Search results for " END"

showing 10 items of 4885 documents

Small endogenous molecules as moiety to improve targeting of CNS drugs.

2016

A major challenge in the development of novel neuro-therapeutic agents is to effectively overcome the blood-brain barrier (BBB), which acts as a 'working dynamic barrier'. The core problem in the treatment of neurodegenerative diseases is failed delivery of potential medicines due to their inadequate permeation rate. Areas covered: The present review gives a summary of endogenous moieties used in synthesizing prodrugs, derivatives and bioisosteric drugs appositely designed to structurally resemble physiological molecular entities able to be passively absorbed or carried by specific carrier proteins expressed at BBB level. In particular, this overview focuses on aminoacidic, glycosyl, purine…

0301 basic medicinePharmaceutical ScienceEndogenyComputational biologyPharmacologyBlood–brain barrierDiffusion03 medical and health sciences0302 clinical medicinemedicinesmall endogenous moleculesMoietyCNS prodrugAnimalsHumansProdrugsmultifunctional drugbiologyMembrane transport proteinChemistryCNS carrierMembrane Transport ProteinsTranslation (biology)TransporterBiological TransportProdrug030104 developmental biologymedicine.anatomical_structurebioisosteric drugCarrier proteinSettore CHIM/09 - Farmaceutico Tecnologico ApplicativoBlood-Brain Barrierbiology.proteinCarrier ProteinsBBB030217 neurology & neurosurgeryCentral Nervous System AgentsExpert opinion on drug delivery
researchProduct

Estrogen Receptor Signaling and the PI3K/Akt Pathway Are Involved in Betulinic Acid-Induced eNOS Activation

2016

Betulinic acid (BA) is a naturally occurring pentacyclic triterpenoid with anti-inflammatory, antiviral and anti-cancer properties. Beneficial cardiovascular effects such as increased nitric oxide (NO) production through enhancement of endothelial NO synthase (eNOS) activity and upregulation of eNOS expression have been demonstrated for this compound. In the present study, immortalized human EA.hy 926 endothelial cells were incubated for up to 1 h with 1–100 µM BA and with the phosphatidylinositol-3-kinase (PI3K) inhibitors LY294002 and wortmannin, or the estrogen receptor (ER) antagonist ICI 182,780. Phosphorylation status of eNOS and total eNOS protein were analyzed by Western blotting us…

0301 basic medicinePharmaceutical ScienceEstrogen receptorPI3KAnalytical ChemistryWortmanninchemistry.chemical_compound0302 clinical medicineEnosDrug DiscoveryLY294002PhosphorylationFulvestrantLungbiologyEstradiolendothelial cellsReceptors EstrogenChemistry (miscellaneous)030220 oncology & carcinogenesisMolecular MedicinePhosphorylationSignal transductionPentacyclic TriterpenesWortmanninSignal Transductionestrogen receptormedicine.medical_specialtyNitric Oxide Synthase Type IIIMorpholinesArticleCell Linelcsh:QD241-44103 medical and health sciencesbetulinic acidlcsh:Organic chemistryInternal medicinemedicineAnimalsHumansPhysical and Theoretical ChemistryProtein kinase BPI3K/AKT/mTOR pathwayendothelial nitric oxide synthaseAktOrganic ChemistryFibroblastsbiology.organism_classificationMolecular biologyTriterpenesbetulinic acid; endothelial nitric oxide synthase; endothelial cells; estrogen receptor; PI3K; AktRatsAndrostadienes030104 developmental biologyEndocrinologychemistryGene Expression RegulationChromonesPhosphatidylinositol 3-KinaseProto-Oncogene Proteins c-aktMolecules
researchProduct

Associations between dietary polyphenols and type 2 diabetes in a cross-sectional analysis of the PREDIMED-Plus Trial: role of body mass index and sex

