Search results for "Screen"

showing 10 items of 1374 documents

New 3-Aryl-2-(2-Thienyl)acrylonitriles with High Activity against Hepatoma Cells

2021

New 2-(thien-2-yl)-acrylonitriles with putative kinase inhibitory activity were prepared and tested for their antineoplastic efficacy in hepatoma models. Four out of the 14 derivatives were shown to inhibit hepatoma cell proliferation at (sub-)micromolar concentrations with IC50 values below that of the clinically relevant multikinase inhibitor sorafenib, which served as a reference. Colony formation assays as well as primary in vivo examinations of hepatoma tumors grown on the chorioallantoic membrane of fertilized chicken eggs (CAM assay) confirmed the excellent antineoplastic efficacy of the new derivatives. Their mode of action included an induction of apoptotic capsase-3 activity, whil…

0301 basic medicinelcsh:Chemistry0302 clinical medicinelcsh:QH301-705.5SpectroscopyMolecular StructureKinaseChemistryLiver NeoplasmsGeneral MedicineHep G2 CellshepatomaComputer Science ApplicationsCAM assayMolecular Docking SimulationChorioallantoic membraneBiochemistry030220 oncology & carcinogenesistyrphostinTyrosine kinasemedicine.drugSorafenibCarcinoma HepatocellularthiopheneThiophenesCatalysisArticleInorganic ChemistryVEGFR inhibition03 medical and health sciencesStructure-Activity RelationshipIn vivomedicineHumansPhysical and Theoretical ChemistryMode of actionMolecular BiologyProtein Kinase InhibitorsCell ProliferationAcrylonitrileDose-Response Relationship DrugOrganic Chemistrymolecular dockingVascular Endothelial Growth Factor Receptor-2anticancer drugs030104 developmental biologylcsh:Biology (General)lcsh:QD1-999ApoptosisDocking (molecular)Drug Screening Assays AntitumorInternational Journal of Molecular Sciences
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Molecular Signatures Associated with Treatment of Triple-Negative MDA-MB231 Breast Cancer Cells with Histone Deacetylase Inhibitors JAHA and SAHA

2017

Jay Amin Hydroxamic Acid (JAHA; N8-ferrocenylN1-hydroxy-octanediamide) is a ferrocene-containing analogue of the histone deacetylase inhibitor (HDACi) suberoylanilide hydroxamic acid (SAHA). JAHA’s cytotoxic activity on MDA-MB231 triple negative breast cancer (TNBC) cells at 72 h has been previously demonstrated with an IC50 of 8.45 M. JAHA’s lethal effect was found linked to perturbations of cell cycle, mitochondrial activity, signal transduction and autophagy mechanisms. In order to glean novel insights on how MDA-MB231 breast cancer cells respond to the cytotoxic effect induced by JAHA, and to compare the biological effect with the related compound SAHA, we have employed a combination of…

0301 basic medicinemedicine.drug_classAntineoplastic AgentsTriple Negative Breast NeoplasmsBiologyHydroxamic AcidsToxicologyStructure-Activity Relationship03 medical and health sciences0302 clinical medicineCell Line TumormedicineHumansCytotoxic T cellFerrous CompoundsSettore BIO/06 - Anatomia Comparata E Citologiaskin and connective tissue diseasesVorinostatTriple-negative breast cancerVorinostatDose-Response Relationship DrugHistone deacetylase inhibitorComputational BiologyGeneral MedicineTriple Negative Breast NeoplasmsCell cycleHistone Deacetylase InhibitorsSettore BIO/18 - Genetica030104 developmental biologyBiochemistryCell culture030220 oncology & carcinogenesisCancer researchHistone deacetylaseJAHA Comet assay MDA-MB231 Histone Deacetylase InhibitorsDrug Screening Assays Antitumormedicine.drug
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Prospecting for cytotoxic and antiprotozoal 4-aryl-4H-chromenes and 10-aryldihydropyrano[2,3-f]chromenes.

2018

Different studies reported that genetic predisposition or metabolic dysfunction are the risk factors for cancer. Infectious parasitic diseases were listed among factors that predispose to cancer. Because of the resemblance between the life cycle of cancer cells and some parasites, this study aimed to prepare pyran derivatives with cytotoxic and antiprotozoal potencies. Therefore, 7 chromenes, 10 pyranocoumarins, and an unexpected intermediate were obtained from a multi-reagent one-pot reaction. These compounds were evaluated for their cytotoxicity on sensitive and resistant leukemia cancer cells lines and against two protozoan parasites, namely Trypanosoma cruzi and Leishmania amazonensis a…

0301 basic medicinemedicine.drug_classAntiparasiticTHP-1 CellsTrypanosoma cruziAntiprotozoal AgentsPharmaceutical ScienceAntineoplastic AgentsApoptosisPharmacology03 medical and health sciencesStructure-Activity RelationshipParasitic Sensitivity TestsDrug DiscoverymedicineTumor Cells CulturedCytotoxic T cellHumansBenzopyransTrypanosoma cruziCytotoxicityAmastigoteCell ProliferationLeishmaniabiologyDose-Response Relationship DrugMolecular StructureChemistryCancerCell Cycle Checkpointsbiology.organism_classificationmedicine.disease030104 developmental biologyCancer cellAntiprotozoalDrug Screening Assays AntitumorArchiv der Pharmazie
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Cervical Cancer Screening: Comparison of Conventional Pap Smear Test, Liquid-Based Cytology, and Human Papillomavirus Testing as Stand-alone or Cotes…

