2023
RAMIHM generates fully human monoclonal antibodies by rapid mRNA immunization of humanized mice and BCR-seq
Ren P, Peng L, Yang L, Suzuki K, Fang Z, Renauer P, Lin Q, Bai M, Li T, Clark P, Klein D, Chen S. RAMIHM generates fully human monoclonal antibodies by rapid mRNA immunization of humanized mice and BCR-seq. Cell Chemical Biology 2023, 30: 85-96.e6. PMID: 36640761, PMCID: PMC9868106, DOI: 10.1016/j.chembiol.2022.12.005.Peer-Reviewed Original ResearchConceptsHuman monoclonal antibodyHumanized miceMonoclonal antibodiesMemory B cell populationsHumanized transgenic miceBroad antibody responseB cell populationsG protein-coupled receptor targetsNeutralizing antibodiesPeripheral bloodAntibody responseImmunotherapy targetClinical vaccinesPlasma BCell sequencingTransgenic miceImmunization methodReceptor targetsAntibodiesMiceCell populationsHigh potencyImmunizationHigh rateAntibody discovery
2021
Potency and Preclinical Evidence of Synergy of Oral Azole Drugs and Miltefosine in an Ex Vivo Model of Leishmania (Viannia) panamensis Infection
Fernández OL, Rosales-Chilama M, Quintero N, Travi BL, Wetzel DM, Gómez MA, Saravia NG. Potency and Preclinical Evidence of Synergy of Oral Azole Drugs and Miltefosine in an Ex Vivo Model of Leishmania (Viannia) panamensis Infection. Antimicrobial Agents And Chemotherapy 2021, 66: e01425-21. PMID: 34694879, PMCID: PMC8765415, DOI: 10.1128/aac.01425-21.Peer-Reviewed Original ResearchConceptsFractional inhibitory concentration indexPeripheral blood mononuclear cellsL. panamensisHuman peripheral blood mononuclear cellsClinical strainsLeishmania panamensis infectionOral azole drugsOral combination therapyFailure of treatmentBlood mononuclear cellsEfficacy of treatmentNovel therapeutic strategiesEffectiveness of treatmentHigh potencyReduction of infectionEx vivo modelInhibitory concentration indexFree drug concentrationPanamensis infectionPreclinical evidenceCombination therapyMononuclear cellsAntimonial drugsCutaneous leishmaniasisDrug combinationsDeintensification or No Statin Treatment Is Associated With Higher Mortality in Patients With Ischemic Stroke or Transient Ischemic Attack
Dearborn-Tomazos JL, Hu X, Bravata DM, Phadke MA, Baye FM, Myers LJ, Concato J, Zillich AJ, Reeves MJ, Sico JJ. Deintensification or No Statin Treatment Is Associated With Higher Mortality in Patients With Ischemic Stroke or Transient Ischemic Attack. Stroke 2021, 52: 2521-2529. PMID: 34015937, DOI: 10.1161/strokeaha.120.030089.Peer-Reviewed Original ResearchConceptsTransient ischemic attackIschemic strokeIschemic attackHospital dischargeHospital admissionHigh mortalityVeterans Health Administration facilitiesHigh-potency statinsUnderutilization of statinsHigh potencyStatin doseStatin medicationBaseline characteristicsMost patientsPrescribed statinsStatin treatmentPharmacy filesStatin potencyAtherosclerotic originUS veteransPractice guidelinesStudy populationHigher oddsPatientsStatinsCharacterization of Vixotrigine, a Broad-Spectrum Voltage-Gated Sodium Channel Blocker
Hinckley C, Kuryshev Y, Sers A, Barre A, Buisson B, Naik H, Hajos M. Characterization of Vixotrigine, a Broad-Spectrum Voltage-Gated Sodium Channel Blocker. Molecular Pharmacology 2021, 99: 49-59. PMID: 33298520, DOI: 10.1124/molpharm.120.000079.Peer-Reviewed Original ResearchConceptsNav blockersNav subtypesVoltage-gated sodium channel subtypesSodium channelsSteady-state inactivation curveSodium channel blockersSodium channel subtypesUse-dependent mannerState-dependent inhibitionVoltage-gated sodium channelsState-dependent blockNeuropathic painAntiepileptic therapyProlong recoveryChannel blockersSensory neuronsChannel subtypesSodium currentBlockersVixotrigineNeural typeSubtypesHigh potencyRecombinant systemsPain
