Search results for " 11"

showing 10 items of 591 documents

Nonacidic Farnesoid X Receptor Modulators.

2017

As a cellular bile acid sensor, farnesoid X receptor (FXR) participates in regulation of bile acid, lipid and glucose homeostasis, and liver protection. Clinical results have validated FXR as therapeutic target in hepatic and metabolic diseases. To date, potent FXR agonists share a negatively ionizable function that might compromise their pharmacokinetic distribution and behavior. Here we report the development and characterization of a high-affinity FXR modulator not comprising an acidic residue.

0301 basic medicineMalemedicine.drug_classPyridinesPeroxisome proliferator-activated receptorReceptors Cytoplasmic and NuclearATP-binding cassette transporterCholesterol 7 alpha-hydroxylase01 natural sciencesRats Sprague-Dawley03 medical and health sciencesStructure-Activity RelationshipDrug StabilityDrug DiscoverymedicineGlucose homeostasisAnimalsHumansPPAR alphaReceptorCholesterol 7-alpha-HydroxylaseATP Binding Cassette Transporter Subfamily B Member 11chemistry.chemical_classificationBile acid010405 organic chemistryChemistryHEK 293 cellsImidazolesMembrane Transport ProteinsHep G2 Cells0104 chemical sciencesMolecular Docking SimulationZolpidem030104 developmental biologyHEK293 CellsBiochemistryMolecular MedicineFarnesoid X receptorATP-Binding Cassette TransportersSterol Regulatory Element Binding Protein 1HeLa CellsJournal of medicinal chemistry
researchProduct

Meta-analysis of genome-wide association studies discovers multiple loci for chronic lymphocytic leukemia

2016

Chronic lymphocytic leukemia (CLL) is a common lymphoid malignancy with strong heritability. To further understand the genetic susceptibility for CLL and identify common loci associated with risk, we conducted a meta-analysis of four genome-wide association studies (GWAS) composed of 3,100 cases and 7,667 controls with follow-up replication in 1,958 cases and 5,530 controls. Here we report three new loci at 3p24.1 (rs9880772, EOMES, P=2.55 × 10−11), 6p25.2 (rs73718779, SERPINB6, P=1.97 × 10−8) and 3q28 (rs9815073, LPP, P=3.62 × 10−8), as well as a new independent SNP at the known 2q13 locus (rs9308731, BCL2L11, P=1.00 × 10−11) in the combined analysis. We find suggestive evidence (P<5 × 10−…

0301 basic medicineMedicin och hälsovetenskapChronic lymphocytic leukemiaGeneral Physics and AstronomyGenome-wide association studyVARIANTSMedical and Health SciencesMalalties hereditàries[ SDV.MHEP.HEM ] Life Sciences [q-bio]/Human health and pathology/HematologyChronicGeneticsRISKLeukemiaMultidisciplinaryBANK1VDP::Medisinske Fag: 700::Helsefag: 800::Samfunnsmedisin sosialmedisin: 801Bcl-2-Like Protein 11QAdaptor Proteins[SDV.MHEP.HEM]Life Sciences [q-bio]/Human health and pathology/HematologySingle NucleotideLymphocytic3. Good healthPRIORITIZATIONMultidisciplinary SciencesLeukemiamedicine.anatomical_structureScience & Technology - Other TopicsTRANSCRIPTION FACTOR EOMESODERMINGenetic disordersEXPRESSIONSUSCEPTIBILITY LOCIScienceEuropean Continental Ancestry GroupFAS GENE-MUTATIONSLocus (genetics)BiologyPolymorphism Single NucleotideGeneral Biochemistry Genetics and Molecular BiologyCLASSIFICATIONWhite PeopleArticle03 medical and health sciencesProto-Oncogene ProteinsMD MultidisciplinarymedicineGenetic predispositionSNPHumansLeucèmia limfocítica crònicaGenetic Predisposition to DiseasePolymorphismB cellSerpinsGenetic associationAdaptor Proteins Signal TransducingScience & TechnologySignal TransducingB-CellMembrane ProteinsGeneral Chemistrymedicine.diseaseLeukemia Lymphocytic Chronic B-Cell030104 developmental biologyChronic lymphocytic leukemiaVDP::Medical disciplines: 700::Health sciences: 800::Community medicine Social medicine: 801Apoptosis Regulatory ProteinsT-Box Domain ProteinsFOLLICULAR LYMPHOMAGenome-Wide Association Study
researchProduct

C2orf69 mutations disrupt mitochondrial function and cause a multisystem human disorder with recurring autoinflammation