2020

Abstract Background: Some countries have implemented stand-alone human papillomavirus (HPV) testing while others consider cotesting for cervical cancer screening. We compared both strategies within a population-based study. Methods: The MARZY cohort study was conducted in Germany. Randomly selected women from population registries aged ≥30 years (n = 5,275) were invited to screening with Pap smear, liquid-based cytology (LBC, ThinPrep), and HPV testing (Hybrid Capture2, HC2). Screen-positive participants [ASC-US+ or high-risk HC2 (hrHC2)] and a random 5% sample of screen-negatives were referred to colposcopy. Post hoc HPV genotyping was conducted by GP5+/6+ PCR-EIA with reverse line blottin…

0301 basic medicinemedicine.medical_specialtyEpidemiologyPopulationUterine Cervical NeoplasmsAlphapapillomavirusCervical cancer screeningSensitivity and SpecificityCohort Studies03 medical and health sciences0302 clinical medicinePregnancyCytologymedicineHumanseducationPapillomaviridaeEarly Detection of CancerVaginal SmearsColposcopyeducation.field_of_studymedicine.diagnostic_testbusiness.industryObstetricsPapillomavirus InfectionsConfidence interval030104 developmental biologyOncologyColposcopy030220 oncology & carcinogenesisVerification biasLiquid-based cytologyFemalebusinessPapanicolaou TestCohort studyCancer Epidemiology, Biomarkers & Prevention
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International working group identifies need for newborn screening for mucopolysaccharidosis type I but states that existing hurdles must be overcome

2018

Abstract Aim Mucopolysaccharidosis type I is a lysosomal storage disorder that can result in significant disease burden, disability and premature death, if left untreated. The aim of this review was to elaborate on the diagnosis of mucopolysaccharidosis type I and the pros and cons of newborn screening. Methods An international working group was established to discuss ways to improve the early diagnosis of mucopolysaccharidosis type I. It consisted of 13 experts in paediatrics, rare diseases and inherited metabolic diseases from Europe and the Middle East. Results It is becoming increasingly clearer that the delay between symptom onset and clinical diagnosis is considerable for mucopolysacc…

0301 basic medicinemedicine.medical_specialtyHaematopoietic stem cell transplantLysosomal storage disorderMucopolysaccharidosis ILysosomal storage disordersReview ArticleDisease03 medical and health sciencesMucopolysaccharidosis type INeonatal Screening0302 clinical medicinemedicineHumansLaronidasePediatrics Perinatology and Child HealthIntensive care medicineReview ArticlesDisease burdenNewborn screeningbusiness.industryMucopolysaccharidosis type IInfant NewbornGeneral MedicineEnzyme replacement therapyInternational working group030104 developmental biologyEnzyme replacement therapyClinical diagnosisPediatrics Perinatology and Child Healthbusiness030217 neurology & neurosurgeryActa Paediatrica
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Transient elastography for screening of liver fibrosis: cost-effectiveness analysis from six prospective cohorts in Europe and Asia

2019

Background & Aims: Non-alcoholic fatty liver disease and alcohol-related liver disease pose an important challenge to current clinical healthcare pathways because of the large number of at-risk patients. Therefore, we aimed to explore the cost-effectiveness of transient elastography (TE) as a screening method to detect liver fibrosis in a primary care pathway. Methods: Cost-effectiveness analysis was performed using real-life individual patient data from 6 independent prospective cohorts (5 from Europe and 1 from Asia). A diagnostic algorithm with conditional inference trees was developed to explore the relationships between liver stiffness, socio-demographics, comorbidities, and hepati…

0301 basic medicinemedicine.medical_specialtyTransient elastographyPopulationLiver fibrosisDisease03 medical and health sciencesLiver disease0302 clinical medicineFibrosisInternal medicinemedicineeducationeducation.field_of_studyAlcohol-related liver diseaseHepatologybusiness.industryFatty liverCost-effectiveness analysismedicine.disease3. Good health030104 developmental biologyStratified screening030211 gastroenterology & hepatologyTransient elastographybusinessHepatic fibrosisNon-alcoholic fatty liver disease
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Large-scale screening of lipase acid deficiency in at risk population

2021

International audience; BACKGROUND: Lysosomal acid lipase deficiency (LALD, OMIM#278000) is a rare lysosomal disorder with an autosomal recessive inheritance. The main clinical manifestations are related to a progressive accumulation of cholesteryl esters, triglycerides or both within the lysosome in different organs such as the liver, spleen, and cardiovascular system. A wide range of clinical severity is associated with LALD including a severe very rare antenatal/neonatal/infantile phenotype named Wolman disease and a late-onset form named cholesteryl ester storage disease (CESD). METHODS: This study aimed to investigate a cohort of at-risk patients (4174) presenting with clinical or biol…

