Search results for "regulation"

showing 10 items of 4463 documents

Targeting Orthosteric and Allosteric Pockets of Aromatase via Dual-Mode Novel Azole Inhibitors

2020

[Image: see text] Breast cancer (BC) is the most diffused cancer type in women and the second leading cause of death among the female population. Effective strategies to fight estrogen responsive (ER+) BC, which represents 70% of all BC cases, rely on estrogen deprivation, via the inhibition of the aromatase enzyme, or the modulation of its cognate estrogen receptor. Current clinical therapies significantly increased patient survival time. Nevertheless, the onset of resistance in metastatic BC patients undergoing prolonged treatments is becoming a current clinical challenge, urgently demanding to devise innovative strategies. In this context, here we designed, synthesized, and performed in …

medicine.drug_classAllosteric regulation01 natural sciencesBiochemistryBreast cancerbreast cancerDrug Discoverymedicinecytochromes P450AromataseCause of deathFemale populationchemistry.chemical_classificationbiology010405 organic chemistrybusiness.industrymolecular dynamicOrganic ChemistryDual modeAromatase inhibitormedicine.diseasemolecular dynamics0104 chemical sciences010404 medicinal & biomolecular chemistryAromatase inhibitorschemistryEstrogenSettore CHIM/03 - Chimica Generale E Inorganicaxanthonebiology.proteinCancer researchAzolebusiness
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Is cytokine expression responsible for differences between allergens and irritants?

1996

Abstract Irritant and allergic contact dermatitis are two very similar diseases, and differentiating between these two can be difficult clinically. Recently, cytokines have been identified as useful tools for differentiation. Thus, our laboratory has identified an early cytokine pattern in the induction phase of contact sensitivity that is specific for allergens and is not found after epicutaneous application of irritants or tolerogens. The upregulation of the Langerhans' cell—derived signal interleukin (IL)-1β early after allergen application especially seems to be highly specific for contact allergens. This cytokine was also found to be essential for the development of epicutaneous sensit…

medicine.drug_classChemistrymedicine.medical_treatmentInterleukinDermatologyAllergensMonoclonal antibodymedicine.disease_causemedicine.diseaseDermatitis ContactProinflammatory cytokineInterleukin-10CytokineAllergenmedicine.anatomical_structureDownregulation and upregulationImmunologyDermatitis Allergic ContactmedicineIrritantsCytokinesHumansAllergic contact dermatitisSensitizationInterleukin-1American journal of contact dermatitis : official journal of the American Contact Dermatitis Society
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Mucin 1 downregulation associates with corticosteroid resistance in chronic rhinosinusitis with nasal polyps

2013

Background A number of patients with chronic rhinosinusitis with nasal polyps (CRSwNP) are resistant to oral corticosteroids. Mucin 1 (MUC1) shows anti-inflammatory properties, and its cytoplasmic tail (CT) interacts with transcription factors, facilitating their nuclear translocation. Because glucocorticoid receptor (GR) nuclear translocation is key to the anti-inflammatory effect of corticosteroids, we hypothesized that MUC1 is involved in the effectiveness of corticosteroids. Objective To analyze the role of MUC1 in corticosteroid effectiveness in different cohorts of patients with CRSwNP and elucidate the possible mechanisms involved. Methods Seventy-three patients with CRSwNP took oral…

medicine.drug_classImmunologyAnti-Inflammatory AgentsDrug ResistanceDown-Regulationdigestive systemNasal PolypsReceptors GlucocorticoidGlucocorticoid receptorDownregulation and upregulationAdrenal Cortex HormonesmedicineHumansImmunology and AllergyNasal polypsSinusitisskin and connective tissue diseasesneoplasmsDexamethasoneMUC1Rhinitisbusiness.industryMucin-1Toll-Like ReceptorsMucinmedicine.diseasebiological factorsdigestive system diseasesNasal MucosaGene Expression RegulationChronic DiseaseImmunologyImmunohistochemistryCorticosteroidbusinessSignal Transductionmedicine.drugJournal of Allergy and Clinical Immunology
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The Efflux Pump MexXY/OprM Contributes to the Tolerance and Acquired Resistance of Pseudomonas aeruginosa to Colistin

2020

The intrinsic resistance of Pseudomonas aeruginosa to polymyxins in part relies on the addition of 4-amino-4-deoxy-l-arabinose (Ara4N) molecules to the lipid A of lipopolysaccharide (LPS), through induction of operon arnBCADTEF-ugd (arn) expression. As demonstrated previously, at least three two-component regulatory systems (PmrAB, ParRS, and CprRS) are able to upregulate this operon when bacteria are exposed to colistin. In the present study, gene deletion experiments with the bioluminescent strain PAO1::lux showed that ParRS is a key element in the tolerance of P. aeruginosa to this last-resort antibiotic (i.e., resistance to early drug killing). Other loci of the ParR regulon, such as th…

