Search results for "Cell death"

showing 10 items of 824 documents

Beyond Pseudo‐natural Products: Sequential Ugi/Pictet‐Spengler Reactions Leading to Steroidal Pyrazinoisoquinolines That Trigger Caspase‐Independent …

2021

In this work, we describe how stereochemically complex polycyclic compounds can be generated by applying a synthetic sequence comprising an intramolecular Ugi reaction followed by a Pictet-Spengler cyclization on steroid-derived scaffolds. The resulting compounds, which combine a fragment derived from a natural product and a scaffold not found in nature. are both structurally distinct and globally similar to natural products at the same time, and interrogate an alternative region of the chemical space. One of the new compounds showed significant antiproliferative activity on HepG2 cells through a caspase-independent cell-death mechanism, an appealing feature when new antitumor compounds are…

StereochemistryAntineoplastic AgentsSequence (biology)01 natural sciencesBiochemistryPiperazineschemistry.chemical_compoundDrug DiscoveryHumansGeneral Pharmacology Toxicology and PharmaceuticsCell ProliferationPharmacologyBiological ProductsNatural productPictet–Spengler reactionCell DeathMolecular Structure010405 organic chemistryOrganic ChemistryCaspase independentStereoisomerismHep G2 CellsIsoquinolinesChemical space0104 chemical sciences010404 medicinal & biomolecular chemistrychemistryCaspasesIntramolecular forceHepg2 cellsMolecular MedicineUgi reactionSteroidsDrug Screening Assays AntitumorChemMedChem
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11H‑Pyrido[3′,2′:4,5]pyrrolo[3,2‑c]cinnoline and Pyrido[3′,2′:4,5]pyrrolo[1,2‑c][1,2,3]benzotriazine: Two New Ring Systems with Antitumor Activity

2014

Derivatives of new ring systems 11H-pyrido[3',2':4,5]pyrrolo[3,2-c]cinnoline and pyrido[3',2':4,5]pyrrolo[1,2-c][1,2,3]benzotriazine have been prepared from the key intermediates 2-(1H-pyrrolo[2,3-b]pyridin-2-yl)anilines in excellent yields (94-99%) and screened by the National Cancer Institute (Bethesda, MD) on about 60 human tumor cell lines derived from nine cancer cell types. The tested compounds exhibited antiproliferative activity against all the human cell lines, showing comparable MG_MID (mean graph midpoint) values in the range of 0.74-1.15 μM. A particular efficacy was observed against the leukemia subpanel (GI50 = 0.73-0.0090 μM). Flow cytometric analysis of the cell cycle demons…

StereochemistryCinnolines; triazinesChemistry PharmaceuticalAntineoplastic AgentsApoptosisHeterocyclic Compounds 2-RingHeterocyclic Compounds 4 or More Ringschemistry.chemical_compoundJurkat CellsCell Line TumorNeoplasmsDrug DiscoverytriazinesHumansCinnolineCell Proliferationchemistry.chemical_classificationReactive oxygen speciesCell DeathChemistryCell growthCell CycleCell MembraneTemperatureDepolarizationCell cycleCaspase InhibitorsMitochondriaEnzyme ActivationCell cultureApoptosisCaspasesCinnolines triazinesCancer cellMolecular MedicineLysosomesReactive Oxygen SpeciesCinnolines
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Stereoselective synthesis and determination of the cytotoxic properties of spicigerolide and three of its stereoisomers.

2003

Stereoselective syntheses of the naturally occurring, cytotoxic lactone spicigerolide and three nonnatural stereoisomers thereof are described. The commercially available sugar l-rhamnose was in all cases the chiral starting material. Key steps in each of these syntheses were asymmetric Brown allylations and ring-closing metatheses. The cytotoxic activities of the four lactones against a range of tumoral lines were then determined.

StereochemistryRhamnoseStereoisomerismAntineoplastic AgentsMetathesisChemical synthesisRhamnosechemistry.chemical_compoundLactonesStructure-Activity RelationshipCell Line TumorCytotoxic T cellStructure–activity relationshipOrganic chemistryHumanschemistry.chemical_classificationCell DeathChemistryorganic chemicalsOrganic ChemistryStereoisomerismGeneral MedicineSpicigerolideAldoseCyclizationOrgan SpecificityStereoselectivityLactoneThe Journal of organic chemistry
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Vulnerability of peripheral catecholaminergic neurons to MPTP is not regulated by alpha-synuclein.

