Search results for "Loi"

showing 10 items of 4617 documents

Synthesis, antitumor activity and CDK1 inhibiton of new thiazole nortopsentin analogues

2017

A new series of thiazole nortopsentin analogues was conveniently synthesized with fair overall yields. The antiproliferative activity of the new derivatives was tested against different human tumor cell lines of the NCI full panel. Four of them showed good antitumor activity with GI(50) values from micro to nanomolar level. The mechanism of the antiproliferative effect of these derivatives, was pro-apoptotic, being associated with externalization of plasma membrane phosphatidylserine and DNA fragmentation. The most active and selective of the new thiazoles confined viable cells in G2/M phase and markedly inhibited in vitro CDK1 activity. (C) 2017 Elsevier Masson SAS.

0301 basic medicineIndolesCell SurvivalStereochemistryMolecular ConformationNortopsentin analogues3-b]pyridinesAntineoplastic AgentsApoptosisMarine alkaloids Nortopsentin analogues Antiproliferative activity Apoptosis CDK1 inhibitors Thiazolyl-1H-pyrrolo[23-b]pyridinesAntiproliferative activity01 natural sciencesStructure-Activity Relationship03 medical and health scienceschemistry.chemical_compoundMarine alkaloidsCDC2 Protein KinaseDrug DiscoveryHumansThiazoleProtein Kinase InhibitorsCell ProliferationPharmacologyCyclin-dependent kinase 1Dose-Response Relationship DrugMarine alkaloids; Nortopsentin analogues; Antiproliferative activity; Apoptosis; CDK1 inhibitors; Thiazolyl-1H-pyrrolo[2; 3-b]pyridines010405 organic chemistryOrganic ChemistryImidazolesGeneral MedicinePhosphatidylserineThiazolyl-1H-pyrrolo[2Settore CHIM/08 - Chimica FarmaceuticaCyclin-Dependent KinasesIn vitro0104 chemical sciencesCDK1 inhibitors030104 developmental biologyMembranechemistryCell cultureApoptosisMCF-7 CellsDNA fragmentationCaco-2 CellsDrug Screening Assays Antitumor
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Sperm chromosomal abnormalities and their contribution to human embryo aneuploidy.

2018

In this work we reviewed 18 years of experience using fluorescence in situ hybridization (FISH) for sperm aneuploidy testing. We evaluated parameters associated with increased numerical sperm chromosome abnormalities and determined the male contribution to embryo aneploidies in terms of reproductive outcome by increased sperm aneuploidy. This retrospective study analyzed data from 2008 sperm samples of infertile males undergoing FISH analysis because of clinical history of repetitive implantation failure, recurrent miscarriage, impaired sperm parameters, or mixed causes. Sperm concentration was the only sperm parameter associated with FISH results—we observed a gradual increase of abnormal …

0301 basic medicineInfertilityMaleendocrine systemmedicine.medical_treatmentAneuploidyFertilization in VitroBiologyIntracytoplasmic sperm injectionMale infertilityAndrology03 medical and health sciences0302 clinical medicinePregnancymedicineHumansSperm Injections IntracytoplasmicPrecision Medicinereproductive and urinary physiologyIn Situ Hybridization FluorescenceInfertility MalePreimplantation DiagnosisRetrospective StudiesChromosome AberrationsComparative Genomic Hybridization030219 obstetrics & reproductive medicineIn vitro fertilisationmedicine.diagnostic_testSperm Counturogenital systemHigh-Throughput Nucleotide SequencingEmbryoCell BiologyGeneral MedicineOligospermiamedicine.diseaseAneuploidySpermSpermatozoa030104 developmental biologyReproductive MedicineSperm MotilityFemaleFluorescence in situ hybridizationBiology of reproduction
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Second-generation preimplantation genetic testing for aneuploidy in assisted reproduction: a SWOT analysis.

2019

Second-generation preimplantation genetic testing for aneuploidy (PGT-A 2.0) in patients with an unfavourable reproductive and IVF prognosis is becoming common practice, with the aim of improving reproductive outcomes. However, there is still no clear evidence on the possible advantages and drawbacks with regard to this procedure. In this discussion paper, based on a SWOT (strengths, weaknesses, opportunities, threats) analysis, the different aspects of this strategy are evaluated. Current evidence suggests that PGT-A 2.0 should not at present have an indiscriminate application, but it might be indicated in cases in which the risk of aneuploidy is increased.

