2019
Stimulation of Caveolin-1 Signaling Improves Arteriovenous Fistula Patency
Hashimoto T, Isaji T, Hu H, Yamamoto K, Bai H, Santana JM, Kuo A, Kuwahara G, Foster TR, Hanisch JJ, Yatsula BA, Sessa WC, Hoshina K, Dardik A. Stimulation of Caveolin-1 Signaling Improves Arteriovenous Fistula Patency. Arteriosclerosis Thrombosis And Vascular Biology 2019, 39: 754-764. PMID: 30786746, PMCID: PMC6436985, DOI: 10.1161/atvbaha.119.312417.Peer-Reviewed Original ResearchMeSH KeywordsAnimalsAorta, AbdominalArteriovenous Shunt, SurgicalCaveolaeCaveolin 1Cells, CulturedDrug Evaluation, PreclinicalHemorheologyHumansLungMaleMiceMice, Inbred C57BLMice, KnockoutNitric OxideNitric Oxide Synthase Type IIIPeptide FragmentsReceptor, EphB4Signal TransductionVascular RemodelingVena Cava, InferiorConceptsCav-1 KO miceAVF maturationWT miceAVF patencyEph-B4KO miceCav-1 functionCav-1Mouse aortocaval fistula modelEphrin-B2/FcArteriovenous fistula patencyAortocaval fistula modelCaveolin-1 SignalingFistula environmentCav-1 mRNAFistula patencyHET miceVenous adaptationEndothelial cell membraneENOS activityFistula modelRC miceControl veinsWall thickeningMice
2018
Modeling elastin-associated vasculopathy with patient induced pluripotent stem cells and tissue engineering
Ellis MW, Luo J, Qyang Y. Modeling elastin-associated vasculopathy with patient induced pluripotent stem cells and tissue engineering. Cellular And Molecular Life Sciences 2018, 76: 893-901. PMID: 30460472, PMCID: PMC6433159, DOI: 10.1007/s00018-018-2969-7.Peer-Reviewed Original ResearchConceptsExtracellular matrix protein elastinAberrant vascular smooth muscle cell (VSMC) proliferationPatient induced pluripotent stem cellsInduced pluripotent stem cellsHuman disease modelingPluripotent stem cell (iPSC) technologyPluripotent stem cellsDrug screening approachesVascular proliferative diseasesVascular smooth muscle cell proliferationStem cell technologyProtein elastinReplenishable supplyDisruption of functionSmooth muscle cell proliferationDisease modelingStem cellsMuscle cell proliferationCell proliferationScreening approachTherapeutic developmentProliferative diseasesElastinBlood vessel dysfunctionTissue engineeringSynthesis and in Vivo Evaluation of a Novel PET Radiotracer for Imaging of Synaptic Vesicle Glycoprotein 2A (SV2A) in Nonhuman Primates
Li S, Cai Z, Wu X, Holden D, Pracitto R, Kapinos M, Gao H, Labaree D, Nabulsi N, Carson RE, Huang Y. Synthesis and in Vivo Evaluation of a Novel PET Radiotracer for Imaging of Synaptic Vesicle Glycoprotein 2A (SV2A) in Nonhuman Primates. ACS Chemical Neuroscience 2018, 10: 1544-1554. PMID: 30396272, PMCID: PMC6810685, DOI: 10.1021/acschemneuro.8b00526.Peer-Reviewed Original ResearchMeSH KeywordsAnimalsDrug Evaluation, PreclinicalGyrus CinguliMacaca mulattaMembrane GlycoproteinsNerve Tissue ProteinsPositron-Emission TomographyPrimatesRadiopharmaceuticalsRatsConceptsSynaptic vesicle glycoprotein 2AStandardized uptake valuePET radiotracersNonhuman primatesAlterations of synapsesC-UCBPeak standardized uptake valueVivo evaluationHigh brain uptakeNovel PET radiotracersBrain uptakeSynaptic densityExcellent radiotracerPsychiatric disordersUptake valueCingulate cortexAlzheimer's diseaseBrain disordersNovel radiotracersRhesus monkeysNeurodegenerative diseasesTissue kineticsDiseaseAttractive imaging propertiesLevetiracetamLiver diseases in the dish: iPSC and organoids as a new approach to modeling liver diseases