2021

BACKGROUND. Deciphering the function of the many genes previously classified as uncharacterized open reading frame (ORF) would complete our understanding of a cell’s function and its pathophysiology. METHODS. Whole-exome sequencing, yeast 2-hybrid and transcriptome analyses, and molecular characterization were performed in this study to uncover the function of the C2orf69 gene. RESULTS. We identified loss-of-function mutations in the uncharacterized C2orf69 gene in 8 individuals with brain abnormalities involving hypomyelination and microcephaly, liver dysfunction, and recurrent autoinflammation. C2orf69 contains an N-terminal signal peptide that is required and sufficient for mitochondrial…

0301 basic medicineMicrocephalyRespiratory chainBiologyMitochondrionCell LineMitochondrial ProteinsTranscriptomeMiceOpen Reading Frames03 medical and health sciencesAll institutes and research themes of the Radboud University Medical Center0302 clinical medicineLoss of Function MutationGlycogen branching enzymemedicineAnimalsHumansGeneMice KnockoutGeneticsMetabolic Disorders Radboud Institute for Molecular Life Sciences [Radboudumc 6]Glycogen Debranching Enzyme SystemGeneral Medicinemedicine.diseaseMitochondriaOpen reading frameRenal disorders Radboud Institute for Molecular Life Sciences [Radboudumc 11]030104 developmental biology030220 oncology & carcinogenesisMicrocephalybiology.proteinClinical MedicineSignal transductionGlycogenJournal of Clinical Investigation
researchProduct

A phase I study of nintedanib combined with cisplatin/gemcitabine as first-line therapy for advanced squamous non-small cell lung cancer (LUME-Lung 3)

2018

Abstract Background There are limited treatment options for squamous non-small cell lung cancer (sqNSCLC) and prognosis remains poor. The safety and pharmacokinetics (PK) of nintedanib, a triple angiokinase inhibitor, plus cisplatin/gemcitabine as first-line treatment for advanced sqNSCLC patients, were evaluated. Materials and methods A phase I, dose-escalation study administering drugs in a 21-day cycle: cisplatin (75 mg/m2, Day 1), gemcitabine (1250 mg/m2, Days 1 and 8) and nintedanib (Days 2–7, 9–21) were given for 4–6 cycles, followed by monotherapy until disease progression or adverse events (AEs). Two nintedanib doses were tested, 150 mg twice daily (bid) and 200 mg bid, to determine…

0301 basic medicineOncologyMaleCancer ResearchPHARMACOKINETICSIndolesLung NeoplasmsPACLITAXELDeoxycytidineANGIOGENESISSquamouschemistry.chemical_compound0302 clinical medicineNon-small cell lung cancerCarcinoma Non-Small-Cell LungAntineoplastic Combined Chemotherapy ProtocolsBIBF 1120Aged 80 and overMiddle AgedPrognosisTreatment OutcomeOncologyPaclitaxelLABEL DOSE-ESCALATION030220 oncology & carcinogenesisNintedanibFemaleCLINICAL-PRACTICE GUIDELINESmedicine.drugPulmonary and Respiratory Medicinemedicine.medical_specialtyBevacizumabMaximum Tolerated DoseNintedanibBEVACIZUMABCONTROLLED-TRIALDisease-Free Survival03 medical and health sciencesPharmacokineticsInternal medicinemedicineHumansAdverse effectAgedNeoplasm StagingTRIPLE ANGIOKINASE INHIBITORCisplatinCARBOPLATINbusiness.industryGemcitabineCarboplatinGemcitabine030104 developmental biologychemistryCisplatinbusinessLung Cancer
researchProduct

Germline variation in the insulin-like growth factor pathway and risk of Barrett's esophagus and esophageal adenocarcinoma

2020

Contains fulltext : 235640.pdf (Publisher’s version ) (Closed access) Genome-wide association studies (GWAS) of esophageal adenocarcinoma (EAC) and its precursor, Barrett's esophagus (BE), have uncovered significant genetic components of risk, but most heritability remains unexplained. Targeted assessment of genetic variation in biologically relevant pathways using novel analytical approaches may identify missed susceptibility signals. Central obesity, a key BE/EAC risk factor, is linked to systemic inflammation, altered hormonal signaling and insulin-like growth factor (IGF) axis dysfunction. Here, we assessed IGF-related genetic variation and risk of BE and EAC. Principal component analys…

