Search results for "Therapeutics"

showing 10 items of 489 documents

Microenvironmental adaptation of experimental tumours to chronic vs acute hypoxia

2004

This study investigated long-term microenvironmental responses (oxygenation, perfusion, metabolic status, proliferation, vascular endothelial growth factor (VEGF) expression and vascularisation) to chronic hypoxia in experimental tumours. Experiments were performed using s.c.-implanted DS-sarcomas in rats. In order to induce more pronounced tumour hypoxia, one group of animals was housed in a hypoxic atmosphere (8% O(2)) for the whole period of tumour growth (chronic hypoxia). A second group was acutely exposed to inspiratory hypoxia for only 20 min prior to the measurements (acute hypoxia), whereas animals housed under normal atmospheric conditions served as controls. Acute hypoxia reduced…

DNA ReplicationMaleCancer ResearchPathologymedicine.medical_specialtyBiologyperfusionRats Sprague-Dawleychemistry.chemical_compoundOxygen ConsumptionVascularityIn vivomedicineAnimalsExperimental TherapeuticshypoxiaCell growthDNA NeoplasmNeoplasms ExperimentalOxygenationHypoxia (medical)VEGFCell HypoxiaRatsVascular endothelial growth factorDisease Models AnimalKineticscell proliferationBlood pressureOncologychemistryvascularityAcute DiseaseChronic Diseaseoxygenationmedicine.symptomPerfusionCell DivisionBritish Journal of Cancer
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Defensive strategies in a big obese group [MECCANISMI DI DIFESA IN UN GRUPPO DI PERSONE CON OBESITA']

2013

Aim. The aim of this study was to explore thè defense mechanisms of people with moderate and severe obesity. In fact, thè defensive structure is an effective predictor for thè best management of thè disease. Methods. 204 people (164 F-40 M) bave been recruited: 40 with BMI between 30 and 34.9, with moderate obesity, 36 with BMI between 35 and 39.9, with severe obesity, and 128 with BMI>40, with serious obesity, ali of them pertaining to thè clinic for obesity treatment at University Hospital of Palermo. Ali subjects were administered thè Defense Mechanisms Inventory (DMI), a type of reactive that explores defense mechanisms. The psychiatric comorbidity was excluded by thè DSM (SCIDI and II)…

Defence mechanismSettore M-PSI/08 - Psicologia ClinicaObesityTherapeuticsSettore MED/25 - PsichiatriaSettore MED/39 - Neuropsichiatria Infantile
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Role of Myeloid-Epithelial-Reproductive Tyrosine Kinase and Macrophage Polarization in the Progression of Atherosclerotic Lesions Associated With Non…

2019

Recent lines of evidence highlight the involvement of myeloid-epithelial-reproductive tyrosine kinase (MerTK) in metabolic disease associated with liver damage. MerTK is mainly expressed in anti-inflammatory M2 macrophages where it mediates transcriptional changes including suppression of proinflammatory cytokines and enhancement of inflammatory repressors. MerTK is regulated by metabolic pathways through nuclear sensors including LXRs, PPARs, and RXRs, in response to apoptotic bodies or to other sources of cholesterol. Nonalcoholic fatty liver disease (NAFLD) is one of the most serious public health problems worldwide. It is a clinicopathological syndrome closely related to obesity, insuli…

Drug targeting0301 basic medicineMacrophageMacrophage polarizationInflammationReviewMonocyteProinflammatory cytokine03 medical and health sciencesMerTK0302 clinical medicineFibrosisNonalcoholic fatty liver diseasemedicineNonalcoholic fatty liver diseaseMacrophagePharmacology (medical)InflammationPharmacologybusiness.industrylcsh:RM1-950Lipid metabolismMERTKmedicine.diseasemacrophagesAtherosclerosis; Drug targeting; Inflammation; Macrophages; MerTK; Monocytes; Nonalcoholic fatty liver diseaselcsh:Therapeutics. Pharmacology030104 developmental biologyAtherosclerosi030220 oncology & carcinogenesisCancer researchatherosclerosismedicine.symptommonocytesbusinessFrontiers in Pharmacology
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Polymer-doxycycline conjugates as fibril disrupters: an approach towards the treatment of a rare amyloidotic disease.

