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showing 10 items of 19256 documents

The Anemonia viridis Venom: Coupling Biochemical Purification and RNA-Seq for Translational Research

2018

Blue biotechnologies implement marine bio-resources for addressing practical concerns. The isolation of biologically active molecules from marine animals is one of the main ways this field develops. Strikingly, cnidaria are considered as sustainable resources for this purpose, as they possess unique cells for attack and protection, producing an articulated cocktail of bioactive substances. The Mediterranean sea anemone Anemonia viridis has been studied extensively for years. In this short review, we summarize advances in bioprospecting of the A. viridis toxin arsenal. A. viridis RNA datasets and toxin data mining approaches are briefly described. Analysis reveals the major pool of neurotoxi…

0301 basic medicineNeurotoxinsPharmaceutical ScienceRNA-SeqVenomReviewComputational biologyCnidarian VenomAnemoniaTranslational Research Biomedicaltranscriptomics03 medical and health sciencescomputational biologyCnidarian VenomsDrug DiscoveryAnimalsData MiningMarine ToxinTranslational Medical Researchlcsh:QH301-705.5Pharmacology Toxicology and Pharmaceutics (miscellaneous)Sea AnemoneBioprospectingbiologyAnimalSequence Analysis RNASustainable resourcesDrug Discovery3003 Pharmaceutical ScienceRNAAnemonebio-prospectingbiology.organism_classificationSea Anemones030104 developmental biologyTranscriptomiclcsh:Biology (General)RNAMarine ToxinsNeurotoxinMarine toxinMarine Drugs
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Identification of noncovalent proteasome inhibitors with high selectivity for chymotrypsin-like activity by a multistep structure-based virtual scree…

2016

Noncovalent proteasome inhibitors introduce an alternative mechanism of inhibition to that of covalent inhibitors, e.g. carfilzomib, used in cancer therapy. A multistep hierarchical structure-based virtual screening (SBVS) of the 65,375 NCI lead-like compound library led to the identification of two compounds (9 and 28) which noncovalently inhibited the chymotrypsin-like (ChT-L) activity (Ki = 2.18 and 2.12 μM, respectively) with little or no effects on the other two major proteasome proteolytic activities, trypsin-like (T-L) and post-glutamyl peptide hydrolase (PGPH) activities. A subsequent hierarchical similarity search over the full NCI database with the most active tripeptide-based inh…

0301 basic medicineNon-covalentVirtual screeningProteasome Endopeptidase ComplexStereochemistryProtein ConformationProteolysisDrug Evaluation PreclinicalTripeptideSubstrate Specificity03 medical and health scienceschemistry.chemical_compoundStructure-Activity RelationshipUser-Computer Interface0302 clinical medicineProtein structureCell Line TumorDrug DiscoverymedicineStructure–activity relationshipChymotrypsinHumansProteasome inhibitorCell ProliferationPharmacologyVirtual screeningmedicine.diagnostic_testOrganic ChemistryGeneral MedicineCarfilzomibPeptide scaffoldMolecular Docking SimulationProteasome inhibitors; Non-covalent; Peptide scaffold; Docking studies; Virtual screening030104 developmental biologyProteasomechemistryBiochemistryDocking (molecular)030220 oncology & carcinogenesisDocking studieProteolysisProteasome InhibitorsEuropean journal of medicinal chemistry
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Exploring the readthrough of nonsense mutations by non-acidic Ataluren analogues selected by ligand-based virtual screening

2016

Abstract Ataluren, also known as PTC124, is a 5-(fluorophenyl)-1,2,4-oxadiazolyl-benzoic acid suggested to suppress nonsense mutations by readthrough of premature stop codons in the mRNA. Potential interaction of PTC124 with mRNA has been recently studied by molecular dynamics simulations highlighting the importance of H-bonding and stacking π−π interactions. A series of non-acidic analogues of PTC124 were selected from a large database via a ligand-based virtual screening approach. Eight of them were synthesized and tested for their readthrough activity using the Fluc reporter harboring the UGA premature stop codon. The most active compound was further tested for suppression of the UGA non…