0301 basic medicineOncologyMaleCancer Researchmedicine.medical_specialtyEsophageal NeoplasmsMedizinSingle-nucleotide polymorphismGenome-wide association studyBiologyAdenocarcinomaPolymorphism Single NucleotideReceptor IGF Type 103 medical and health sciencesBarrett Esophagus0302 clinical medicineRisk FactorsSomatomedinsInternal medicineGenetic variationmedicineBiomarkers TumorSNPHumansGenetic Predisposition to DiseaseRisk factorGerm-Line MutationCancer Biomarkers and Molecular EpidemiologyInsulin-like growth factor 1 receptorGenetic associationAgedGeneral MedicineMiddle Agedmedicine.diseaseRenal disorders Radboud Institute for Molecular Life Sciences [Radboudumc 11]030104 developmental biology030220 oncology & carcinogenesisBarrett's esophagusFemaleHuman medicineCarrier ProteinsGenome-Wide Association StudySignal TransductionCarcinogenesis
researchProduct

Imatinib rechallenge in patients with advanced gastrointestinal stromal tumors following progression with imatinib, sunitinib and regorafenib

2018

Background: Rechallenge with imatinib is an option in advanced gastrointestinal stromal tumor (GIST) patients following progression with standard tyrosine-kinase inhibitors (TKIs), imatinib, sunitinib and regorafenib. We retrospectively collected data from metastatic Italian GIST patients treated with imatinib resumption after progression to conventional TKIs. Methods: A total of 104 eligible advanced GIST patients, previously treated with imatinib, sunitinib and regorafenib, were collected from six referral Italian institutions. Mutational analysis was recorded and correlated with survival and response according to RECIST 1.1 or CHOI criteria. Results: Overall, 71 patients treated with ima…

0301 basic medicineOncologymedicine.medical_specialtyStromal cellrechallengelcsh:RC254-28203 medical and health scienceschemistry.chemical_compound0302 clinical medicineInternal medicineRegorafenibhemic and lymphatic diseasesmedicineIn patientStromal tumorneoplasmsOriginal ResearchGiSTbusiness.industrySunitinibImatiniblcsh:Neoplasms. Tumors. Oncology. Including cancer and carcinogensexon 11 KIT mutationTKI030104 developmental biologyOncologychemistryexon 11 KIT mutation; GIST; imatinib; rechallenge; TKIimatinib030220 oncology & carcinogenesisbusinessGIST; TKI; exon 11 KIT mutation; imatinib; rechallengemedicine.drugGIST
researchProduct

Exosomal miRNA analysis in Non-Small Cell Lung Cancer (NSCLC) patients' plasma through qPCR : a feasible liquid biopsy tool

2016

Abstract: The discovery of alterations in the EGFR and ALK genes, amongst others, in NSCLC has driven the development of targeted-drug therapy using selective tyrosine kinase inhibitors (TKIs). To optimize the use of these TKIs, the discovery of new biomarkers for early detection and disease progression is mandatory. These plasma-isolated exosomes can be used as a non-invasive and repeatable way for the detection and followup of these biomarkers. One ml of plasma from 12 NSCLC patients, with different mutations and treatments (and 6 healthy donors as controls), were used as exosome sources. After RNAse treatment, in order to degrade circulating miRNAs, the exosomes were isolated with a comm…

0301 basic medicinePathologyLung NeoplasmsImmunology and Microbiology (all)General Chemical EngineeringBiopsynon-small cell lung cancer (NSCLC)NSCLCExosomes0302 clinical medicineCarcinoma Non-Small-Cell LungChemical Engineering (all)CancerGeneral NeuroscienceMicroRNAReal-time polymerase chain reaction030220 oncology & carcinogenesisBiomarker (medicine)MedicineEndopeptidase KCase-Control StudieEngineering sciences. TechnologyHumanmedicine.medical_specialtyReal-Time Polymerase Chain ReactionExosomeGeneral Biochemistry Genetics and Molecular BiologyRibonucleaseIssue 11103 medical and health sciencesRibonucleasesmicroRNAmedicineBiomarkers TumorHumansLiquid biopsymiRNANeuroscience (all)Biochemistry Genetics and Molecular Biology (all)Liquid biopsyGeneral Immunology and Microbiologybusiness.industryCancerBiomarkermedicine.diseaseMicrovesiclesExosomeLung NeoplasmMicroRNAs030104 developmental biologyCase-Control StudiesCancer researchReagent Kits DiagnosticbusinessJournal of visualized experiments
researchProduct

Jacobsen syndrome and neonatal bleeding: report on two unrelated patients

2021

Abstract Introduction In 1973, Petrea Jacobsen described the first patient showing dysmorphic features, developmental delay and congenital heart disease (atrial and ventricular septal defect) associated to a 11q deletion, inherited from the father. Since then, more than 200 patients have been reported, and the chromosomal critical region responsible for this contiguous gene disorder has been identified. Patients’ presentation We report on two unrelated newborns observed in Italy affected by Jacobsen syndrome (JBS, also known as 11q23 deletion). Both patients presented prenatal and postnatal bleeding, growth and developmental delay, craniofacial dysmorphisms, multiple congenital anomalies, a…