2010

Although generally considered a prototypical movement disorder, Parkinson's disease is commonly associated with a broad-spectrum of non-motor symptoms, including autonomic dysfunctions caused by significant alterations in catecholaminergic neurons of the peripheral sympathetic nervous system. Here we present evidence that alpha-synuclein is highly expressed by sympathetic ganglion neurons throughout embryonic and postnatal life and that it is found in tyrosine hydroxylase-positive sympathetic fibers innervating the heart of adult mice. However, mice deficient in alpha-synuclein do not exhibit any apparent alterations in sympathetic development. Sympathetic neurons isolated from mouse embryo…

Sympathetic nervous system1-Methyl-4-phenylpyridiniumα-Synuclein knockoutTyrosine 3-MonooxygenaseNeurotoxinsNeurotrophic factorSubstantia nigraBiologylcsh:RC321-571chemistry.chemical_compoundMiceCatecholaminesSympathetic Fibers PostganglionicParkinsonian DisordersNeurotrophic factorsmedicineNeurotoxinAutonomic gangliaAnimalslcsh:Neurosciences. Biological psychiatry. NeuropsychiatryCells CulturedNeuronsGanglia SympatheticCell DeathMPTPSympathetic ganglionMice Mutant Strainsnervous system diseasesMPP+medicine.anatomical_structureNeurologychemistrynervous system1-Methyl-4-phenyl-1236-tetrahydropyridinePeripheral nervous systemSympathetic nervous systemNerve Degenerationalpha-SynucleinCatecholaminergic cell groupsPeripheral nervous systemNeuroscienceNeurobiology of disease
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Immune ambivalence: The schizophrenic bleomycin.

2013

In addition to cytotoxic effects, anticancer agents can exert multiple immunomodulatory functions. We have recently described the molecular mechanisms whereby bleomycin can 1) promote endoplasmic reticulum stress, causing the immunogenic death of cancer cells and hence strengthening antitumor CD8+ T cell responses; and 2) induce the secretion of transforming growth factor β (TGFβ), which stimulates regulatory T cells. This suggests that bleomycin may be favorably combined with TGFβ-targeting strategies.

T cellImmunologyBleomycinregulatory T cellschemistry.chemical_compoundImmune systemimmunogenic cell deathmedicineImmunology and AllergyCytotoxic T cellAuthor's Viewtransforming growth factor betabiologybusiness.industryTransforming growth factor betamedicine.anatomical_structuremouse studyOncologychemistryCancer cellImmunologyCancer researchbiology.proteinImmunogenic cell deathbusinessbleomycineTransforming growth factorOncoimmunology
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Regulation of T-cell apoptosis in inflammatory bowel disease: to die or not to die, that is the mucosal question.

2001

T-cell resistance against apoptosis contributes to inappropriate T-cell accumulation and the perpetuation of chronic mucosal inflammation in inflammatory bowel diseases (IBDs). Anti-interleukin-12 (IL-12) and anti-IL-6 receptor antibodies suppress colitis activity by the induction of T-cell apoptosis. These findings have important implications for the design of effective treatment regimens in IBD.

T-LymphocytesImmunologyApoptosisInflammatory bowel diseaseImmunology and AllergyMedicineEffective treatmentAnimalsHumansColitisIntestinal MucosaReceptorImmunity MucosalT-cell apoptosisbiologyCell Deathbusiness.industryInflammatory Bowel Diseasesmedicine.diseaseInflammatory Bowel Diseasesdigestive system diseasesApoptosisImmunologybiology.proteinAntibodybusinessTrends in immunology
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Tolerance without clonal expansion: self-antigen-expressing B cells program self-reactive T cells for future deletion.

2008

Abstract B cells have been shown in various animal models to induce immunological tolerance leading to reduced immune responses and protection from autoimmunity. We show that interaction of B cells with naive T cells results in T cell triggering accompanied by the expression of negative costimulatory molecules such as PD-1, CTLA-4, B and T lymphocyte attenuator, and CD5. Following interaction with B cells, T cells were not induced to proliferate, in a process that was dependent on their expression of PD-1 and CTLA-4, but not CD5. In contrast, the T cells became sensitive to Ag-induced cell death. Our results demonstrate that B cells participate in the homeostasis of the immune system by abl…

T-LymphocytesProgrammed Cell Death 1 ReceptorAutoimmunityAntigens CD/biosynthesisAntigens CD5/geneticsAutoantigensInterleukin 21MiceImmunology and AllergyCytotoxic T cellHomeostasisCTLA-4 AntigenIL-2 receptorAntigens Differentiation/biosynthesisB-LymphocytesAntigens CD/geneticsB-Lymphocytes/immunologyT-Lymphocytes/metabolismNatural killer T cellCell biologymedicine.anatomical_structureHomeostasis/immunology2723 Immunology and AllergyAntigens CD5/biosynthesisAntigens Differentiation/geneticsAntigens CD5/immunologyT cellImmunologyAntigens CD/immunologyClonal Deletion610 Medicine & healthchemical and pharmacologic phenomenaMice TransgenicBiologyAutoantigens/biosynthesisCD5 AntigensAutoimmunity/physiologyAutoantigens/immunologyAntigens CDmedicineAnimalsB-Lymphocytes/metabolismAntigen-presenting cellCell Proliferation2403 ImmunologyAntigens Differentiation/immunologyGene Expression Regulation/immunologyCD40Clonal Deletion/physiologyT-Lymphocytes/immunologyAntigens Differentiation10040 Clinic for NeurologyB-1 cellGene Expression Regulationbiology.protein
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Retinoic Acid Induces Apoptosis-Associated Neural Differentiation of a Murine Teratocarcinoma Cell Line

