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showing 10 items of 626 documents

Selectivity of pharmacological tools: implications for use in cell physiology. A Review in the Theme: Cell Signaling: Proteins, Pathways and Mechanis…

2014

Pharmacological inhibitors are frequently used to identify the receptors, receptor subtypes, and associated signaling pathways involved in physiological cell responses. Based on the effects of such inhibitors conclusions are drawn about the involvement of their assumed target or lack thereof. While such inhibitors can be useful tools for a better physiological understanding, their uncritical use can lead to incorrect conclusions. This article reviews the concept of inhibitor selectivity and its implication for cell physiology. Specifically, we discuss the implications of using inhibitor vs. activator approaches, issues of direct vs. indirect pathway modulation, implications of inverse agoni…

Cell physiologyCell signalingPhysiologyAdrenergic beta-AntagonistsCellAllosteric regulationImidazolesCell CommunicationCell BiologyAdrenergic beta-AgonistsBiologyPharmacologyIndirect pathway of movementCell Physiological PhenomenaReceptors G-Protein-CoupledFunctional antagonismmedicine.anatomical_structuremedicineAnimalsHumansSignal transductionReceptorNeuroscienceProtein BindingSignal TransductionAmerican Journal of Physiology-Cell Physiology
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Bis-cyclohexyl-crown-ethers as allosteric carriers

1992

Abstract Several bis-cyclohexyl-crown-ethers have been synthesized and used as carriers for alkaline cations. These compounds should all show negative allosteric cooperativity, but only 1 exhibits an odd cation transport behavior across the liquid organic membranes.

MembraneChemistryBiological modelingOrganic ChemistryDrug DiscoveryAllosteric regulationCrown (botany)Polymer chemistryIonophoreOrganic chemistryCooperativityBiochemistryCation transportTetrahedron
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El modulador alostérico negativo de los mGluR5, MPEP, potencia la reinstauración de la preferencia condicionada inducida con priming de cocaína

2019

Cocaine addiction is a chronic disorder with high relapse rates; therefore, understanding the neuronal mechanisms underlying drug-seeking during relapse is a priority to develop targeted pharmacotherapy. The metabotropic glutamate receptor 5 (mGluR5) seems to be involved in the reinstatement induced by cocaine-associated cues. The main objective of the study was to evaluate the efficacy of MPEP, a negative allosteric modulator of mGluR5, in attenuating or potentiating the reinstatement induced by priming doses of cocaine in the CPP paradigm, ultimately to further knowledge regarding the role of the mGluR5 in relapse into cocaine abuse. OF1 mice (48 female and 48 male) were conditioned in th…

Allosteric modulatorMetabotropic glutamate receptor 5business.industryAddictionmedia_common.quotation_subjectMedicine (miscellaneous)Extinction (psychology)PharmacologyChronic disordersPsychiatry and Mental healthnervous systemmental disordersMedicinebusinessPriming (psychology)Cocaine abusemedia_commonAdicciones
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Helminth parasites in faecal samples from the endangered Iberian lynx (Lynx pardinus).

2011

The Iberian lynx is the most endangered felid in the world. Enteropathogens may threaten its survival, and therefore we analysed faecal samples from 66 different individuals (37 males and 29 females), the largest population representation studied to date. The samples were obtained from November 2005 to October 2008 in the two areas where the Iberian lynx survives: Sierra Morena and Donana (Andalusia, southern Spain). A total of 56.1% samples were parasitized with at least 6 species of helminths, including two cestodes (Hymenolepis spp. and Taenia spp.) and four Nematodes (Ancylostoma spp., Toxocara spp., Toxascaris leonina, and Capillaria sp.). In this work, the presence of Hymenolepis is r…

MaleVeterinary medicineeducation.field_of_studyToxascaris leoninaGeneral VeterinarybiologyCapillariaPopulationEndangered SpeciesEndangered speciesGeneral Medicinebiology.organism_classificationFecesAncylostomaSpainLynxTaeniaHelminthsAnimalsParasitologyFemaleHelminthiasis AnimalHymenolepis (tapeworm)educationVeterinary parasitology
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Yritysten tilinpäätöstietojen toimipaikkaistamisen ongelma : yleistetyn regressioestimoinnin sovellus rekisteritutkimuksessa

2003

yleistetty regressioestimointitoimipaikatregressioanalyysilisäinformaatiotilastomenetelmättoimipaikkaistaminenrekisteritotantarekisteritutkimusyritystutkimusimputointijalostusarvoestimointi
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Multi or Single-Kinase Inhibitors to Counteract Drug Resistance in Cancer: What is New?