Fiorotto R, Amenduni M, Mariotti V, Fabris L, Spirli C, Strazzabosco M. Liver diseases in the dish: iPSC and organoids as a new approach to modeling liver diseases. Biochimica Et Biophysica Acta (BBA) - Molecular Basis Of Disease 2018, 1865: 920-928. PMID: 30264693, PMCID: PMC6658095, DOI: 10.1016/j.bbadis.2018.08.038.Peer-Reviewed Reviews, Practice Guidelines, Standards, and Consensus StatementsMeSH KeywordsDrug Evaluation, PreclinicalGene EditingHumansInduced Pluripotent Stem CellsLiver DiseasesOrganoidsPrimary Cell CultureConceptsLiver diseaseStem cell fieldHepatocyte-like cellsPluripotent stem cellsRegenerative medicineNext-generation toolsSurvival of patientsRecent technological advancesMononuclear blood cellsPotential applicationsGene editingQuality of lifeLiver cell typesDisease modelingCell fieldAdequate cellular modelsLiver transplantationOrgan failureLiver specimensDiseaseStem cellsBlood cellsLiver cellsDrug testingSkin fibroblastsEditing N-Glycan Site Occupancy with Small-Molecule Oligosaccharyltransferase Inhibitors
Rinis N, Golden JE, Marceau CD, Carette JE, Van Zandt MC, Gilmore R, Contessa JN. Editing N-Glycan Site Occupancy with Small-Molecule Oligosaccharyltransferase Inhibitors. Cell Chemical Biology 2018, 25: 1231-1241.e4. PMID: 30078634, PMCID: PMC6337728, DOI: 10.1016/j.chembiol.2018.07.005.Peer-Reviewed Original ResearchMeSH KeywordsBenzamidesCatalytic DomainDrug Evaluation, PreclinicalEnzyme InhibitorsGene Knockout TechniquesHEK293 CellsHexosyltransferasesHumansMembrane ProteinsStructure-Activity RelationshipSulfonamidesConceptsNGI-1Cellular unfolded protein responseMultisubunit enzyme complexN-glycan site occupancyUnfolded protein responseSubset of glycoproteinsSubunit-specific inhibitorsSecretory pathwayCatalytic subunitProtein responseEnzyme complexTarget proteinsOligosaccharyltransferasePharmacologic inhibitionGlycosylationProteinCell modelBiological effectsInhibitorsStructure-activity relationshipsSTT3BSTT3APharmacological approachesSubunitsSite occupancy
2017
From in silico hit to long-acting late-stage preclinical candidate to combat HIV-1 infection
Kudalkar SN, Beloor J, Quijano E, Spasov KA, Lee WG, Cisneros JA, Saltzman WM, Kumar P, Jorgensen WL, Anderson KS. From in silico hit to long-acting late-stage preclinical candidate to combat HIV-1 infection. Proceedings Of The National Academy Of Sciences Of The United States Of America 2017, 115: e802-e811. PMID: 29279368, PMCID: PMC5789948, DOI: 10.1073/pnas.1717932115.Peer-Reviewed Original ResearchMeSH KeywordsAnimalsAnti-HIV AgentsComputer SimulationDisease Models, AnimalDrug Delivery SystemsDrug Evaluation, PreclinicalDrug SynergismHIV InfectionsHIV-1MiceMice, Inbred BALB CNanoparticlesConceptsHIV-1 drugsDrug-resistant HIV-1 strainsHIV-1 drug-resistant strainsPreclinical candidateDrug-resistant HIV-1HIV-1-infected T cellsDaily treatment regimensActive antiretroviral therapyT cell lossSynergistic antiviral activityHIV-1 infectionAnti-HIV-1 agentsCombination drug regimensHIV-1 strainsMajor therapeutic challengeHIV-1 pandemicPlasma drug concentrationsDrug-resistant strainsVivo pharmacokinetic behaviorAntiretroviral therapyDrug regimensTherapeutic challengeViral loadTreatment regimensSingle doseCalreticulin inhibits inflammation‐induced osteoclastogenesis and bone resorption