2019
Nitric oxide-donor/PARP-inhibitor combination: A new approach for sensitization to ionizing radiation
Wilson A, Menon V, Khan Z, Alam A, Litovchick L, Yakovlev V. Nitric oxide-donor/PARP-inhibitor combination: A new approach for sensitization to ionizing radiation. Redox Biology 2019, 24: 101169. PMID: 30889466, PMCID: PMC6423503, DOI: 10.1016/j.redox.2019.101169.Peer-Reviewed Original ResearchConceptsPARP inhibitorsBRCA1/2 mutationsSingle agentTumor microenvironmentAdditional therapeutic benefitBRCA1 expressionNew drug combinationsDNA-damaging therapiesNon-toxic concentrationsTumor-targeting approachesCancer patientsOvarian cancerBreast cancerDrug combinationsTherapeutic benefitClinical developmentTumorsRadiation treatmentCancerOxidative stressSubsequent inhibitionSynthetic lethality approachSensitizationHigh potencyDNA damage
2016
The ALK/ROS1 Inhibitor PF-06463922 Overcomes Primary Resistance to Crizotinib in ALK-Driven Neuroblastoma
Infarinato NR, Park JH, Krytska K, Ryles HT, Sano R, Szigety KM, Li Y, Zou HY, Lee NV, Smeal T, Lemmon MA, Mossé YP. The ALK/ROS1 Inhibitor PF-06463922 Overcomes Primary Resistance to Crizotinib in ALK-Driven Neuroblastoma. Cancer Discovery 2016, 6: 96-107. PMID: 26554404, PMCID: PMC4707106, DOI: 10.1158/2159-8290.cd-15-1056.Peer-Reviewed Original ResearchMeSH KeywordsAminopyridinesAnaplastic Lymphoma KinaseAnimalsCell Line, TumorCrizotinibDrug Resistance, NeoplasmHumansLactamsLactams, MacrocyclicMiceMutationNeuroblastomaPhosphorylationProtein Kinase InhibitorsPyrazolesPyridinesReceptor Protein-Tyrosine KinasesTreatment OutcomeXenograft Model Antitumor AssaysConceptsAnaplastic lymphoma kinaseCrizotinib resistancePF-06463922ALK variantsTreatment of patientsALK inhibitor crizotinibPatient-derived xenograftsXenograft mouse modelPreclinical rationaleClinical obstacleNeuroblastoma modelClinical trialsTumor regressionPrimary resistanceInhibitor crizotinibXenograft tumorsMouse modelXenograft modelLymphoma kinaseNeuroblastomaCrizotinibHigh potencyF1174LVivo dataImproved potency
2015
Synthesis of 3‐[18F]Fluoro‐5‐(2‐Pyridinylethynyl)Benzonitrile ([18F]FPEB)
Liang S, Yokell D, Jackson R, Rice P, Livni E, Alagille D, Tamagnan G, Collier T, Vasdev N. Synthesis of 3‐[18F]Fluoro‐5‐(2‐Pyridinylethynyl)Benzonitrile ([18F]FPEB). 2015, 41-51. DOI: 10.1002/9781118834114.ch5.Peer-Reviewed Original ResearchMetabotropic glutamate receptor subtype 5Regional brain concentrationsHealthy human subjectsBrain concentrationsBrain penetranceMGluR5 antagonistSubtype 5Parkinson's diseasePathologic processesAlzheimer's diseaseNeuropsychiatric disordersNeurodegenerative diseasesDiseaseHigh potencyHuman subjectsEvidence pointsFragile X syndromeControl testsRadiochemical purityCritical roleX syndromeMGluR5SyndromeAntagonistAbnormalitiesIn Vitro and in Vivo Neuronal Nicotinic Receptor Properties of (+)- and (−)-Pyrido[3,4]homotropane [(+)- and (−)-PHT]: (+)-PHT Is a Potent and Selective Full Agonist at α6β2 Containing Neuronal Nicotinic Acetylcholine Receptors
