carcinogenesisFOLFIRIMetastaticFemaleKRASGuideline AdherenceColorectal NeoplasmsCàncer Pacientsmedicine.drugResearch ArticleProto-Oncogene Proteins B-rafmedicine.medical_specialtyProto-Oncogene Proteins p21(ras)03 medical and health sciencesInternal medicinemedicineHumansAgedRetrospective StudiesClinical practice guidelineChemotherapybusiness.industryRetrospective cohort studymedicine.diseaseColorectal cancerdigestive system diseases030104 developmental biologySpainMutationObservational studybusiness
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BRG1/SMARCA4 is essential for neuroblastoma cell viability through modulation of cell death and survival pathways.

2016

Neuroblastoma (NB) is a neoplasm of the sympathetic nervous system, and is the most common solid tumor of infancy. NBs are very heterogeneous, with a clinical course ranging from spontaneous regression to resistance to all current forms of treatment. High-risk patients need intense chemotherapy, and only 30-40% will be cured. Relapsed or metastatic tumors acquire multi-drug resistance, raising the need for alternative treatments. Owing to the diverse mechanisms that are responsible of NB chemoresistance, we aimed to target epigenetic factors that control multiple pathways to bypass therapy resistance. We found that the SWI/SNF-related, matrix-associated, actin-dependent regulator of chromat…

0301 basic medicineMaleCancer ResearchCombination therapyCell SurvivalBiologyMolecular oncologyTranscriptome03 medical and health sciencesNeuroblastomaPhosphatidylinositol 3-Kinases0302 clinical medicineGrowth factor receptorNeuroblastomaCell Line TumorGeneticsmedicineHumansMolecular BiologyProtein kinase BPI3K/AKT/mTOR pathwayCell ProliferationCell DeathDNA HelicasesNuclear ProteinsCell cyclemedicine.diseaseGene Expression Regulation Neoplastic030104 developmental biologyProto-Oncogene Proteins c-bcl-2030220 oncology & carcinogenesisImmunologyCancer researchFemaleTranscriptomeSignal TransductionTranscription FactorsOncogene
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Germinal Centers Determine the Prognostic Relevance of Tertiary Lymphoid Structures and Are Impaired by Corticosteroids in Lung Squamous Cell Carcino…

2018

Abstract In solid tumors, the presence of lymph node–like structures called tertiary lymphoid structures (TLS) is associated with improved patient survival. However, little is known about how TLS develop in cancer, how their function affects survival, and whether they are affected by cancer therapy. In this study, we used multispectral microscopy, quantitative pathology, and gene expression profiling to analyze TLS formation in human lung squamous cell carcinoma (LSCC) and in an experimental model of lung TLS induction. We identified a niche of CXCL13+ perivascular and CXCL12+LTB+ and PD-L1+ epithelial cells supporting TLS formation. We also characterized sequential stages of TLS maturation…

0301 basic medicineMaleCancer ResearchLung Neoplasmsmedicine.medical_treatmentApoptosis03 medical and health sciencesMiceLymphocytes Tumor-InfiltratingAdrenal Cortex HormonesCarcinoma Non-Small-Cell LungAntineoplastic Combined Chemotherapy ProtocolsCarcinomaTumor Cells CulturedTumor MicroenvironmentMedicineAnimalsHumansCXCL13Lung cancerSurvival rateAgedCell ProliferationChemotherapyTumor microenvironmentbusiness.industryGene Expression ProfilingCancerGerminal centerMiddle Agedmedicine.diseaseGerminal CenterPrognosisXenograft Model Antitumor Assays3. Good healthMice Inbred C57BLSurvival Rate030104 developmental biologyTertiary Lymphoid StructuresOncologyCancer researchCarcinoma Squamous CellFemalebusinessFollow-Up StudiesCancer research
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Phase II study of necitumumab plus modified FOLFOX6 as first-line treatment in patients with locally advanced or metastatic colorectal cancer

2016

Background:This single-arm phase II study investigated the EGFR monoclonal antibody necitumumab plus modified FOLFOX6 (mFOLFOX6) in first-line treatment of locally advanced or metastatic colorectal cancer (mCRC).Methods:Patients received 800-mg intravenous necitumumab (day 1; 2-week cycles), followed by oxaliplatin 85 mg m -2, folinic acid 400 mg m -2, and 5-fluorouracil (400 mg m -2 bolus then 2400 mg m -2 over 46 h). Radiographic evaluation was performed every 8 weeks until progression. Primary endpoint was objective response rate.Results:Forty-four patients were enrolled and treated. Objective response rate was 63.6% (95% confidence interval 47.8-77.6); complete response was observed in …

0301 basic medicineMaleCancer ResearchOrganoplatinum CompoundsLeucovorinPhases of clinical researchmedicine.disease_causeGastroenterology0302 clinical medicineadvanced colorectal cancerAntineoplastic Combined Chemotherapy ProtocolsClinical endpointNeoplasm MetastasisNecitumumabModified FOLFOX6Aged 80 and overnecitumumabAntibodies MonoclonalMiddle AgedOxaliplatinTreatment OutcomeOncologyFluorouracil030220 oncology & carcinogenesisFemaleKRASFluorouracilColorectal Neoplasmsmedicine.drugAdultmedicine.medical_specialtyEGFRNeutropeniamodified FOLFOX6Antibodies Monoclonal HumanizedDisease-Free SurvivalProto-Oncogene Proteins p21(ras)03 medical and health sciencesFolinic acidInternal medicinemedicineKRASHumansAdvanced colorectal cancerAgedbusiness.industrymedicine.diseaseSurvival AnalysisSurgeryOxaliplatinCancérologie030104 developmental biologyClinical StudybusinessNecitumumabBritish Journal of Cancer
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Predictive and prognostic value of magnesium serum level in FOLFIRI plus cetuximab or bevacizumab treated patients with stage IV colorectal cancer: r…

2020

Magnesium wasting is a frequent side effect of epidermal growth factor receptor (EGFR)-antibody treatment as magnesium-absorption mechanisms are dependent on EGFR signaling. EGFR-inhibition results in decreased renal reabsorption. There is evidence that hypomagnesemia during cetuximab treatment correlates with response. The prognostic role of hypomagnesemia during bevacizumab treatment has not been studied yet. Here, we evaluate the prognostic value of hypomagnesemia in patients with metastatic colorectal cancer treated with FOLFIRI plus cetuximab or bevacizumab as first-line therapy. A total of 391 of 752 patients of the firstline irinotecan study population had magnesium levels measured a…

0301 basic medicineMaleCancer Researchmedicine.medical_specialtyRenal Tubular Transport Inborn ErrorsBevacizumabSide effectColorectal cancerHypercalciuriaLeucovorinCetuximabIrinotecanGastroenterologyHypomagnesemia03 medical and health sciences0302 clinical medicineInternal medicineAntineoplastic Combined Chemotherapy ProtocolsmedicineHumansPharmacology (medical)MagnesiumAgedRetrospective StudiesPharmacologyCetuximabbusiness.industryHazard ratiomedicine.diseasePrognosisIrinotecanBevacizumabSurvival RateNephrocalcinosis030104 developmental biologyOncology030220 oncology & carcinogenesisFOLFIRICamptothecinFemaleFluorouracilbusinessColorectal Neoplasmsmedicine.drugFollow-Up StudiesAnti-cancer drugs
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