Fischer CR, Mikami M, Minematsu H, Nizami S, Lee H, Stamer D, Patel N, Soung D, Back JH, Song L, Drissi H, Lee FY. Calreticulin inhibits inflammation‐induced osteoclastogenesis and bone resorption. Journal Of Orthopaedic Research® 2017, 35: 2658-2666. PMID: 28460421, PMCID: PMC8996436, DOI: 10.1002/jor.23587.Peer-Reviewed Original ResearchConceptsRecombinant human calreticulinIntracellular proteinsCalcium-binding chaperoneDifferent cell typesRecombinant formTranscription factorsFusion of monocytesExtracellular functionsNew therapeutic opportunitiesK activityCathepsin K activityCell typesCalreticulinCytoplasmic 1Anti-osteoclastogenic effectPrecursor cellsMetastatic bone cancerFactor 1Human calreticulinActivated T cellsOsteoclast precursor cellsProteinNuclear factorC-fosMouse calvarial bonesCombined HMG-COA reductase and prenylation inhibition in treatment of CCM
Nishimura S, Mishra-Gorur K, Park J, Surovtseva YV, Sebti SM, Levchenko A, Louvi A, Gunel M. Combined HMG-COA reductase and prenylation inhibition in treatment of CCM. Proceedings Of The National Academy Of Sciences Of The United States Of America 2017, 114: 5503-5508. PMID: 28500274, PMCID: PMC5448170, DOI: 10.1073/pnas.1702942114.Peer-Reviewed Original ResearchMeSH KeywordsAnimalsAstrocytesDiphosphonatesDrosophilaDrug Evaluation, PreclinicalDrug Therapy, CombinationEndothelial CellsFatty Acids, MonounsaturatedFemaleFluvastatinHemangioma, Cavernous, Central Nervous SystemHigh-Throughput Screening AssaysHydroxymethylglutaryl-CoA Reductase InhibitorsImidazolesIndolesMaleMAP Kinase Signaling SystemMicePregnancyProtein PrenylationZoledronic AcidConceptsCerebral cavernous malformationsTreatment of CCMsCommon vascular anomaliesPotential pharmacological treatment optionsFocal neurological deficitsPharmacological treatment optionsCCM diseaseAcute mouse modelCentral nervous systemNeurological deficitsHemorrhagic strokePharmacological therapyLesion burdenVascular deficitsSymptomatic lesionsCombination therapyTreatment optionsVascular anomaliesGlial cellsCavernous malformationsMouse modelPrimary astrocytesNervous systemDrug AdministrationSustained inhibitionTargeting the mitochondrial pyruvate carrier attenuates fibrosis in a mouse model of nonalcoholic steatohepatitis
McCommis KS, Hodges WT, Brunt EM, Nalbantoglu I, McDonald WG, Holley C, Fujiwara H, Schaffer JE, Colca JR, Finck BN. Targeting the mitochondrial pyruvate carrier attenuates fibrosis in a mouse model of nonalcoholic steatohepatitis. Hepatology 2017, 65: 1543-1556. PMID: 28027586, PMCID: PMC5397348, DOI: 10.1002/hep.29025.Peer-Reviewed Original ResearchConceptsStellate cell activationPeroxisome proliferator-activated receptor γProliferator-activated receptor γNonalcoholic steatohepatitisMitochondrial pyruvate carrier 2Cell activationRodent modelsReceptor γDevelopment of NASHNonalcoholic fatty liver diseaseDose-limiting side effectHepatic stellate cell activationFatty liver diseaseInsulin-sensitizing thiazolidinedionesLiver of miceLiver-specific deletionExpression of markersTrans fatty acidsMetabolic syndromeLiver diseaseHepatocyte dysfunctionHepatic fibrosisLiver fibrosisPharmacologic developmentMouse modelEstablished patterns of animal study design undermine translation of disease-modifying therapies for Parkinson’s disease