Carroll FI, Navarro H, Mascarella SW, Castro AH, Luetje CW, Wageman CR, Marks MJ, Jackson A, Damaj MI. In Vitro and in Vivo Neuronal Nicotinic Receptor Properties of (+)- and (−)-Pyrido[3,4]homotropane [(+)- and (−)-PHT]: (+)-PHT Is a Potent and Selective Full Agonist at α6β2 Containing Neuronal Nicotinic Acetylcholine Receptors. ACS Chemical Neuroscience 2015, 6: 920-926. PMID: 25891987, PMCID: PMC5589077, DOI: 10.1021/acschemneuro.5b00077.Peer-Reviewed Original ResearchMeSH Keywordsalpha7 Nicotinic Acetylcholine ReceptorAnimalsConditioning, PsychologicalCorpus StriatumDopamineDose-Response Relationship, DrugMaleMice, Inbred ICRMolecular StructureNeuronsNicotinic AgonistsNicotinic AntagonistsPyridinesRatsReceptors, NicotinicSpatial BehaviorSynaptosomesTropanesXenopus laevisConceptsNicotinic antagonistsNeuronal nicotinic acetylcholine receptorsLow efficacy partial agonistSelective full agonistHot plate testNicotinic acetylcholine receptorsPlace preference studiesNicotine rewardAntinociceptive activityΑ3β4 nAChRsΑ7 nAChRsElectrophysiological studiesΑ4β2 nAChRsAcetylcholine receptorsAgonist activityPartial agonistFull agonistNAChRsFull agonismPartial agonismAntagonistΑ4β2MiceReceptor propertiesHigh potency
2014
Fyn kinase inhibition as a novel therapy for Alzheimer’s disease
Nygaard HB, van Dyck CH, Strittmatter SM. Fyn kinase inhibition as a novel therapy for Alzheimer’s disease. Alzheimer's Research & Therapy 2014, 6: 8. PMID: 24495408, PMCID: PMC3978417, DOI: 10.1186/alzrt238.Peer-Reviewed Original ResearchAlzheimer's diseasePathogenesis of ADTreatment of ADPhase Ib studyLate-stage clinical testingUnique therapeutic targetMajor pathologic hallmarkDevastating neurodegenerative disorderPathologic hallmarkNovel therapiesIb studyTherapeutic strategiesTherapeutic targetSmall molecule inhibitorsClinical testingTyrosine kinase FynCellular prion proteinNeurodegenerative disordersDiseaseAβ oligomersCell surface bindingMultisite studyHigh potencyMolecule inhibitorsTherapy
2010
A Remote Arene-Binding Site on Prostate Specific Membrane Antigen Revealed by Antibody-Recruiting Small Molecules
Zhang AX, Murelli RP, Barinka C, Michel J, Cocleaza A, Jorgensen WL, Lubkowski J, Spiegel DA. A Remote Arene-Binding Site on Prostate Specific Membrane Antigen Revealed by Antibody-Recruiting Small Molecules. Journal Of The American Chemical Society 2010, 132: 12711-12716. PMID: 20726553, PMCID: PMC2965167, DOI: 10.1021/ja104591m.Peer-Reviewed Original Research
1985
GABA‐Modulin: A Synaptosomal Basic Protein that Differs from Small Myelin Basic Protein of Rat Brain
Vaccarino F, Tronconi B, Panula P, Guidotti A, Costa E. GABA‐Modulin: A Synaptosomal Basic Protein that Differs from Small Myelin Basic Protein of Rat Brain. Journal Of Neurochemistry 1985, 44: 278-290. PMID: 3964832, DOI: 10.1111/j.1471-4159.1985.tb07142.x.Peer-Reviewed Original ResearchMeSH KeywordsAmino AcidsAnimalsBrain ChemistryCarrier ProteinsChromatography, High Pressure LiquidCyanogen BromideGABA Plasma Membrane Transport ProteinsMembrane ProteinsMembrane Transport ProteinsMuscimolMyelin ProteinsMyelin SheathNerve Tissue ProteinsOrganic Anion TransportersPeptide FragmentsRatsSubcellular FractionsSynaptosomesTissue DistributionConceptsGABA-modulinSmall myelin basic proteinMyelin basic proteinRat brainBasic proteinModulation of GABANeuronal membrane functionNeurotransmitter receptorsSynaptosomal fractionGABA bindingSynaptic membranesSynaptosomal membranesStaphylococcal V8 protease digestionSynaptosomal proteinsNeuronal specificityAcid compositionHigh potencyGABAHigh-affinity bindingBrainMyelinAmino acid compositionTotal synaptosomal proteinApparent molecular weightMembrane function
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