0301 basic medicineInfertilityPregnancy RateReproduction (economics)AneuploidyBlastocyst biopsy03 medical and health sciences0302 clinical medicinePregnancymedicineLive birthHumansIn patientGenetic TestingSWOT analysisPreimplantation DiagnosisGenetic testing030219 obstetrics & reproductive medicinePreimplantation genetic testingmedicine.diagnostic_testbusiness.industryAssisted reproductionObstetrics and Gynecologymedicine.diseaseAneuploidyImplantationAbortion Spontaneous030104 developmental biologyReproductive MedicineRisk analysis (engineering)InfertilityFemalebusinessLive birthDevelopmental Biology
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Chromophore-Protein Interplay During the Phytochrome Photocycle Revealed by Step-Scan FTIR Spectroscopy

2018

Phytochrome proteins regulate many photoresponses of plants and microorganisms. Light absorption causes isomerization of the biliverdin chromophore, which triggers a series of structural changes to activate the signaling domains of the protein. However, the structural changes are elusive, and therefore the molecular mechanism of signal transduction remains poorly understood. Here, we apply two-color step-scan infrared spectroscopy to the bacteriophytochrome from Deinococcus radiodurans. We show by recordings in H2O and D2O that the hydrogen bonds to the biliverdin D-ring carbonyl become disordered in the first intermediate (Lumi-R) forming a dynamic microenvironment, then completely detach …

0301 basic medicineInfrared spectroscopyMolecular Dynamics SimulationBiochemistryCatalysis03 medical and health scienceschemistry.chemical_compoundchromophore-protein interplayColloid and Surface ChemistryBacterial ProteinsSpectroscopy Fourier Transform InfraredPeptide bondta116BiliverdinbiologyPhytochromeHydrogen bondBiliverdineta1182WaterHydrogen BondingDeinococcus radioduransGeneral ChemistryChromophorePhotochemical Processesbiology.organism_classification030104 developmental biologychemistryBiophysicsProtein Conformation beta-StrandDeinococcusPhytochromevalokemiaproteiinitSignal transductionstep-scan FTIR spectroscopyAdenylyl CyclasesJournal of the American Chemical Society
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Berberine Mediated Positive Inotropic Effects on Rat Hearts via a Ca2+-Dependent Mechanism

2020

Previous studies showed that berberine, an alkaloid from Coptis Chinensis Franch, might exert a positive inotropic effect on the heart. However, the underlying mechanisms were unclear. Here, we reported that berberine at 10-20 µM increased the left ventricular (LV) developed pressure and the maximal rate of the pressure rising, and it increased the maximal rate of the pressure descending at 20 µM in Langendorff-perfused isolated rat hearts. These effects diminished with the concentration of berberine increasing to 50 µM. In the concentration range of 50-300 µM, berberine increased the isometric tension of isolated left ventricular muscle (LVM) strips with or without electrical stimulations,…

0301 basic medicineInotropeheartPharmacology03 medical and health scienceschemistry.chemical_compound0302 clinical medicineBerberineNifedipineberberineExtracellularmedicineMyocytePharmacology (medical)positive inotropic effectPharmacologybiologyAlkaloidlcsh:RM1-950Coptis chinensisNa+biology.organism_classificationCa2+030104 developmental biologylcsh:Therapeutics. Pharmacologychemistry030220 oncology & carcinogenesisIntracellularmedicine.drugFrontiers in Pharmacology
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Exogenous TNFR2 activation protects from acute GvHD via host T reg cell expansion

2015

Activation of TNFR2 with a novel agonist expands T reg cells in vivo and protects allo-HCT recipients from acute GvHD while sparing antilymphoma and antiinfectious properties of transplanted donor T cells.

0301 basic medicineInterleukin 2medicine.medical_treatmentImmunologyGraft vs Host DiseaseMice Inbred Strainschemical and pharmacologic phenomenaHematopoietic stem cell transplantationBiologyT-Lymphocytes RegulatoryArticleMice03 medical and health sciencesInterleukin 21immune system diseaseshemic and lymphatic diseasesmedicineAnimalsReceptors Tumor Necrosis Factor Type IIImmunology and AllergyCytotoxic T cellddc:610Research Articlesintegumentary systemMyeloid-Derived Suppressor CellsHematopoietic Stem Cell TransplantationFOXP3hemic and immune systemsmedicine.diseaseLeukemiaddc:57030104 developmental biologysurgical procedures operativeAcute DiseaseImmunologyMyeloid-derived Suppressor CellInterleukin-2FemaleTumor necrosis factor receptor 2medicine.drug
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Human apolipoprotein A-I Gly26Arg stimulation of inflammatory responses via NF-kB activation: Potential roles in amyloidosis?

2018

The cascade of molecular events leading to Human apolipoprotein A–I (apoA–I) amyloidosis is not completely understood, not even the pathways that determine clinical manifestations associated to systemic protein deposition in organs such as liver, kidney and heart. About twenty natural variants of apoA–I were described as inducing amyloidosis, but the mechanisms driving their aggregation and deposition are still unclear. We previously identified that the mutant Gly26Arg but not Lys107-0 induced the release of cytokines and reactive oxygen species from cultured RAW 264.7 murine macrophages, suggesting that part of the pathogenic pathway could elicit of an inflammatory signal. In this work we …

0301 basic medicineLipopolysaccharideMACROPHAGES ACTIVATIONMutantStimulationInflammationOxidative phosphorylationPathology and Forensic MedicineCiencias Biológicas03 medical and health scienceschemistry.chemical_compoundINFLAMMATIONPhysiology (medical)APOLIPOPROTEIN A-I VARIANTSmedicineNUCLEAR FACTOR-ΚBchemistry.chemical_classificationReactive oxygen speciesAmyloidosisNF-κBBioquímica y Biología Molecularmedicine.diseaseCell biology030104 developmental biologychemistryAMYLOIDOSISlipids (amino acids peptides and proteins)medicine.symptomCIENCIAS NATURALES Y EXACTASPathophysiology
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Amyloid β-peptide insertion in liposomes containing GM1-cholesterol domains.

