Search results for " TOXICOLOGY AND PHARMACEUTICS"

showing 10 items of 461 documents

New insights in primary ciliary dyskinesia

2017

Introduction: Primary ciliary dyskinesia (PCD) is a rare genetic disease with an estimated prevalence of 1:20.000 births. It is characterized by abnormal motility of cilia, leading to impaired mucociliary clearance, and subsequent infection and chronic inflammation of the airways. PCD also affects spermatozoa and cilia in the Fallopian tubes, contributing to fertility issues; dyskinesia of embryonic nodal cilia causes a random distribution of the organs. Areas covered: An overview of the history, genetics, clinical manifestations in children and adults, diagnostic tests, treatments, and prognosis are reviewed. We also discuss current research and future prospects of PCD. Expert opinion: As …

0301 basic medicinePathologymedicine.medical_specialtyDiagnostic methodsbusiness.industryHealth PolicyCiliumMotilityClinical featuresDiseaseDiagnostic methodsmedicine.disease03 medical and health sciencesPrimary ciliary dyskinesia030104 developmental biology0302 clinical medicine030228 respiratory systemGeneticsotorhinolaryngologic diseasesmedicinePharmacology (medical)TherapybusinessPharmacology Toxicology and Pharmaceutics (miscellaneous)Primary ciliary dyskinesia
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Cystic fibrosis treatment: targeting the basic defect

2017

ABSTRACTIntroduction: Cystic Fibrosis (CF) is a disease caused by different class mutations in the CF transmembrane conductance regulator (CFTR) gene. It can therefore benefit from a personalized medicine approach based on the individual genotype of each patient.Areas covered: This review provides a detailed overview of the current major development of new CF treatments that target the basic CF defect. The review summarizes gene therapy, mRNA repair strategies, read-through agents, and CFTR-modulators (potentiators, correctors, stabilizers, amplifiers and different combination therapies).Expert opinion: We are currently perhaps at the most exciting stage in the history of CF, with the poten…

0301 basic medicinePathologymedicine.medical_specialtyMutationCombination therapybusiness.industryHealth PolicyGenetic enhancementDiseasePotentiatorBioinformaticsmedicine.diseasemedicine.disease_causeCystic fibrosisIvacaftor03 medical and health sciences030104 developmental biology0302 clinical medicine030228 respiratory systemMedicinePharmacology (medical)Personalized medicinebusinessPharmacology Toxicology and Pharmaceutics (miscellaneous)medicine.drugExpert Opinion on Orphan Drugs
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Antimicrobial and Antibiofilm Activity of a Recombinant Fragment of β-Thymosin of Sea Urchin Paracentrotus lividus

2018

With the aim to obtain new antimicrobials against important pathogens such as Staphylococcus aureus and Pseudomonas aeruginosa, we focused on antimicrobial peptides (AMPs) from Echinoderms. An example of such peptides is Paracentrin 1 (SP1), a chemically synthesised peptide fragment of a sea urchin thymosin. In the present paper, we report on the biological activity of a Paracentrin 1 derivative obtained by recombination. The recombinant paracentrin RP1, in comparison to the synthetic SP1, is 22 amino acids longer and it was considerably more active against the planktonic forms of S. aureus ATCC 25923 and P. aeruginosa ATCC 15442 at concentrations of 50 &micro