0301 basic medicineNonsense mutationDrug Evaluation PreclinicalMolecular ConformationCystic Fibrosis Transmembrane Conductance RegulatorMolecular Dynamics SimulationOxadiazolemedicine.disease_causeCftr geneCFTR gene03 medical and health scienceschemistry.chemical_compoundDrug DiscoverymedicineHumansRNA MessengerPharmacologyGeneticsOxadiazolesMessenger RNAVirtual screeningMutationNonsense mutationChemistryDrug Discovery3003 Pharmaceutical ScienceOrganic ChemistryGeneral MedicineLigand (biochemistry)PTCs readthroughMolecular biologyStop codonAtaluren030104 developmental biologyCodon NonsenseCystic fibrosiHeLa CellsEuropean Journal of Medicinal Chemistry
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Archaeology and ichnology at Gombore II-2, Melka Kunture, Ethiopia: everyday life of a mixed age hominin group 700,000 years ago

2018

AbstractWe report the occurrence at 0.7 million years (Ma) of an ichnological assemblage at Gombore II-2, which is one of several archaeological sites at Melka Kunture in the upper Awash Valley of Ethiopia, 2000 m asl. Adults and children potentially as young as 12 months old left tracks in a silty substrate on the shore of a body of water where ungulates, as well as other mammals and birds, congregated. Furthermore, the same layers contain a rich archaeological and palaeontological record, confirming that knapping was taking place in situ and that stone tools were used for butchering hippo carcasses at the site. The site gives direct information on hominin landscape use at 0.7 Ma and may p…

0301 basic medicineOld Left010506 paleontologySciencegrowthtanzanialengthEnvironment01 natural sciencesArticlemultidisciplinary; growth; foot; children; site; footprints; tanzania; height; length; tracks; kenya; ethiopia03 medical and health sciencesIchnologychildrenGroup (stratigraphy)siteAssemblage (archaeology)AnimalsHumansEveryday lifeHistory Ancient0105 earth and related environmental sciencesShoregeography.geographical_feature_categoryKnappingFossilsQRPaleontologyHominidae15. Life on landfootprintstracksArchaeology030104 developmental biologyGeographykenyaArchaeologyfootMedicineethiopiamultidisciplinaryheight
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Identification of accessory olfactory system and medial amygdala in the zebrafish

2017

AbstractZebrafish larvae imprint on visual and olfactory cues of their kin on day 5 and 6 postfertilization, respectively. Only imprinted (but not non-imprinted) larvae show strongly activated crypt (and some microvillous) cells demonstrated by pERK levels after subsequent exposure to kin odor. Here, we investigate the olfactory bulb of zebrafish larvae for activated neurons located at the sole glomerulus mdG2 which receives crypt cell input. Imprinted larvae show a significantly increased activation of olfactory bulb cells compared to non-imprinted larvae after exposure to kin odor. Surprisingly, pERK activated Orthopedia-positive cell numbers in the intermediate ventral telencephalic nucl…

0301 basic medicineOlfactory systemanimal structuresGene ExpressionSensory systemImprinting PsychologicalAmygdalaArticleOlfactory Receptor Neurons03 medical and health sciences0302 clinical medicinemedicineAnimalsPhosphorylationZebrafishZebrafishFluorescent DyesGlomerulus (olfaction)Microscopy ConfocalMitogen-Activated Protein Kinase 3MultidisciplinarybiologyfungiOlfactory PathwaysCarbocyaninesZebrafish ProteinsAmygdalabiology.organism_classificationOlfactory BulbOlfactory bulbCell biologySmell030104 developmental biologymedicine.anatomical_structureOdorHypothalamusLarvaOdorants030217 neurology & neurosurgeryTranscription FactorsScientific Reports
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High Fructose Diet inducing diabetes rapidly impacts olfactory epithelium and behavior in mice