Zeiss CJ, Allore HG, Beck AP. Established patterns of animal study design undermine translation of disease-modifying therapies for Parkinson’s disease. PLOS ONE 2017, 12: e0171790. PMID: 28182759, PMCID: PMC5300282, DOI: 10.1371/journal.pone.0171790.Peer-Reviewed Original ResearchConceptsDisease-modifying therapiesClinical outcome measuresDisease-modifying interventionsNon-human primatesParkinson's diseaseOutcome measuresStudy designHuman studiesToxin-induced modelsHuman interventional studiesLongitudinal clinical outcomesPreclinical study designStudy design dataToxic protocolsClinical outcomesContemporary cohortNeuropathologic dataStudy design factorsInterventional studyMultiple time pointsPD phenotypeAnimal studiesIntervention characteristicsIntervention categoriesProgressive natureStructural and Preclinical Studies of Computationally Designed Non-Nucleoside Reverse Transcriptase Inhibitors for Treating HIV infection
Kudalkar SN, Beloor J, Chan AH, Lee WG, Jorgensen WL, Kumar P, Anderson KS. Structural and Preclinical Studies of Computationally Designed Non-Nucleoside Reverse Transcriptase Inhibitors for Treating HIV infection. Molecular Pharmacology 2017, 91: 383-391. PMID: 28167742, PMCID: PMC5363707, DOI: 10.1124/mol.116.107755.Peer-Reviewed Original ResearchConceptsNon-nucleoside reverse transcriptase inhibitorBALB/c miceReverse transcriptase inhibitorHIV infectionC miceTranscriptase inhibitorAntiviral activityCompound INew non-nucleoside reverse transcriptase inhibitorHIV-1 non-nucleoside reverse transcriptase inhibitorDetectable acute toxicityTreating HIV InfectionSingle intraperitoneal doseAnti-HIV-1 potencyMT-2 cellsDrug-resistant variantsCompound IISerum residence timeAnti-viral potencyHIV-1 RTClinical benefitClinical efficacyIntraperitoneal doseWild-type HIV-1 RTPlasma clearance
2016
Targeting the HSP60/10 chaperonin systems of Trypanosoma brucei as a strategy for treating African sleeping sickness
Abdeen S, Salim N, Mammadova N, Summers CM, Goldsmith-Pestana K, McMahon-Pratt D, Schultz PG, Horwich AL, Chapman E, Johnson SM. Targeting the HSP60/10 chaperonin systems of Trypanosoma brucei as a strategy for treating African sleeping sickness. Bioorganic & Medicinal Chemistry Letters 2016, 26: 5247-5253. PMID: 27720295, DOI: 10.1016/j.bmcl.2016.09.051.Peer-Reviewed Original ResearchMeSH KeywordsAnimalsAntiprotozoal AgentsChaperonin 10Chaperonin 60Drug Evaluation, PreclinicalHigh-Throughput Screening AssaysHumansTrypanosoma brucei bruceiTrypanosomiasis, AfricanConceptsT. brucei infectionBrucei infectionComplex treatment regimensFirst-line drugsNew therapeutic strategiesLeishmania major promastigotesAnti-parasitic potentialTreatment regimensTherapeutic windowTherapeutic strategiesCurrent drugsMajor promastigotesEncouraging initial resultsHuman liverAntibiotic resistanceGreater cytotoxicityProtozoan parasiteKidney cellsMedicinal chemistry optimizationInfectionInhibitorsPotent inhibitorBrucei parasitesDrugsCytotoxicityOpen Source Drug Discovery with the Malaria Box Compound Collection for Neglected Diseases and Beyond