2019

Overweight and obesity are important risk factors for type 2 diabetes (T2D). Moving towards healthier diets, namely, diets rich in bioactive compounds, could decrease the odds of suffering T2D. However, those individuals with high body mass index (BMI) may have altered absorption or metabolism of some nutrients and dietary components, including polyphenols. Therefore, we aimed to assess whether high intakes of some classes of polyphenols are associated with T2D in a population with metabolic syndrome and how these associations depend on BMI and sex. This baseline cross-sectional analysis includes 6633 participants from the PREDIMED-Plus trial. Polyphenol intakes were calculated from food fr…

0301 basic medicinePhysiologyCross-sectional studyClinical BiochemistryHydroxycinnamic acidsType 2 diabetesOverweightBiochemistry0302 clinical medicinepreventionFlavonoidesmetabolitesrisk2. Zero hungereducation.field_of_studyDiabetisDiabetes1. No poverty3. Good healthObesitatDietamedicine.symptommanagementHydroxybenzoic acidHydroxybenzoic acidsPhenolic acidsPopulationmen030209 endocrinology & metabolismArticleLignansCatechins2 cohorts03 medical and health sciencesEnvironmental healthcatechins diet flavonoids hydroxybenzoic acids hydroxycinnamic acids lignans obesity phenolic acids proanthocyanidinsmedicineProanthocyanidinsObesityeducationMolecular BiologyFlavonoids030109 nutrition & dieteticsbusiness.industrylcsh:RM1-950biomarkersnutritional and metabolic diseasesCell Biologymedicine.diseaseObesityDietlcsh:Therapeutics. PharmacologyMetabolic syndromebusinessBody mass index
researchProduct

MicroRNA as crucial regulators of gene expression in estradiol-treated human endothelial cells.

2018

Background/Aims: Estrogen signalling plays an important role in vascular biology as it modulates vasoactive and metabolic pathways in endothelial cells. Growing evidence has also established microRNA (miRNA) as key regulators of endothelial function. Nonetheless, the role of estrogen regulation on miRNA profile in endothelial cells is poorly understood. In this study, we aimed to determine how estrogen modulates miRNA profile in human endothelial cells and to explore the role of the different estrogen receptors (ERα, ERβ and GPER) in the regulation of miRNA expression by estrogen. Methods: We used miRNA microarrays to determine global miRNA expression in human umbilical vein endothelial cel…

0301 basic medicinePhysiologymedicine.drug_classEndothelial cellsCèl·lulesDown-RegulationEstrogen receptorEstrogen receptorsBiologylcsh:PhysiologyEpigenetic regulationReceptors G-Protein-Coupledlcsh:Biochemistry03 medical and health sciencesDownregulation and upregulationmicroRNAGene expressionHuman Umbilical Vein Endothelial CellsmedicineCluster AnalysisHumanslcsh:QD415-436EpigeneticsCells CulturedOligonucleotide Array Sequence AnalysisPrincipal Component AnalysisReceptors d'hormoneslcsh:QP1-981EstradiolGene Expression ProfilingUp-RegulationCell biologyGene expression profilingMicroRNAsMetabolic pathway030104 developmental biologyReceptors EstrogenEstrogenMiRNA
researchProduct

Stem Cells in Pituitary Tumors: Experimental Evidence Supporting Their Existence and Their Role in Tumor Clinical Behavior

2019

Although generally benign, pituitary tumors frequently show local invasiveness and resistance to pharmacological therapy. After the demonstration of the existence of pituitary gland stem cells, over the past decade, the presence of a stem cell subpopulation in pituitary tumors has been investigated, analogous to the cancer stem cell model developed for malignant tumors. This review recapitulates the experimental evidence supporting the existence of a population of stem-like cells in pituitary tumors, focusing on their potential role in tumor initiation, progression, recurrence and resistance to pharmacological therapy.