0301 basic medicineSettore BIO/05 - ZoologiaPharmaceutical Science<i>Staphylococcus aureus</i>Peptide<i>Paracentrotus lividus</i>Settore BIO/19 - Microbiologia Generalemedicine.disease_causebiofilmDrug DiscoveryPharmacology Toxicology and Pharmaceutics (miscellaneous)lcsh:QH301-705.5chemistry.chemical_classificationbiologyMicrobial Sensitivity TestChemistrymolecular dynamicBiological activityRecombinant ProteinAntimicrobialRecombinant ProteinsAnti-Bacterial AgentsBiochemistrySettore CHIM/03 - Chimica Generale E InorganicaStaphylococcus aureusPeptidePseudomonas aeruginosaStaphylococcus aureuParacentrotusAntibacterial activityAMP (antimicrobial peptides)Staphylococcus aureusSea UrchinAntimicrobial peptidesMicrobial Sensitivity TestsParacentrotus lividusArticle03 medical and health sciencesAnti-Bacterial AgentmedicineAnimalsAMP (antimicrobial peptides); Paracentrotus lividus; Pseudomonas aeruginosa; Staphylococcus aureus; biofilm; molecular dynamics; thymosinAnimalBiofilmthymosinbiology.organism_classificationmolecular dynamics<i>Pseudomonas aeruginosa</i>030104 developmental biologylcsh:Biology (General)Paracentrotus lividusBiofilmsSea UrchinsParacentrotuPeptidesParacentrotus lividuMarine Drugs
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Immunization with a Synthetic Human MUC1 Glycopeptide Vaccine against Tumor-Associated MUC1 Breaks Tolerance in Human MUC1 Transgenic Mice.

2017

Breaking tolerance is crucial for effective tumor immunotherapy. We showed that vaccines containing tumor-associated human MUC1 glycopeptides induce strong humoral antitumor responses in mice. The question remained whether such vaccines work in humans, in systems where huMUC1 is a self-antigen. To clarify the question, mice transgenic in expressing huMUC1, mimicking the self-tolerant environment, and wild-type mice were vaccinated with a synthetic vaccine. This vaccine comprised STn and Tn antigens bound to a MUC1 tandem repeat peptide coupled to tetanus toxoid. The vaccine induced strong immune responses in wild-type and huMUC1-transgenic mice without auto-aggressive side effects. All anti…

0301 basic medicineSynthetic vaccinemedicine.medical_treatmentBreast NeoplasmsMice TransgenicBiology01 natural sciencesBiochemistryCancer Vaccines03 medical and health sciencesImmune systemAntigenCancer immunotherapyDrug DiscoverymedicineTetanus ToxoidAnimalsHumansAntigens Tumor-Associated CarbohydrateGeneral Pharmacology Toxicology and PharmaceuticsPharmacologyVaccines Synthetic010405 organic chemistryTetanusOrganic ChemistryMucin-1ToxoidImmunotherapymedicine.diseaseVirologyPeptide Fragments0104 chemical sciencesMice Inbred C57BL030104 developmental biologyImmunizationImmunologyMCF-7 CellsMolecular MedicineFemaleImmunizationChemMedChem
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Validated HPLC-UV detection method for the simultaneous determination of ceftolozane and tazobactam in human plasma

2018

Aim: A simple, rapid, economical and sensitive HPLC-UV method was developed for the simultaneous quantification of ceftolozane and tazobactam in plasma samples. Methodology: After deproteinization followed by a liquid–liquid back-extraction, the compounds were separated on a C18 column (150 mm × 4.6 mm, 5 μm) with UV-visible detection at 220 nm. The mobile phase consisted of acetonitrile and potassium dihydrogenphosphate buffer at pH 3.0 (8:92, v/v), delivered isocratically at a flow rate of 1.0 ml/min and at a column oven temperature of 30°C. Cefepime was used as an internal standard. Results: Linearity was achieved in the concentration range of 0.50–100.00 μg/ml for ceftolozane and 0.25–…

0301 basic medicineTazobactam030106 microbiologyClinical BiochemistryPenicillanic Acid01 natural sciencesHigh-performance liquid chromatographyTazobactamAnalytical ChemistryPlasma03 medical and health sciencesmedicineHumansSample preparationGeneral Pharmacology Toxicology and PharmaceuticsChromatography High Pressure LiquidReproducibilityChromatographyPlasma samplesmedicine.diagnostic_testChemistry010401 analytical chemistryGeneral MedicineAnti-Bacterial AgentsCephalosporins0104 chemical sciencesMedical Laboratory TechnologyTherapeutic drug monitoringHuman plasmaCeftolozanemedicine.drugBioanalysis
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Effects of Pimozide Derivatives on pSTAT5 in K562 Cells