Van Voorhis WC, Adams JH, Adelfio R, Ahyong V, Akabas MH, Alano P, Alday A, Resto Y, Alsibaee A, Alzualde A, Andrews KT, Avery SV, Avery VM, Ayong L, Baker M, Baker S, Mamoun C, Bhatia S, Bickle Q, Bounaadja L, Bowling T, Bosch J, Boucher LE, Boyom FF, Brea J, Brennan M, Burton A, Caffrey CR, Camarda G, Carrasquilla M, Carter D, Cassera M, Cheng K, Chindaudomsate W, Chubb A, Colon BL, Colón-López DD, Corbett Y, Crowther GJ, Cowan N, D’Alessandro S, Le Dang N, Delves M, DeRisi JL, Du AY, Duffy S, El-Sayed S, Ferdig MT, Robledo J, Fidock DA, Florent I, Fokou PV, Galstian A, Gamo FJ, Gokool S, Gold B, Golub T, Goldgof GM, Guha R, Guiguemde WA, Gural N, Guy RK, Hansen MA, Hanson KK, Hemphill A, van Huijsduijnen R, Horii T, Horrocks P, Hughes TB, Huston C, Igarashi I, Ingram-Sieber K, Itoe MA, Jadhav A, Jensen A, Jensen LT, Jiang RH, Kaiser A, Keiser J, Ketas T, Kicka S, Kim S, Kirk K, Kumar VP, Kyle DE, Lafuente MJ, Landfear S, Lee N, Lee S, Lehane AM, Li F, Little D, Liu L, Llinás M, Loza MI, Lubar A, Lucantoni L, Lucet I, Maes L, Mancama D, Mansour NR, March S, McGowan S, Vera I, Meister S, Mercer L, Mestres J, Mfopa AN, Misra RN, Moon S, Moore JP, da Costa F, Müller J, Muriana A, Hewitt S, Nare B, Nathan C, Narraidoo N, Nawaratna S, Ojo KK, Ortiz D, Panic G, Papadatos G, Parapini S, Patra K, Pham N, Prats S, Plouffe DM, Poulsen SA, Pradhan A, Quevedo C, Quinn RJ, Rice CA, Rizk M, Ruecker A, St. Onge R, Ferreira R, Samra J, Robinett NG, Schlecht U, Schmitt M, Villela F, Silvestrini F, Sinden R, Smith DA, Soldati T, Spitzmüller A, Stamm SM, Sullivan DJ, Sullivan W, Suresh S, Suzuki BM, Suzuki Y, Swamidass SJ, Taramelli D, Tchokouaha LR, Theron A, Thomas D, Tonissen KF, Townson S, Tripathi AK, Trofimov V, Udenze KO, Ullah I, Vallieres C, Vigil E, Vinetz JM, Vinh P, Vu H, Watanabe NA, Weatherby K, White PM, Wilks AF, Winzeler EA, Wojcik E, Wree M, Wu W, Yokoyama N, Zollo PH, Abla N, Blasco B, Burrows J, Laleu B, Leroy D, Spangenberg T, Wells T, Willis PA. Open Source Drug Discovery with the Malaria Box Compound Collection for Neglected Diseases and Beyond. PLOS Pathogens 2016, 12: e1005763. PMID: 27467575, PMCID: PMC4965013, DOI: 10.1371/journal.ppat.1005763.Peer-Reviewed Original ResearchMeSH KeywordsAntimalarialsDatasets as TopicDrug DiscoveryDrug Evaluation, PreclinicalHumansMalariaNeglected DiseasesSmall Molecule LibrariesConceptsOpen Source Drug DiscoveryDrug discoverySubsequent medicinal chemistry effortsMedicinal chemistry programsMedicinal chemistry effortsMalaria BoxHuman cancer cell line panelMedicinal chemistryChemistry programChemistry effortsMalaria Venture (MMV) Malaria BoxCompound collectionsFamily of structuresCancer cell line panelPhysical compoundsHuman tumor cell linesCompoundsBiological assaysCell line panelPromising candidateValuable starting pointMalaria parasitesImmense potentialLine panelMultiple life cycle stagesAfatinib plus Cetuximab Delays Resistance Compared to Single-Agent Erlotinib or Afatinib in Mouse Models of TKI-Naïve EGFR L858R-Induced Lung Adenocarcinoma
Pirazzoli V, Ayeni D, Meador CB, Sanganahalli BG, Hyder F, de Stanchina E, Goldberg SB, Pao W, Politi K. Afatinib plus Cetuximab Delays Resistance Compared to Single-Agent Erlotinib or Afatinib in Mouse Models of TKI-Naïve EGFR L858R-Induced Lung Adenocarcinoma. Clinical Cancer Research 2016, 22: 426-435. PMID: 26341921, PMCID: PMC4715986, DOI: 10.1158/1078-0432.ccr-15-0620.Peer-Reviewed Original ResearchMeSH KeywordsAdenocarcinomaAdenocarcinoma of LungAfatinibAnimalsCell Line, TumorCetuximabDrug Evaluation, PreclinicalDrug Resistance, NeoplasmDrug Therapy, CombinationErbB ReceptorsErlotinib