0301 basic medicinePituitary glandrecurrencePharmacological therapyMini ReviewEndocrinology Diabetes and MetabolisminvasivenessPopulation030209 endocrinology & metabolismTumor initiationmedicine.disease_causelcsh:Diseases of the endocrine glands. Clinical endocrinologyresistance03 medical and health sciences0302 clinical medicineEndocrinologyCancer stem cellpituitary tumorsstem cellsmedicineeducationinvasiveness; pituitary tumors; recurrence; resistance; stem cells; tumourigenesiseducation.field_of_studylcsh:RC648-665business.industryPituitary tumorsmedicine.disease030104 developmental biologymedicine.anatomical_structuretumourigenesisCancer researchStem cellCarcinogenesisbusinessFrontiers in Endocrinology
researchProduct

TGF-β Serum Levels in Diabetic Retinopathy Patients and the Role of Anti-VEGF Therapy.

2020

Transforming growth factor &beta

0301 basic medicinePlacental growth factorMaleVascular Endothelial Growth Factor Aserum biomarkersGastroenterologylcsh:ChemistryPathogenesischemistry.chemical_compound0302 clinical medicineTransforming Growth Factor betaMedicineMolecular Targeted Therapylcsh:QH301-705.5SpectroscopyAfliberceptAged 80 and overGeneral MedicineDiabetic retinopathyTGFComputer Science ApplicationsVascular endothelial growth factor ABiomarker (medicine)Intercellular Signaling Peptides and ProteinsFemaleTomography Optical Coherencemedicine.drugmedicine.medical_specialtyanti-VEGFAAnti-VEGFA; Diabetic retinopathy; Serum biomarkers; TGFCatalysisArticleProinflammatory cytokineInorganic Chemistry03 medical and health sciencesTGFβInternal medicineHumansPhysical and Theoretical ChemistryMolecular BiologyAgedDiabetic Retinopathybusiness.industryOrganic Chemistrymedicine.diseaseeye diseases030104 developmental biologylcsh:Biology (General)lcsh:QD1-999chemistryDiabetes Mellitus Type 2ROC Curve030221 ophthalmology & optometryGlycated hemoglobinbusinessBiomarkersInternational journal of molecular sciences
researchProduct

Prognostic use of soluble fms-like tyrosine kinase-1 and placental growth factor in patients with coronary artery disease.

2015

Background: Intention of the study is to assess the cardiovascular mortality of patients with coronary artery disease (CAD) with the biomarkers of angiogenesis PlGF and its endogenous inhibitor sFlt-1. Methods: The cohort included n = 1848 patients with CAD and 282 subjects without CAD. In 85 patients cardiovascular mortality, as combination of fatal myocardial infarction or any cardiac death, during a median follow-up duration of 3.9 years was reported. Results: In Kaplan–Meier curve analysis PlGF in rising thirds was not predictive regarding outcome (p = 0.54), the same was shown for sFlt-1 (p = 0.44). Cox regression for the fully adjusted model provided a hazard ratio (HR) of 0.8 (p = 0…

0301 basic medicinePlacental growth factorMalemedicine.medical_specialtyClinical BiochemistryCoronary Artery DiseaseKaplan-Meier Estimate030204 cardiovascular system & hematologyPregnancy ProteinsCoronary artery disease03 medical and health scienceschemistry.chemical_compound0302 clinical medicineInternal medicineDrug DiscoveryNatriuretic Peptide BrainmedicineHumansMyocardial infarctionPlacenta Growth FactorVascular Endothelial Growth Factor Receptor-1Proportional hazards modelbusiness.industryBiochemistry (medical)Hazard ratioMiddle Agedmedicine.diseasePrognosisPeptide FragmentsVascular endothelial growth factor030104 developmental biologyEndocrinologychemistryCohortCardiologyFemalebusinessSoluble fms-like tyrosine kinase-1Follow-Up StudiesBiomarkers in medicine
researchProduct

The habitual nature of food purchases at the supermarket: Implications for policy making