2016

AbstractType 2 Diabetes (T2D), a major public health issue reaching worldwide epidemic, has been correlated with lower olfactory abilities in humans. As olfaction represents a major component of feeding behavior, its alteration may have drastic consequences on feeding behaviors that may in turn aggravates T2D. In order to decipher the impact of T2D on the olfactory epithelium, we fed mice with a high fructose diet (HFruD) inducing early diabetic state in 4 to 8 weeks. After only 4 weeks of this diet, mice exhibited a dramatic decrease in olfactory behavioral capacities. Consistently, this decline in olfactory behavior was correlated to decreased electrophysiological responses of olfactory n…

0301 basic medicineOlfactory systemmedicine.medical_specialtyolfaction;fructose;diabete;physiology;behavior;mouseinjuryPopulationType 2 diabetesOlfactionBiologysystemleptinArticleinsulin-resistance03 medical and health sciencescardiac-hypertrophyneuropeptide-y0302 clinical medicineInsulin resistance[ SDV.MHEP ] Life Sciences [q-bio]/Human health and pathologyInternal medicineDiabetes mellitusmedicineFood and Nutritioneducationmarker proteineducation.field_of_studyMultidisciplinaryLeptinNeurosciencesapoptosismedicine.disease3. Good health030104 developmental biologyEndocrinologymedicine.anatomical_structuresensory neuronsNeurons and CognitionAlimentation et NutritionOlfactory epithelium030217 neurology & neurosurgery[SDV.MHEP]Life Sciences [q-bio]/Human health and pathologymellitus
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Scabrous overexpression in the eye affects R3/R4 cell fate specification and inhibits notch signaling

2015

Background Planar cell polarity (PCP) in the Drosophila eye is generated when immature ommatidial preclusters acquire opposite chirality in the dorsal and ventral halves of the eye imaginal disc and rotate 90 ° toward the equator. The scabrous (sca) gene is involved in R8 differentiation and in the correct spacing of ommatidial clusters in eye imaginal discs, but it was also suggested to be required during ommatidial rotation. However, no clear relationships between sca and other genes involved in the process were established. Results To explore the role of Sca in PCP establishment, we performed an RNAi-based modifier genetic screen using the rough eye phenotype of sca-overexpressing flies.…

0301 basic medicineOmmatidial rotationbiologyCellular differentiationNotch signaling pathwayCell fate determinationbiology.organism_classificationCell biology03 medical and health sciencesImaginal disc030104 developmental biologyDrosophila melanogasterDrosophila ProteinDevelopmental BiologyGenetic screenDevelopmental Dynamics
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Prognostic clinical factors in patients affected by non-small-cell lung cancer receiving Nivolumab

2020

Background: Immune-checkpoint inhibitors have radically changed the treatment landscape of Non-Small-Cell Lung Cancer (NSCLC). It is still unclear whether specific clinical characteristics might identify those patients benefiting from immunotherapy more than others. The aim of this study was to identify clinical characteristics associated with disease-specific survival (DSS), time-to-treatment failure (TTF), objective responses (OR) and progressive disease (PD) in NSCLC patients treated with Nivolumab. Methods: This was a multicenter retrospective study conducted on 294 patients treated with Nivolumab for advanced NSCLC. Results: Of the more than 50 variables analyzed, five showed a signifi…

0301 basic medicineOncologyAdultMalemedicine.medical_specialtyLung Neoplasmsmedicine.medical_treatmentClinical BiochemistryKaplan-Meier EstimateDisease-Free SurvivalDrug Administration ScheduleNO03 medical and health sciences0302 clinical medicineInternal medicineCarcinoma Non-Small-Cell LungDrug DiscoverymedicineMalignant pleural effusionHumansimmunotherapy; malignant pleural effusion; nivolumab; non-small-cell lung cancerIn patientmalignant pleural effusionLung cancerImmune Checkpoint InhibitorsRetrospective StudiesPharmacologynivolumabbusiness.industryBrain NeoplasmsLiver NeoplasmsImmunotherapymedicine.diseasePrognosisPleural Effusion Malignantrespiratory tract diseases030104 developmental biologyTreatment Outcomenon-small-cell lung cancer030220 oncology & carcinogenesisFemalesense organsNon small cellimmunotherapyNivolumabbusiness
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The Emerging Therapeutic Landscape of ALK Inhibitors in Non-Small Cell Lung Cancer.