2014

The term amyloidosis describes neurological diseases where an abnormal protein is misfolded and accumulated as deposits in organs and tissues, known as amyloid, disrupting their normal function. In the most common familial amyloid polyneuropathy (FAP), transthyretin (TTR) displays this role primarily affecting the peripheral nervous system (PNS). Advanced stages of this inherited rare amyloidosis, present as fibril deposits that are responsible for disease progression. In order to stop disease progression, herein we designed an efficient family of nanoconjugates as fibril disrupters. These polymer conjugates are based on doxycycline (doxy), already in phase II trials for Alzheimer's disease…

DrugAmyloidErythrocytesAmyloidmedia_common.quotation_subjectPharmaceutical ScienceMice TransgenicFibrilHemolysisPlasmaIn vivomedicinePolymeric drugAnimalsTissue DistributionAmyloid disruptersmedia_commonDoxycyclineAmyloid Neuropathies FamilialMice Inbred BALB CbiologyChemistryAmyloidosismedicine.diseaseRare diseasesRatsTransthyretinPolymer-drug conjugateDisease Models AnimalDrug LiberationBiochemistryPolyglutamic AcidDoxycyclineDrug deliveryDrug deliverybiology.proteinCancer researchPolymer therapeuticsmedicine.drugJournal of controlled release : official journal of the Controlled Release Society
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Predicting the risk of drug–drug interactions in psychiatric hospitals: a retrospective longitudinal pharmacovigilance study

2021

ObjectivesThe aim was to use routine data available at a patient’s admission to the hospital to predict polypharmacy and drug–drug interactions (DDI) and to evaluate the prediction performance with regard to its usefulness to support the efficient management of benefits and risks of drug prescriptions.DesignRetrospective, longitudinal study.SettingWe used data from a large multicentred pharmacovigilance project carried out in eight psychiatric hospitals in Hesse, Germany.ParticipantsInpatient episodes consecutively discharged between 1 October 2017 and 30 September 2018 (year 1) or 1 January 2019 and 31 December 2019 (year 2).Outcome measuresThe proportion of rightly classified hospital epi…

DrugHospitals PsychiatricLongitudinal studymedicine.medical_specialtymedia_common.quotation_subjectHealth informaticslaw.invention03 medical and health sciencesPharmacovigilance0302 clinical medicinelawRisk FactorsGermanyPharmacovigilanceMedicineHumans1723Drug Interactions030212 general & internal medicine1506Longitudinal StudiesMedical prescriptionPsychiatryhealth informaticsmedia_commonRetrospective StudiesPolypharmacyClinical pharmacologyReceiver operating characteristicbusiness.industryRGeneral MedicinePharmacology and Therapeuticspsychiatry030227 psychiatryPharmaceutical PreparationsMedicineclinical pharmacologybusinessBMJ Open
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Clinical and immunological aspects of microRNAs in neonatal sepsis

2022

Abstract Neonatal sepsis constitutes a highly relevant public health challenge and is the most common cause of infant morbidity and mortality worldwide. Recent studies have demonstrated that during infection epigenetic changes may occur leading to reprogramming of gene expression. Post-transcriptional regulation by short non-coding RNAs (e.g., microRNAs) have recently acquired special relevance because of their role in the regulation of the pathophysiology of sepsis and their potential clinical use as biomarkers. ~22-nucleotide of microRNAs are not only involved in regulating multiple relevant cellular and molecular functions, such as immune cell function and inflammatory response, but have…

Epigenetic changesInflammationRM1-950BioinformaticsEpigenesis GeneticSepsisImmune systemInfant morbiditymicroRNAmedicineAnimalsHumansEpigeneticsInflammationPharmacologyNeonatal sepsisbusiness.industryInfant NewbornImmunityGeneral MedicinePrognosismedicine.diseaseMicroRNAsGene Expression RegulationNeonatal sepsisTherapeutics. Pharmacologymedicine.symptombusinessReprogrammingBiomarkersBiomedicine & Pharmacotherapy
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Glycosylated macromolecular conjugates of antiviral drugs with a polyaspartamide.

2004

Two new polymeric conjugates for specific liver targeting were prepared by conjugation of sugar moieties and antiviral drugs to alpha, beta-poly[N-2-(hydroxyethyl)-DL-aspartamide] (PHEA). PHEA-galactopyranosylphenylthiocarbamide-mono-O-succinylganciclovir (conjugate 7) and PHEA-mannopyranosylphenylthiocarbamide-O-succinylacyclovir (conjugate 8) were synthesized according to a multi-step procedure which allowed for obtaining high product yield and process standardization. Conjugate 7 contained 7.5 and 8.5% of galactose and ganciclovir (substituent/repeating unit, mol/mol), respectively, and conjugate 8 contained 14.2 and 10.8% of mannose and acyclovir, respectively. In vitro studies demonstr…

Ganciclovirchemistry.chemical_classificationMaleMice Inbred BALB CGlycosylationStereochemistryMacromolecular SubstancesSubstituentPharmaceutical ScienceMannoseGlycosidic bondAntiviral Agentschemistry.chemical_compoundHydrolysisMicePoly(hydroxyethylaspartamide) Bioconjugates Polymer therapeutics Liver targeting AntiviralschemistrySettore CHIM/09 - Farmaceutico Tecnologico ApplicativoGalactosemedicineMoietyAnimalsPeptidesmedicine.drugConjugateJournal of drug targeting
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Serological identification and expression analysis of gastric cancer-associated genes