2023

The concept of protein kinase inhibition starts from the groundbreaking research on the role of these proteins in the regulation of fundamental processes, including proliferation, cell cycle, apoptosis, metabolism, and inflammation. Kinase genetic mutations, as well as overexpression and dysregulation, can contribute to the development of several diseases, including neoplasms, leading to relapses and resistance to standard drug chemotherapy [1-3].

PharmacologySmall molecules kinase inhibitorspolypharmacologycovalent kinase inhibitorsallosteric inhibitorsDrug DiscoveryOrganic ChemistryMolecular Medicineanticancer drug combinationsBiochemistrykinase genetic aberrationSettore CHIM/08 - Chimica Farmaceutica
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Étude paléoenvironnementale et paléoclimatique multiproxiesdes bassins fini-carbonifères à permiens du N-E duMassif central.

2021

National audience; Les bassins intracontinentaux fini-carbonifères à permiens d'Autun et de Decize-LaMachine (NE du Massif central) ont fait l'objet d'un travail de thèse s'appuyant sur denombreuses méthodes d'analyse appliquées à haute résolution sur des données deforages et quelques coupes.Les interprétations des résultats sédimentologiques (faciès, diagraphies, sismique), destratigraphie séquentielle, de géochimie et isotopie organique (carbone et azote) et deminéralogie ont permis de reconstituer de la manière la plus précise possible l'évolutiondes environnements sédimentaires de ces bassins dans l'espace et au cours du temps.Il en ressort que les deux bassins étudiés dominés par des d…

cyclostratigraphiecontinental[SDU.STU.GC]Sciences of the Universe [physics]/Earth Sciences/Geochemistry[SDU.STU.ST]Sciences of the Universe [physics]/Earth Sciences/Stratigraphygéochimie[SDU.STU.GC] Sciences of the Universe [physics]/Earth Sciences/Geochemistry[SDU.STU.ST] Sciences of the Universe [physics]/Earth Sciences/StratigraphyCarbonifèreargilesPermien
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Morphological changes in adherent cells induced by Clostridium difficile toxins.

1991

Mice Inbred BALB CClostridioides difficileCytotoxinsMacrophagesBacterial ToxinsClostridium difficileBiologyIn Vitro TechniquesBiochemistryMicrobiologyEnterotoxinsMiceMicroscopy ElectronBacterial ProteinsCell AdhesionAnimalsBiochemical Society transactions
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Preconcentration and speciation analysis of mercury : 3D printed metal scavenger-based solid-phase extraction followed by analysis with inductively c…

2021

A selective method for preconcentration and determination of methylmercury (MeHg) and inorganic mercury (iHg) in natural water samples at the ng L−1 level has been developed. The method involves adsorption of Hg species into a 3D printed metal scavenger and sequential elution with acidic thiourea solutions before ICP-MS determination. Experimental parameters affecting the preconcentration of MeHg and iHg such as the sample matrix, effect of the flow rate on adsorption, eluent composition, and elution mode have been studied in detail. The obtained method detection limits, considering the preconcentration factors of 42 and 93, were found to be 0.05 ng L−1 and 0.08 ng L−1 for MeHg and iHg, res…

massaspektrometriamercurySolid Phase ExtractionelohopeaMercury3D printinganalyyttinen kemiaMethylmercury CompoundsvedenlaatuympäristökemiaMass SpectrometryAnalytical ChemistryspeciationInductively coupled plasma mass spectrometrysuodattimetpitoisuusPrinting Three-Dimensionalpreconcentration3D-tulostusnatural waterympäristömyrkytbiosaatavuus
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Global, Regional, and National Cancer Incidence, Mortality, Years of Life Lost, Years Lived With Disability, and Disability-Adjusted Life-years for 3…

2017

Importance: Cancer is the second leading cause of death worldwide. Current estimates on the burden of cancer are needed for cancer control planning.Objective: To estimate mortality, incidence, years lived with disability (YLDs), years of life lost (YLLs), and disability-adjusted life-years (DALYs) for 32 cancers in 195 countries and territories from 1990 to 2015.Evidence Review: Cancer mortality was estimated using vital registration system data, cancer registry incidence data (transformed to mortality estimates using separately estimated mortality to incidence [MI] ratios), and verbal autopsy data. Cancer incidence was calculated by dividing mortality estimates through the modeled MI ratio…

0301 basic medicineGerontologyCancer ResearchPopulationArticle03 medical and health sciences0302 clinical medicineBreast cancerGlobal healthcancerMedicineDisability-adjusted life yeareducationDisease burdeneducation.field_of_studyestimate mortalityCancer preventioncancer preventionbusiness.industryMortality rate1. No povertymedicine.disease3. Good health030104 developmental biologyYears of potential life lostOncology030220 oncology & carcinogenesisbusinessearly diagnosisDemography
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