medicine.drug_classOperonPolymyxinMutantMicrobial Sensitivity Testsmedicine.disease_causeMicrobiologyLipid A03 medical and health sciencesBacterial ProteinsMechanisms of ResistanceDrug Resistance BacterialmedicinePharmacology (medical)ComputingMilieux_MISCELLANEOUS030304 developmental biologyPharmacology0303 health sciencesColistin030306 microbiologyPseudomonas aeruginosaChemistryMembrane Transport ProteinsGene Expression Regulation BacterialAnti-Bacterial AgentsInfectious DiseasesRegulonPseudomonas aeruginosa[SDE]Environmental SciencesColistinlipids (amino acids peptides and proteins)EffluxGene DeletionBacterial Outer Membrane Proteinsmedicine.drugAntimicrobial Agents and Chemotherapy
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Emotional lability in children and adolescents with attention deficit/hyperactivity disorder (ADHD): clinical correlates and familial prevalence

2010

Background: The goal of this study was to investigate the occurrence, severity and clinical correlates of emotional lability (EL) in children with attention deficit/hyperactivity disorder (ADHD), and to examine factors contributing to EL and familiality of EL in youth with ADHD. Methods: One thousand, one hundred and eighty-six children with ADHD combined type and 1827 siblings (aged 6–18 years) were assessed for symptoms of EL, ADHD, associated psychopathology and comorbid psychiatric disorders with a structured diagnostic interview (PACS) as well as parent and teacher ratings of psychopathology (SDQ; CPRS-R:L; CTRS-R:L). Analyses of variance, regression analyses, ?2-tests or loglinear mod…

medicine.medical_specialty05 social sciencesmedicine.diseaseIrritabilityEmotional dysregulationbehavioral disciplines and activities03 medical and health sciencesPsychiatry and Mental health0302 clinical medicineEl NiñoConduct disordermental disordersPediatrics Perinatology and Child HealthDevelopmental and Educational PsychologymedicineAttention deficit hyperactivity disorder0501 psychology and cognitive sciencesBipolar disordermedicine.symptomPsychiatryPsychology030217 neurology & neurosurgeryDevelopmental psychopathology050104 developmental & child psychologyPsychopathologyJournal of Child Psychology and Psychiatry
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Effects of endocrine disruptors on genes associated with 17 beta-estradiol metabolism and excretion

2008

International audience; In order to provide a global analysis of the effects of endocrine disruptors on the hormone cellular bioavailability, we combined 17 beta-estradiol (E2) cellular flow studies with real-time PCR and Western blot expression measurements of genes involved in the hormone metabolism and excretion. Three endocrine disruptors commonly found in food were chosen for this study, which was conducted in the estrogen receptor (ER) negative hepatoblastoma HepG2 cell line: bisphenol A (BPA), genistein (GEN) and resveratrol (RES). We showed that 24h after a single dose treatment with genistein, resveratrol or bisphenol A, the expression of ATP-binding cassette transporters (the mult…

medicine.medical_specialtyATP-BINDING CASSETTE TRANSPORTERS[SDV]Life Sciences [q-bio]Clinical BiochemistryBlotting WesternEstrogen receptorGenistein010501 environmental sciencesBiologyPharmacologyResveratrol01 natural sciencesBiochemistryCell LineENDOCRINE DISRUPTORS03 medical and health scienceschemistry.chemical_compoundEndocrinologyInternal medicineUDP-GLUCURONOSYLTRANFERASEmedicineHumansHormone metabolismRNA MessengerMolecular Biology030304 developmental biology0105 earth and related environmental sciencesDNA PrimersPharmacology0303 health sciencesBase SequenceEstradiolReverse Transcriptase Polymerase Chain ReactionMultidrug resistance-associated protein 2Organic ChemistrySULFOTRANSFERASEEndocrinologyEndocrine disruptorchemistryGene Expression Regulation13. Climate actionESTRADIOL METABOLISMMultidrug Resistance-Associated Proteinshormones hormone substitutes and hormone antagonistsHormone
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Effects of physical provocations on heart rate reactivity and reactive aggression in children

2006

This article presents complementary data on the relationship between the intensity of offensive and defensive aggression that was investigated by means of the computerised Pulkkinen Aggression Machine (PAM) paradigm [Juujarvi et al., 2001; Aggr Behav 27:430-445]. The recording of the electrocardiogram was conducted in a sample of 109 children (61 boys and 48 girls) while they completed the PAM. Across the conditions of controlled aggression, the simulated attack and defence evoked a mean increase of HR by 2.7 beats per minute (bpm), but the variation between children was substantial (-10.9 to +11.4 bpm). Children who showed a strong HR increase, moderate HR increase, or HR decrease were com…

medicine.medical_specialtyAggressionSocial anxietyPoison controlAudiologyDevelopmental psychologyArts and Humanities (miscellaneous)Injury preventionHeart rateDevelopmental and Educational PsychologymedicineHeart rate variabilityAutoregulationmedicine.symptomPsychologyReactivity (psychology)General PsychologyAggressive Behavior
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OGT and OGA expression in postmenopausal skeletal muscle associates with hormone replacement therapy and muscle cross-sectional area