2017

STAT5 is a transcription factor, a member of the STAT family of signaling proteins. STAT5 is involved in many types of cancer, including chronic myelogenous leukemia (CML), in which this protein is found constitutively activated as a consequence of BCR-ABL expression. The neuroleptic drug pimozide was recently reported to act as an inhibitor of STAT5 phosphorylation and is capable of inducing apoptosis in CML cells in vitro. Our research group has synthesized simple derivatives of pimozide with cytotoxic activity and that are able to decrease the levels of phosphorylated STAT5. In this work we continued the search for novel STAT5 inhibitors, synthesizing compounds in which the benzoimidazol…

0301 basic medicineantiproliferationApoptosisPharmacologyBiochemistryAntineoplastic Agent0302 clinical medicinePimozidehemic and lymphatic diseasesDrug DiscoverySTAT5 Transcription FactorCytotoxic T cellPhosphorylationGeneral Pharmacology Toxicology and PharmaceuticsBCR-ABL-expressing leukemia; STAT5 inhibitors; antiproliferation; apoptosis; pimozideSTAT5Molecular StructurebiologyPimozidefood and beverages030220 oncology & carcinogenesisMolecular MedicinePhosphorylationHumanmedicine.drugAntineoplastic AgentsNOStructure-Activity Relationship03 medical and health sciencesK562 CellmedicineHumansTranscription factorCell ProliferationPharmacologyDose-Response Relationship DrugCell growthSTAT5 inhibitorsOrganic ChemistryApoptosiSTAT5 inhibitormedicine.disease030104 developmental biologyPharmacology Toxicology and Pharmaceutics (all)biology.proteinCancer researchBCR-ABL-expressing leukemiaDrug Screening Assays AntitumorK562 CellsK562 cellsChronic myelogenous leukemiaChemMedChem
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A new class of phenylhydrazinylidene derivatives as inhibitors of Staphylococcus aureus biofilm formation

2016

In the struggle against the emergence of the antibiotic resistance, new molecules targeting biofilm formation could be useful as adjuvant of conventional antibiotics. This study focused on a new class of 2-phenylhydrazinylidene derivatives as antivirulence agents. The compound 12e showed interesting activities against biofilm formation of all tested Staphylococcus aureus strains with IC50 ranging from 1.7 to 43 µM; compounds 12f and 13a resulted strong inhibitors of S. aureus ATCC 6538 and ATCC 29213 biofilm formation with IC50 of 0.9 and 0.8 µM, respectively. A preliminary study on the mechanism of action was carried on evaluating the inhibition of sortase A transpeptidase. Compound 12e re…

0301 basic medicinemedicine.drug_class030106 microbiologyAntibioticsBacterial adhesionAntibiofilm agentSettore BIO/19 - Microbiologia Generalemedicine.disease_causeMicrobiologyAntivirulence agent03 medical and health sciencesAntibiotic resistanceIn vivomedicineGeneral Pharmacology Toxicology and PharmaceuticsbiologyChemistrySortase AOrganic ChemistryBiofilmPhenylhydrazinylidene derivativebiochemical phenomena metabolism and nutritionbiology.organism_classificationSettore CHIM/08 - Chimica FarmaceuticaGalleria mellonellaSettore AGR/11 - Entomologia Generale E Applicata030104 developmental biologyMechanism of actionBiochemistryStaphylococcus aureusPharmacology Toxicology and Pharmaceutics (all)Sortase Amedicine.symptomMedicinal Chemistry Research
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Citations and metrics of journals discontinued from Scopus for publication concerns: the GhoS(t)copus Project