HydrochlorideLung NeoplasmsMiceMice, NudeMutationNeoplasm Recurrence, LocalProtein Kinase InhibitorsProtein-Tyrosine KinasesProto-Oncogene Proteins p21(ras)QuinazolinesConceptsTyrosine kinase inhibitorsLung adenocarcinomaLung cancerMouse modelAdvanced EGFR-mutant lung adenocarcinomaFirst-generation tyrosine kinase inhibitorSingle-agent tyrosine kinase inhibitorsEGFR-mutant lung cancerEGFR-mutant lung adenocarcinomaEGFR tyrosine kinase inhibitorsCetuximab-resistant tumorsPotential of afatinibFirst-line therapyMutant lung cancerEGFR antibody cetuximabCombination of afatinibEGFR-TKI afatinibClinical trial developmentEffective treatment strategiesDrug-resistant tumorsAgent erlotinibTKI-naïveAfatinib treatmentTumor escapeClinical trialsComparative evaluation of two glycine transporter 1 radiotracers [11C]GSK931145 and [18F]MK‐6577 in baboons
Zheng MQ, Lin SF, Holden D, Naganawa M, Ropchan JR, Najafzaden S, Kapinos M, Tabriz M, Carson RE, Hamill TG, Huang Y. Comparative evaluation of two glycine transporter 1 radiotracers [11C]GSK931145 and [18F]MK‐6577 in baboons. Synapse 2016, 70: 112-120. PMID: 26671330, DOI: 10.1002/syn.21879.Peer-Reviewed Original ResearchAnimalsBenzamidesBrainBrain MappingCarbon RadioisotopesChromatography, High Pressure LiquidDrug Evaluation, PreclinicalFemaleGlycine AgentsGlycine Plasma Membrane Transport ProteinsKineticsLinear ModelsMagnetic Resonance ImagingMolecular StructurePapioPositron-Emission TomographyRadiopharmaceuticalsSulfonamidesA Novel Inherently Radiopaque Bead for Transarterial Embolization to Treat Liver Cancer - A Pre-clinical Study
Duran R, Sharma K, Dreher MR, Ashrafi K, Mirpour S, Lin M, Schernthaner RE, Schlachter TR, Tacher V, Lewis AL, Willis S, Hartog M, Radaelli A, Negussie AH, Wood BJ, Geschwind JF. A Novel Inherently Radiopaque Bead for Transarterial Embolization to Treat Liver Cancer - A Pre-clinical Study. Theranostics 2016, 6: 28-39. PMID: 26722371, PMCID: PMC4679352, DOI: 10.7150/thno.13137.Peer-Reviewed Original ResearchMeSH KeywordsAnimalsDisease Models, AnimalDrug Evaluation, PreclinicalEmbolization, TherapeuticFluoroscopyLiver NeoplasmsMicrospheresRabbitsRadiographyStaining and LabelingConceptsEquilibrium water contentDurable suspensionLower equilibrium water contentPhysicomechanical propertiesBead locationSingle shotBead sizeSize distributionSimilar penetrationSimilar size distributionX-ray attenuationBead typesWater contentDeliverabilityBeadsLC beadsHigh densitySuspension timePenetrationCone-beam CTDensityRoMicroshperesSuspensionNon-target arteries
2015
The Discovery and Characterization of the α‑Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptor Potentiator N‑{(3S,4S)‑4-[4-(5-Cyano-2-thienyl)phenoxy]tetrahydrofuran-3-yl}propane-2-sulfonamide (PF-04958242)
Shaffer CL, Patel NC, Schwarz J, Scialis RJ, Wei Y, Hou XJ, Xie L, Karki K, Bryce DK, Osgood SM, Hoffmann WE, Lazzaro JT, Chang C, McGinnis DF, Lotarski SM, Liu J, Obach RS, Weber ML, Chen L, Zasadny KR, Seymour PA, Schmidt CJ, Hajós M, Hurst RS, Pandit J, O’Donnell C. The Discovery and Characterization of the α‑Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptor Potentiator N‑{(3S,4S)‑4-[4-(5-Cyano-2-thienyl)phenoxy]tetrahydrofuran-3-yl}propane-2-sulfonamide (PF-04958242). Journal Of Medicinal Chemistry 2015, 58: 4291-4308. PMID: 25905800, DOI: 