2020

The treatment of metastatic non-small cell lung cancer (NSCLC) has undergone a paradigm shift over the last decade. Better molecular characterization of the disease has led to the rapid improvement of personalized medicine and the prompt delivery of targeted therapies to patients with NSCLC. The discovery of the EML4-ALK fusion gene in a limited subset of patients affected by NSCLC and the subsequent clinical development of crizotinib in 2011 has been an impressive milestone in lung cancer research. Unfortunately, acquired resistances regularly develop, hence disease progression occurs. Afterward, modern tyrosine kinase inhibitors (TKIs), such as ceritinib, alectinib, brigatinib, and lorlat…

0301 basic medicineOncologyAlectinibALK inhibitorsmedicine.medical_specialtybrigatinibBrigatinibmedicine.medical_treatmentPharmaceutical Sciencenon-small cell lung cancer (NSCLC)lcsh:Medicinelcsh:RS1-441ReviewALK inhibitorTargeted therapylcsh:Pharmacy and materia medica03 medical and health sciences0302 clinical medicinelorlatinibInternal medicineDrug DiscoveryMedicineAnaplastic lymphoma kinaseceritinibalectinibensartinibcrizotinibCrizotinibCeritinibbusiness.industrylcsh:Rmedicine.diseaseLorlatinibrespiratory tract diseasesnon-small cell lung cancer (NSCLC)030104 developmental biologytyrosine kinase inhibitors (TKIs)030220 oncology & carcinogenesisMolecular Medicinebusinessmedicine.drugPharmaceuticals (Basel, Switzerland)
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Efficacy and safety of everolimus in extrapancreatic neuroendocrine tumor: a comprehensive review of literature

2016

BACKGROUND Everolimus, an oral mTOR (mammalian target of rapamycin) inhibitor, is currently approved for the treatment of progressive pancreatic neuroendocrine tumors (NETs). Although promising, only scattered data, often from nondedicated studies, are available for extrapancreatic NETs. PATIENTS AND METHODS A systematic review of the published data was performed concerning the use of everolimus in extrapancreatic NET, with the aim of summarizing the current knowledge on its efficacy and tolerability. Moreover, the usefulness of everolimus was evaluated according to the different sites of the primary. RESULTS The present study included 22 different publications, including 874 patients and 4…

0301 basic medicineOncologyCancer ResearchLung NeoplasmsAdrenal Gland NeoplasmsColorectal NeoplasmNeuroendocrine tumorsSettore MED/13 - EndocrinologiaAntineoplastic Agent0302 clinical medicineEndocrinologyNeuroendocrine tumors; everolimus; extrapancreatic; efficacy; safetyProspective cohort studyNeuroendocrine TumorsEverolimuOncologyTolerability030220 oncology & carcinogenesisIleal NeoplasmSafetyColorectal Neoplasmsmedicine.drugHumanmedicine.medical_specialtyEfficacyAntineoplastic AgentsPheochromocytomaExtrapancreatic neuroendocrine tumorDisease-Free Survival03 medical and health sciencesNeuroendocrine tumorStomach NeoplasmsStomach NeoplasmInternal medicinemedicineHumansEverolimusThyroid NeoplasmsAdverse effectEverolimusbusiness.industryRetrospective cohort studymedicine.diseaseDiscontinuationCarcinoma NeuroendocrineClinical trialIleal NeoplasmsAdrenal Gland NeoplasmLung Neoplasm030104 developmental biologyEndocrinologybusiness
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