2020

Abstract Supermarkets have become the most important provider of food products worldwide. However, empirical evidence about how consumers make their food purchase decisions in this environment is still scarce. The present field study aimed to: i) explore how people make their in-store food purchases, and ii) identify the information they search for when making those purchases. Consumers (n = 144) were intercepted when entering the facilities of three supermarkets in two Uruguayan cities. They were asked to wear a mobile eye-tracker while they made their purchases as they normally do. The great majority of the consumers bought at least one food product or beverage (92%) and, on average, exam…

0301 basic medicinePoint of salePolicy makingPsychological intervention030209 endocrinology & metabolismContext (language use)computer.software_genreHealthful foodBeveragesFood Preferences03 medical and health sciences0302 clinical medicineHumansSupermarketsPolicy MakingEmpirical evidenceGeneral Psychology030109 nutrition & dieteticsNutrition and DieteticsAdvertisingConsumer BehaviorProduct (business)Shopping basketFoodBusinesscomputerAppetite
researchProduct

Emerging Roles of RNA 3′-end Cleavage and Polyadenylation in Pathogenesis, Diagnosis and Therapy of Human Disorders

2020

A crucial feature of gene expression involves RNA processing to produce 3′ ends through a process termed 3′ end cleavage and polyadenylation (CPA). This ensures the nascent RNA molecule can exit the nucleus and be translated to ultimately give rise to a protein which can execute a function. Further, alternative polyadenylation (APA) can produce distinct transcript isoforms, profoundly expanding the complexity of the transcriptome. CPA is carried out by multi-component protein complexes interacting with multiple RNA motifs and is tightly coupled to transcription, other steps of RNA processing, and even epigenetic modifications. CPA and APA contribute to the maintenance of a multitude of dive…

0301 basic medicinePolyadenylationcardiovascular disorderslcsh:QR1-502ReviewComputational biologyBiologyPolyadenylationCleavage (embryo)Biochemistrylcsh:MicrobiologyTranscriptome03 medical and health sciences0302 clinical medicineTranscription (biology)NeoplasmsGene expressionHumansDirectionalitycancerheterocyclic compoundsEpigeneticsMolecular BiologyRNA Cleavagediseasetherapyalternative polyadenylationRNAfood and beveragesNeurodegenerative Diseases3′ end processing030104 developmental biologyCardiovascular Diseases030220 oncology & carcinogenesisneurodegenerative disorderscardiovascular systemRNAbiomarkercleavage and polyadenylationBiomolecules
researchProduct

Basement Membrane Mimics of Biofunctionalized Nanofibers for a Bipolar-Cultured Human Primary Alveolar-Capillary Barrier Model

2017

In vitro reconstruction of an alveolar barrier for modeling normal lung functions and pathological events serve as reproducible, high-throughput pharmaceutical platforms for drug discovery, diagnosis, and regenerative medicine. Despite much effort, the reconstruction of organ-level alveolar barrier functions has failed due to the lack of structural similarity to the natural basement membrane, functionalization with specific ligands for alveolar cell function, the use of primary cells and biodegradability. Here we report a bipolar cultured alveolar-capillary barrier model of human primary cells supported by a basement membrane mimics of fully synthetic bifunctional nanofibers. One-step elect…

0301 basic medicinePolymers and PlasticsPolyestersNanofibersBiocompatible MaterialsBioengineeringNanotechnology02 engineering and technologyRegenerative medicineBasement MembranePermeabilityPolyethylene GlycolsBiomaterialsAlveolar cells03 medical and health sciencesTissue engineeringCell Line TumorCell AdhesionHuman Umbilical Vein Endothelial CellsMaterials ChemistrymedicineHumansBasement membraneTissue EngineeringTissue ScaffoldsChemistryEndothelial Cellsrespiratory system021001 nanoscience & nanotechnologyElectrospinningPolyester030104 developmental biologymedicine.anatomical_structureNanofiberBiophysicsSurface modification0210 nano-technologyBiomacromolecules
researchProduct