10.1021/acs.jmedchem.5b00300.Peer-Reviewed Original ResearchMeSH KeywordsAdministration, OralAdolescentAdultAgedAnimalsBinding SitesDisease Models, AnimalDogsDose-Response Relationship, DrugDrug DiscoveryDrug Evaluation, PreclinicalDrug StabilityFemaleHumansMaleMemory, Short-TermMice, Inbred C57BLMiddle AgedProtein ConformationRats, Sprague-DawleyReceptors, AMPASchizophreniaStructure-Activity RelationshipSulfonamidesThiophenesYoung AdultConceptsΑ-aminoIsoxazolepropionic acid receptor potentiatorsAdequate therapeutic indexPharmacokinetic variabilityClinical studiesReceptor potentiatorsTherapeutic indexPreclinical characterizationCognitive deficitsMetabolic stabilityPhenyl motifLigand-binding domainLead compoundsSubsequent replacementGluA2 ligand-binding domainPatientsSchizophreniaInsulin therapy normalizes reduced myocardial β-adrenoceptors at both the onset and after sustained hyperglycemia in diabetic rats
Haley JM, Thackeray JT, Kolajova M, Thorn SL, DaSilva JN. Insulin therapy normalizes reduced myocardial β-adrenoceptors at both the onset and after sustained hyperglycemia in diabetic rats. Life Sciences 2015, 132: 101-107. PMID: 25934520, DOI: 10.1016/j.lfs.2015.03.024.Peer-Reviewed Original ResearchConceptsCardiac β-ARPositron emission tomographyΒ-ARHeart rateInsulin therapyDiabetes mellitusΒ-adrenoceptorsCV functionWestern blottingInsulin effectDuration of hyperglycemiaMyocardial β-adrenoceptorsΒ-AR expressionOnset of hyperglycemiaWeeks of hyperglycemiaCardiac β-adrenoceptorsΒ-AR subtypesReduced heart rateMyocardial β-ARsGlycemic therapyStreptozotocin ratsSerial echocardiographySTZ ratsGlycemic controlCardiovascular dysfunctionChinese herbal medicine for miscarriage affects decidual micro-environment and fetal growth
Piao L, Chen C, Yeh C, Basar M, Masch R, Cheng Y, Lockwood CJ, Schatz F, Huang SJ. Chinese herbal medicine for miscarriage affects decidual micro-environment and fetal growth. Placenta 2015, 36: 559-566. PMID: 25771406, PMCID: PMC4395550, DOI: 10.1016/j.placenta.2015.02.006.Peer-Reviewed Original ResearchConceptsFirst trimester decidual cellsIL-1βDecidual cellsPlacental weightFetal growthFood intakeResorption rateFetal resorption rateM-CSFMaternal food intakeC motif ligand 2Intrauterine growth restrictionIGF-IR expressionInducible protein-10Anti-CD163 antibodyQRT-PCRChinese herbal formulaIL-8 productionChinese herbal medicineG-CSF expressionEndothelial cell angiogenesisPlacental IGFDecidual macrophagesFetal weightCytokine expressionLocal delivery of paclitaxel in the treatment of peripheral arterial disease
Ng VG, Mena C, Pietras C, Lansky AJ. Local delivery of paclitaxel in the treatment of peripheral arterial disease. European Journal Of Clinical Investigation 2015, 45: 333-345. PMID: 25615282, DOI: 10.1111/eci.12407.Peer-Reviewed Original ResearchConceptsPeripheral artery diseaseEndovascular revascularizationArtery diseaseLocal deliveryClinical studiesLocal drug deliveryPeripheral arterial diseasePeripheral vascular diseasePrimary patency rateSystemic adverse effectsUse of paclitaxelLong-term efficacyDrug-Eluting BalloonDrug-eluting stentsTerms of efficacyBrief exposure periodArterial diseaseBalloon angioplastyPatency ratesVascular diseaseBalloon catheterCoated balloonMEDLINE searchStent failureActive drug
This site is protected by hCaptcha and its Privacy Policy and Terms of Service apply