0301 basic medicinePediatricsmedicine.medical_specialtyGenotype-phenotype correlationHeart diseaseGenetic counselingCase ReportIn situ hybridization030105 genetics & heredityPediatricsRJ1-57003 medical and health sciences0302 clinical medicineaCGHJBSmedicineHumansJacobsen Distal 11q Deletion SyndromeJacobsen syndromeCraniofacialGenetic Association StudiesCerebral Hemorrhage11q23 deletionbusiness.industryInfant NewbornEarly diagnosimedicine.diseaseEarly diagnosisPancytopeniaThrombocytopeniaItalyFemalePresentation (obstetrics)business030217 neurology & neurosurgeryComparative genomic hybridizationItalian Journal of Pediatrics
researchProduct

The C-terminal Domains of Apoptotic BH3-only Proteins Mediate Their Insertion into Distinct Biological Membranes

2016

Changes in the equilibrium of pro- and anti-apoptotic members of the B-cell lymphoma-2 (Bcl-2) protein family in the mitochondrial outer membrane (MOM) induce structural changes that commit cells to apoptosis. Bcl-2 homology-3 (BH3)-only proteins participate in this process by either activating pro-apoptotic effectors or inhibiting anti-apoptotic components and by promoting MOM permeabilization. The association of BH3-only proteins with MOMs is necessary for the activation and amplification of death signals; however, the nature of this association remains controversial, as these proteins lack a canonical transmembrane sequence. Here we used an in vitro expression system to study the inserti…

0301 basic medicineProtein familyCèl·lulesBiologyBiochemistryMitochondrial Proteins03 medical and health sciencesProtein DomainsMembranes (Biologia)Protein-fragment complementation assayMembrane BiologyMicrosomesProto-Oncogene ProteinsHumansMolecular BiologyAdaptor Proteins Signal TransducingGeneticsBcl-2-Like Protein 11030102 biochemistry & molecular biologyCell MembraneBcl-2 familyProteïnes de membranaMembrane ProteinsBiological membraneCell BiologyFusion proteinTransmembrane proteinCell biology030104 developmental biologyMembraneProto-Oncogene Proteins c-bcl-2Membrane proteinB-cell lymphoma 2 (Bcl-2) family BH3-only apoptosis membrane insertion membrane protein mitochondrial apoptosis transmembrane domainApoptosis Regulatory ProteinsHydrophobic and Hydrophilic InteractionsHeLa CellsJournal of Biological Chemistry
researchProduct

Cocirculation of Hajj and non-Hajj strains among serogroup W meningococci in Italy, 2000 to 2016

2019

In Italy, B and C are the predominant serogroups among meningococci causing invasive diseases. Nevertheless, in the period from 2013 to 2016, an increase in serogroup W Neisseria meningitidis (MenW) was observed. This study intends to define the main characteristics of 63 MenW isolates responsible of invasive meningococcal disease (IMD) in Italy from 2000 to 2016. We performed whole genome sequencing on bacterial isolates or single gene sequencing on culture-negative samples to evaluate molecular heterogeneity. Our main finding was the cocirculation of the Hajj and the South American sublineages belonging to MenW/clonal complex (cc)11, which gradually surpassed the MenW/cc22 in Italy. All M…

0301 basic medicineSerotypeMaleCefotaximeinvasive bacterial infectionsEpidemiologymolecular methodsNeisseria meningitidismedicine.disease_causeDisease Outbreaks0302 clinical medicineGenotypemolecular method030212 general & internal medicinenational surveillance systemChildPhylogenyAged 80 and overSurveillanceNeisseria meningitidisitaly; neisseria meningitidis; capsular serogroup w; clonal complex 11; invasive bacterial infections; invasive meningococcal disease; molecular methods; national surveillance systeminvasive bacterial infectionMiddle Aged3. Good healthItalyChild PreschoolPopulation SurveillanceFemalePublic Healthmedicine.drugAdultAdolescentAntibiotic sensitivity030106 microbiologyBiologySerogroup03 medical and health sciencesYoung AdultNeisseria meningitidis Serogroup W-135VirologymedicineNeisseria meningitidiHumanscapsular serogroup WAgedWhole Genome Sequencinginvasive meningococcal diseaseEnvironmental and Occupational HealthPublic Health Environmental and Occupational HealthInfant NewbornInfantSequence Analysis DNAVirologyPenicillinMeningococcal Infectionsclonal complex 11capsular serogroup W; clonal complex 11; invasive bacterial infections; invasive meningococcal disease; Italy; molecular methods; national surveillance system; Neisseria meningitidis; Epidemiology; Public Health Environmental and Occupational Health; VirologyHajjRifampicin
researchProduct