0301 basic medicinemedicine.medical_specialty[SDV]Life Sciences [q-bio]Clinical BiochemistryAcid lipase deficiencyDBSSpleenDried blood spotLysosomal acid lipase deficiencyBiochemistryGastroenterologyCESDCholesterol ester storage disease03 medical and health sciences0302 clinical medicinePregnancyLysosomeInternal medicinemedicineHumansAllelebusiness.industryBiochemistry (medical)Infant NewbornWolman DiseaseLipaseGeneral MedicineCholesterol ester storage diseaseLALSterol Esterasemedicine.diseasePhenotype3. Good healthDried blood spot[SDV] Life Sciences [q-bio]030104 developmental biologymedicine.anatomical_structureWolman030220 oncology & carcinogenesisCohortScreeningFemaleCholesterol Estersbusiness
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Clinical application of mutational analysis in breast cancer patients: The relevance of PIK3CA analysis for precision medicine

2019

Abstract Background The identification of biomarkers to drive treatment is one of the most important objectives of precision medicine. During last years, the role of PIK3CA mutations have been related to clinical benefit deriving from treatment with PI3K, and mTOR inhibitors. In breast cancer (BC), PIK3CA mutations are widely present and the use, in clinical trials, of selective inhibitors improved clinical outcomes. The aim of this study is to assess the value of a monocentric genomic screening program to select patients for trials with experimental targeted agents. Methods We examined PIK3CA mutation in a cohort of 312 metastatic BC patients diagnosed at Hospital Clinico Valencia-INCLIVA …

0301 basic medicinemedicine.medical_specialtybusiness.industryHematologymedicine.diseaseDiscovery and development of mTOR inhibitorsPrecision medicineGenomic screeningClinical trialMutational analysis03 medical and health sciences030104 developmental biology0302 clinical medicineBreast cancerOncology030220 oncology & carcinogenesisInternal medicineCohortmedicinebusinessTriple negativeAnnals of Oncology
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Vacuolated PAS-Positive Lymphocytes on Blood Smear: An Easy Screening Tool and a Possible Biomarker for Monitoring Therapeutic Responses in Late Onse…

2018

Background: Primary aim was to investigate the diagnostic value of PAS-positive vacuolated lymphocytes on blood smear in Late Onset Pompe Disease (LOPD) patients and, secondly, to evaluate its potential utility in monitoring treatment effects.Methods: We examined blood smear of 26 LOPD patients. We evaluated 10 treated and 16 untreated LOPD patients. Among the latter group, 7 patients later initiated ERT and were tested again 6 months after start. Blood smear was also sampled from 82 controls and 19 patients with other muscle glycogenoses (MGSDs). PAS staining was used to evaluate: (1) presence of lymphocytes with glycogen-filled vacuoles, (2) quantification of vacuolated lymphocytes.Result…

0301 basic medicinemedicine.medical_specialtytherapeutic monitoringBlood smear; LOPD screening test; PAS-positive lymphocytes; Pompe disease; Therapeutic monitoring; Neurology; Neurology (clinical)Late onsetPeriodic acid–Schiff stainDiseasePAS-positive lymphocytesGastroenterologylcsh:RC346-429Vacuolated Lymphocytes03 medical and health sciences0302 clinical medicineInternal medicineBlood smear; LOPD screening test; PAS-positive lymphocytes; Pompe disease; Therapeutic monitoringmedicineScreening toolLOPD screening testlcsh:Neurology. Diseases of the nervous systemOriginal Researchbusiness.industryPompe diseasePredictive value030104 developmental biologyBlood smearNeurologyblood smearBiomarker (medicine)Neurology (clinical)business030217 neurology & neurosurgeryFrontiers in neurology
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Discovery of Natural Products as Novel and Potent FXR Antagonists by Virtual Screening

2018

Farnesoid X receptor (FXR) is a member of nuclear receptor family involved in multiple physiological processes through regulating specific target genes. The critical role of FXR as a transcriptional regulator makes it a promising target for diverse diseases, especially those related to metabolic disorders such as diabetes and cholestasis. However, the underlying activation mechanism of FXR is still a blur owing to the absence of proper FXR modulators. To identify potential FXR modulators, an in-house natural product database (NPD) containing over 4,000 compounds was screened by structure-based virtual screening strategy and subsequent hit-based similarity searching method. After the yeast t…

0301 basic medicinenatural product01 natural scienceslcsh:Chemistry03 medical and health scienceschemistry.chemical_compoundTranscriptional regulationGeneIC50Original ResearchVirtual screeningNatural productantagonistmolecular dockingsimilarity searchingGeneral Chemistryvirtual screening0104 chemical sciencesChemistry010404 medicinal & biomolecular chemistry030104 developmental biologyFXRlcsh:QD1-999Nuclear receptorBiochemistrychemistryFarnesoid X receptorGuggulsteroneFrontiers in Chemistry
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