2002

Serological identification of tumour antigens by recombinant expression cloning has proved to be an effective strategy for the identification of cancer-associated genes having a relevance to cancer aetiology and progression, and for defining possible targets for immunotherapeutic intervention. In the present study we applied this technique to identify immunogenic proteins for gastric cancer that resulted in isolation of 14 distinct serum-reactive antigens. In order to evaluate their role in tumourigenesis and assess the immunogenicity of the identified antigens, we characterised each cDNA clone by DNA sequence analysis, mRNA tissue distribution, comparison of mRNA levels in cancerous and ad…

Gene isoformCancer ResearchCandidate geneNUCB2autoantibodiesMolecular Sequence Datatumour antigensTbdn-1GranulinBiologymedicine.disease_causeAntigens NeoplasmStomach NeoplasmsComplementary DNAGene expressionmedicineHumansExperimental TherapeuticsGeneGene LibraryReverse Transcriptase Polymerase Chain ReactionChromosome MappingCancerSEREXSequence Analysis DNAmedicine.diseaseMolecular biologyOncologyTACC1CarcinogenesisBritish Journal of Cancer
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3H-1,2-benzoxathiepine 2,2-dioxides: a new class of isoform-selective carbonic anhydrase inhibitors

2017

Abstract A new chemotype with carbonic anhydrase (CA, EC 4.2.1.1) inhibitory action has been discovered, the homo-sulfocoumarins (3H-1,2-benzoxathiepine 2,2-dioxides) which have been designed considering the (sulfo)coumarins as lead molecules. An original synthetic strategy of a panel of such derivatives led to compounds with a unique inhibitory profile and very high selectivity for the inhibition of the tumour associated (CA IX/XII) over the cytosolic (CA I/II) isoforms. Although the CA inhibition mechanism with these new compounds is unknown for the moment, we hypothesize that it may be similar to that of the sulfocoumarins, i.e. hydrolysis to the corresponding sulfonic acids which therea…

Gene isoformStereochemistryHigh selectivityInhibitory postsynaptic potential01 natural sciencesStructure-Activity RelationshipHydrolysisCarbonic anhydraseDrug DiscoveryHumansMoleculeCarbonic Anhydrase InhibitorsCarbonic AnhydrasesPharmacologyCarbonic anhydraseDose-Response Relationship DrugMolecular Structurebiology010405 organic chemistryChemistrylcsh:RM1-950Active sitehomo-sulfocoumarinsGeneral MedicineCyclic S-Oxides0104 chemical sciencesinhibitor010404 medicinal & biomolecular chemistryCytosollcsh:Therapeutics. PharmacologyBiochemistrysulfocoumarinbiology.proteinResearch PaperJournal of Enzyme Inhibition and Medicinal Chemistry
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Disparity between Inter-Patient Molecular Heterogeneity and Repertoires of Target Drugs Used for Different Types of Cancer in Clinical Oncology

2020

Inter-patient molecular heterogeneity is the major declared driver of an expanding variety of anticancer drugs and personalizing their prescriptions. Here, we compared interpatient molecular heterogeneities of tumors and repertoires of drugs or their molecular targets currently in use in clinical oncology. We estimated molecular heterogeneity using genomic (whole exome sequencing) and transcriptomic (RNA sequencing) data for 4890 tumors taken from The Cancer Genome Atlas database. For thirteen major cancer types, we compared heterogeneities at the levels of mutations and gene expression with the repertoires of targeted therapeutics and their molecular targets accepted by the current guideli…

Gene mutationMedical OncologychemotherapyGenomeTranscriptomelcsh:ChemistryDrug Delivery SystemsProstateNeoplasmstumor heterogeneityMedicineCluster AnalysisMolecular Targeted TherapyPathology MolecularPrecision Medicinelcsh:QH301-705.5targeted therapeuticscancer drugsSpectroscopyExome sequencingGeneral MedicineGenomicspersonalized medicineComputer Science ApplicationsDrug repositioningmedicine.anatomical_structureAntineoplastic AgentsComputational biologyCatalysisArticleInorganic Chemistrymolecular diagnosticsGenetic HeterogeneityDrug TherapyExome SequencingHumansPhysical and Theoretical ChemistryMolecular Biologygenomeclinical oncologybusiness.industryOrganic ChemistryMolecular diagnosticsmutationslcsh:Biology (General)lcsh:QD1-999MutationPersonalized medicinebusinesstranscriptomeInternational Journal of Molecular Sciences
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