2020

Background: Scopus is a leading bibliometric database. It contains a large part of the articles cited in peer-reviewed publications. The journals included in Scopus are periodically re-evaluated to ensure they meet indexing criteria and some journals might be discontinued for 'publication concerns'. Previously published articles may remain indexed and can be cited. Their metrics have yet to be studied. This study aimed to evaluate the main features and metrics of journals discontinued from Scopus for publication concerns, before and after their discontinuation, and to determine the extent of predatory journals among the discontinued journals. Methods: We surveyed the list of discontinued jo…

0301 basic medicinemedicine.medical_specialtyGeneral Immunology and Microbiologymetricbusiness.industryScopusGeneral Medicinepredatory.General Biochemistry Genetics and Molecular BiologyDiscontinuation03 medical and health sciencesMisconduct030104 developmental biology0302 clinical medicinePublishingScopuFamily medicinejournalMedicineSubject areascitation countGeneral Pharmacology Toxicology and Pharmaceuticsbusiness030217 neurology & neurosurgeryindexingF1000Research
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Impact of freeze-thaw cytoablation on aqueous outflow patterns in ex vivo anterior chamber perfusion cultures and whole eyes

2022

Background: Porcine eyes have been widely used as ex vivo models in glaucoma research, as they share similar features with human eyes. Freeze-thawing is a non-invasive technique that has been used to obliterate living cells in anterior segment ex vivo cultures, to prepare them for further research such as cellular repopulation. This technique has previously been shown to reduce the intraocular pressure (IOP) in porcine eyes. The aim of this study was to investigate whether freeze-thaw cytoablation causes corresponding canalogram outflow changes in perfused anterior segment cultures (AFT) and whole porcine eyes (WFT). We hypothesized that the known IOP drop in AFT after trabecular meshwork a…

0301 basic medicinemedicine.medical_specialtyIntraocular pressuregenetic structuresvirusesGlaucomaTexas RedGeneral Biochemistry Genetics and Molecular Biology03 medical and health scienceschemistry.chemical_compound0302 clinical medicineOphthalmologymedicineFluoresceinGeneral Pharmacology Toxicology and PharmaceuticsGeneral Immunology and MicrobiologyChemistryvirus diseasesGeneral Medicinebiochemical phenomena metabolism and nutritionmedicine.diseasedigestive system diseases030104 developmental biologymedicine.anatomical_structure030221 ophthalmology & optometryOutflowTrabecular meshworksense organsPerfusionEx vivoF1000Research
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Identification of metastasis-related genes by genomic and transcriptomic studies in murine melanoma.

2021

Abstract Aims We systematically characterized metastatic murine B16-F10 melanoma, a sub-line derived from murine melanoma B16-F1 cells. Materials and methods RNA-sequencing and network analyses (Ingenuity Pathway Analysis) were performed to identify novel potential metastasis mechanisms. Chromosomal aberrations were identified by multicolor fluorescence in situ hybridization (mFISH) using all 21 murine whole chromosome painting probes. Key findings Numerous genes were overexpressed in B16-F10 cells, some of which have been already described as being metastasis-linked. Nr5a1/sf1, a known prognostic marker for adrenal tumors, was 177-fold upregulated in B16-F10 cells compared to B16-F1 cells.…

0301 basic medicinemedicine.medical_specialtyMelanoma ExperimentalBiologymedicine.disease_cause030226 pharmacology & pharmacyGeneral Biochemistry Genetics and Molecular BiologyMetastasisTranscriptome03 medical and health sciencesMice0302 clinical medicineCell Line TumormedicineAnimalsGeneral Pharmacology Toxicology and PharmaceuticsNeoplasm MetastasisneoplasmsMelanomaIn Situ Hybridization FluorescenceGenomemedicine.diagnostic_testSequence Analysis RNAMelanomaCytogeneticsCancerGeneral MedicineGenomicsmedicine.diseasecarcinogenesis ; chromosomal aberrations ; cytogenetics ; melanoma ; rna-sequencing ; transcriptomicsSquamous carcinomaMice Inbred C57BL030104 developmental biologyCancer researchCarcinogenesisTranscriptomeFluorescence in situ hybridizationLife sciences
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