2002

Abstract: Incubation with all-trans retinoic acid (RA) induces PCC7-Mz1 embryonic carcinoma cells to cease proliferation and to develop into a tissue-like pattern of neuronal, astroglial, and fibroblast-like derivatives over a period of several days. Concomitant with the induction of differentiation by RA, a sizable fraction of the Mz1 stem cells detaches and dies, with the maximal level of cell death achieved after 10 h of RA treatment. This RA-induced cell death fulfills all criteria of apoptosis, including nuclear condensation, intranucleosomal DNA degradation, expression of cysteine aspases (caspases), and the formation of apoptotic bodies. Apoptosis could be suppressed by the pan-caspa…

TeratocarcinomaProgrammed cell deathCellular differentiationRetinoic acidApoptosisTretinoinBiochemistryMiceCellular and Molecular Neurosciencechemistry.chemical_compoundGAP-43 ProteinTumor Cells CulturedAnimalsProtein Kinase CProtein kinase CCaspaseNeuronsbiologyCell DifferentiationGenes bcl-2Cell biologyGene Expression RegulationchemistryBiochemistryCell cultureApoptosisPhorbolbiology.proteinJournal of Neurochemistry
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2-Hydroxyoleic Acid Induces ER Stress and Autophagy in Various Human Glioma Cell Lines

2012

Background: 2-Hydroxyoleic acid is a synthetic fatty acid with potent anti-cancer activity which does not induce undesired side effects. However, the molecular and cellular mechanisms by which this compound selectively kills human glioma cancer cells without killing normal cells is not fully understood. The present study was designed to determine the molecular bases underlying the potency against 1321N1, SF-767 and U118 human glioma cell lines growth without affecting non cancer MRC-5 cells. Methodology/Principal Findings: The cellular levels of endoplasmic reticulum (ER) stress, unfolded protein response (UPR) and autophagy markers were determined by quantitative RT-PCR and immunoblotting …

Tetrazolium SaltsOleic AcidsEndoplasmic ReticulumBiochemistry2-Hydroxyoleic AcidDrug DiscoveryMolecular Cell BiologyNeurological TumorsLungProtein MetabolismCellular Stress ResponsesMultidisciplinaryCell DeathBrain NeoplasmsQFatty AcidsRGliomaLipidsSignaling CascadesCell biologyOncologyMedicineSignal transductionResearch ArticleBiotechnologySignal TransductionCell SurvivalScienceAntineoplastic AgentsBiologyStress Signaling CascadeCell LineGliomaCell Line TumormedicineAutophagyHumansBiologyAutophagyProteinsCancers and NeoplasmsFibroblastsmedicine.diseaseChaperone ProteinsThiazolesMetabolismCell cultureApoptosisCancer cellUnfolded protein responsePLoS ONE
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Short‐term hypoxia promotes vascularization in co‐culture system consisting of primary human osteoblasts and outgrowth endothelial cells

2019

Prevascularization of tissue constructs before implantation has been developed as a novel and promising concept for successful implantation. Since hypoxia might induce angiogenesis, we have investigated the effects of hypoxic treatment on vascularization by using co-cultures of primary human osteoblasts (POBs) and outgrowth endothelial cells. Our results show that: (a) repeated short-term hypoxia (2% O2 for 8 hr), not long-term hypoxia (2% O2 for 24 hr), over 1 or 2 weeks, significantly enhances microvessel formation in co-cultures; (b) sustained hypoxia, not short-term or long-term hypoxia, causes cytotoxicity in mono- and co-cultures; (c) the expression of some angiogenic and inflammatory…

Time FactorsMaterials scienceCell SurvivalAngiogenesisProtein subunitmedicine.medical_treatment0206 medical engineeringBiomedical EngineeringNeovascularization Physiologic02 engineering and technologyBone tissueBiomaterialschemistry.chemical_compoundmedicineHumansRNA MessengerCytotoxicityMicrovesselCells CulturedOsteoblastsCell DeathGrowth factorMetals and AlloysEndothelial CellsHypoxia (medical)021001 nanoscience & nanotechnology020601 biomedical engineeringCell HypoxiaCoculture TechniquesUp-RegulationVascular endothelial growth factormedicine.anatomical_structurechemistryCeramics and CompositesCancer researchInflammation Mediatorsmedicine.symptom0210 nano-technologyJournal of Biomedical Materials Research Part A
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