2015

Neuronal membrane damage is related to the early impairments appearing in Alzheimer's disease due to the interaction of the amyloid β-peptide (Aβ) with the phospholipid bilayer. In particular, the ganglioside GM1, present with cholesterol in lipid rafts, seems to be able to initiate Aβ aggregation on membrane. We studied the thermodynamic and structural effects of the presence of GM1 on the interaction between Aβ and liposomes, a good membrane model system. Isothermal Titration Calorimetry highlighted the importance of the presence of GM1 in recruiting monomeric Aβ toward the lipid bilayer. Light and Small Angle X-ray Scattering revealed a different pattern for GM1 containing liposomes, bot…

0301 basic medicineLiposomeGangliosideAmyloid beta-PeptidesAmyloidCalorimetry Differential ScanningChemistryBilayerOrganic ChemistryBiophysicsIsothermal titration calorimetryG(M1) GangliosideBiochemistry03 medical and health sciences030104 developmental biologyMembraneCholesterolBiochemistryLiposomesThermodynamicslipids (amino acids peptides and proteins)A?-membrane interaction; Double layer perturbation; Isothermal titration calorimetry; Small angle X-ray scatteringLipid bilayerLipid raftBiophysical chemistry
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Myeloid cells do not contribute to gender-dependent differences in disease outcome in murine cutaneous leishmaniasis.

2015

Gender-associated differences in the outcome of infections are well known. Apart from behavior-released differences in their incidence, immunological factors also contribute to disease outcome. The underlying mechanisms are often unknown. Here, we show that in murine experimental leishmaniasis, female mice develop larger skin lesions that harbor significantly more parasites, exhibit increased parasite dissemination to visceral organs associated with a shift towards T helper (Th) 2 immunity with increased levels of IL-4. Antigen presenting cells (APC) responsible for T cell priming, such as macrophages or dendritic cells, were not involved in the process. Additionally, in adoptive transfer e…

0301 basic medicineMaleAdoptive cell transferMyeloidStromal cellT cellImmunologyLeishmaniasis CutaneousBiology03 medical and health sciencesMice0302 clinical medicineImmune systemTh2 CellsCutaneous leishmaniasismedicineAnimalsHumansCell LineageMyeloid CellsAntigen-presenting cellTh1-Th2 BalanceCells CulturedCell DifferentiationDendritic cellmedicine.diseaseHormonesMice Inbred C57BLDisease Models Animal030104 developmental biologymedicine.anatomical_structureImmunologyDisease ProgressionFemaleSexDisease SusceptibilityInterleukin-4Stromal Cells030215 immunologyCellular immunology
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The concerted amyloid-beta clearance of LRP1 and ABCB1/P-gp across the blood-brain barrier is linked by PICALM

2018

The accumulation of neurotoxic amyloid-beta (Aβ) in the brain is a characteristic hallmark of Alzheimer's disease (AD). The blood-brain barrier (BBB) provides a large surface area and has been shown to be an important mediator for removal of brain Aβ. Both, the ABC transporter P-glycoprotein (ABCB1/P-gp) and the receptor low-density lipoprotein receptor-related protein 1 (LRP1) have been implicated to play crucial roles in Aβ efflux from brain. Here, with immunoprecipitation experiments, co-immunostainings and dual inhibition of ABCB1/P-gp and LRP1, we show that both proteins are functionally linked, mediating a concerted transcytosis of Aβ through endothelial cells. Late-onset AD risk fact…

0301 basic medicineMaleAmyloid betaSwineImmunologyPrimary Cell CultureATP-binding cassette transporterBlood–brain barrierClathrinArticlePICALM03 medical and health sciencesBehavioral NeuroscienceMice0302 clinical medicineAlzheimer DiseasemedicineAnimalsATP Binding Cassette Transporter Subfamily B Member 1Mice KnockoutAmyloid beta-PeptidesbiologyEndocrine and Autonomic SystemsChemistryTumor Suppressor ProteinsPhosphatidylinositol bindingBrainEndothelial CellsLRP1Peptide FragmentsCell biologyDisease Models Animal030104 developmental biologymedicine.anatomical_structureTranscytosisReceptors LDLBlood-Brain BarrierMonomeric Clathrin Assembly Proteinsbiology.proteinTranscytosis030217 neurology & neurosurgeryLow Density Lipoprotein Receptor-Related Protein-1Brain, Behavior, and Immunity
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