2013

Protein glycosylation via O-linked N-acetylglucosaminylation (O-GlcNAcylation) is an important post-translational regulatory mechanism mediated by O-GlcNAc transferase (OGT) and responsive to nutrients and stress. OGT attaches an O-GlcNAc moiety to proteins, while O-GlcNAcase (OGA) catalyzes O-GlcNAc removal. In skeletal muscle of experimental animals, prolonged increase in O-GlcNAcylation associates with age and muscle atrophy. Here we examined the effects of hormone replacement therapy (HRT) and power training (PT) on muscle OGT and OGA gene expression in postmenopausal women generally prone to age-related muscle weakness. In addition, the associations of OGT and OGA gene expressions with…

medicine.medical_specialtyAgingGlycosylationTime Factorsmedicine.drug_classPlyometric ExerciseBiologyta3111N-AcetylglucosaminyltransferasesBiochemistryGene Expression Regulation EnzymologicEndocrinologyDownregulation and upregulationInternal medicineGene expressionGeneticsmedicineHumansMuscle StrengthRNA Messengerta315Muscle SkeletalMolecular BiologyFinlandGlyceraldehyde 3-phosphate dehydrogenasePlyometric power trainingEstrogen Replacement Therapyta1182Age FactorsMuscle weaknessSkeletal muscleta3141Cell BiologyMiddle Agedbeta-N-AcetylhexosaminidasesMuscle atrophyPostmenopausePhenotypeTreatment OutcomeEndocrinologymedicine.anatomical_structureEstrogenbiology.proteinFemaleMuscle atrophymedicine.symptomProtein Processing Post-TranslationalMuscle ContractionMuscle contraction
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Estradiol or genistein prevent Alzheimer's disease-associated inflammation correlating with an increase PPAR gamma expression in cultured astrocytes.

2009

Inflammation has been implicated in neurodegenerative disorders such as Alzheimer's disease (AD). The main inflammatory players in AD are the glial cells which initiate the inflammatory response. One of the earliest neuropathological changes in AD is the accumulation of astrocytes at sites of A beta deposition. It is desirable to find methods of tipping the balance towards anti-inflammatory state. Estrogenic compounds have shown anti-inflammatory and also antioxidant activity. Astrocytes were pretreated with 17-beta estradiol or with genistein, and 48 h later treated with 5 microM amyloid beta (A beta) for 24 h. We found that A beta induces inflammatory mediators, such as cyclooxygenase 2 (…

medicine.medical_specialtyAmyloid betaInterleukin-1betaGenisteinPeroxisome proliferator-activated receptorNitric Oxide Synthase Type IIInflammationEnzyme-Linked Immunosorbent Assaychemistry.chemical_compoundInternal medicinemedicineAnimalsDrug InteractionsMolecular BiologyProtein Kinase InhibitorsCells Culturedchemistry.chemical_classificationCerebral CortexAmyloid beta-PeptidesbiologyDose-Response Relationship DrugEstradiolTumor Necrosis Factor-alphaGeneral NeuroscienceInterleukinEstrogensGenisteinPeptide FragmentsRatsPPAR gammaEndocrinologymedicine.anatomical_structurechemistryGene Expression RegulationCyclooxygenase 2Astrocytesbiology.proteinNeurogliaTumor necrosis factor alphaNeurology (clinical)medicine.symptomDevelopmental BiologyAstrocyteBrain research
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Analysis of molecular mechanisms and anti-tumoural effects of zoledronic acid in breast cancer cells

2012

Zoledronic acid (ZOL) is the most potent nitrogen-containing bisphosphonate (N-BPs) that strongly binds to bone mineral and acts as a powerful inhibitor of bone resorption, already clinically available for the treatment of patients with osteolytic metastases. Recent data also suggest that ZOL, used in breast cancer, may provide more than just supportive care modifying the course of the disease, though the possible molecular mechanism of action is still unclear. As breast cancer is one of the primary tumours with high propensity to metastasize to the bone, we investigated, for the first time, differential gene expression profile on Michigan Cancer Foundation-7 (MCF-7) breast cancer cells tre…

medicine.medical_specialtyAngiogenesismedicine.medical_treatmentBlotting WesternAngiogenesis InhibitorsAntineoplastic AgentsBreast NeoplasmsBiologyReal-Time Polymerase Chain ReactionZoledronic AcidZOL FN1 TGF-b1 THBS-1 invasion breast cancerBone resorptionThrombospondin 1Transforming Growth Factor beta1breast cancerBreast cancerTGF-β1Internal medicineThrombospondin 1medicineHumansBone ResorptionCell ProliferationMatrigelDiphosphonatesFN1Gene Expression ProfilingImidazolesCancerOriginal ArticlesCell BiologyZOLBisphosphonateMicroarray Analysisinvasionmedicine.diseaseFibronectinsUp-RegulationGene Expression Regulation NeoplasticEndocrinologyZoledronic acidTHBS-1MCF-7 CellsCancer researchMolecular MedicineFemalemedicine.drug
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