2025
Selective Mu-Opioid Receptor Imaging Using 18F‑Labeled Carfentanils
Lee S, Pearson T, Dhaynaut M, MacDonagh A, Wey H, Wilks M, Roth B, Hooker J, Normandin M. Selective Mu-Opioid Receptor Imaging Using 18F‑Labeled Carfentanils. Journal Of Medicinal Chemistry 2025, 68: 1632-1644. PMID: 39772615, DOI: 10.1021/acs.jmedchem.4c02287.Peer-Reviewed Original ResearchConceptsMu-opioid receptorsPositron emission tomographyIn vivo PET scansCarbon-11Neurobiological studiesCopper-mediated radiofluorinationMu-opioidReceptor imagingPET scansBrain uptakeFavorable pharmacokineticsImaging evaluationHigh molar activityMass doseEmission tomographyHalf-life of fluorine-18Synthetic opioidsFluorine-18Half-lifeIn vitro binding assaysBinding assaysClinical research useMolar activityCarfentanilResearch use
2024
The molecular basis of sugar detection by an insect taste receptor
Gomes J, Singh-Bhagania S, Cenci M, Chacon Cordon C, Singh M, Butterwick J. The molecular basis of sugar detection by an insect taste receptor. Nature 2024, 629: 228-234. PMID: 38447670, PMCID: PMC11062906, DOI: 10.1038/s41586-024-07255-w.Peer-Reviewed Original ResearchLigand-binding pocketGustatory receptorsD-fructoseMolecular basisStructure-guided mutagenesisSilkworm Bombyx moriPatterns of chemical groupsIon conductivitySugar selectivityAllosteric pathwaysBombyx moriExperimental binding assaysReceptor-ligand interactionsL-sorboseComputational dockingAromatic residuesActive ligandsAllosteric couplingConformational changesSugar detectionBinding assaysFunctional assaysChemical specificityChemical groupsTaste receptors
2022
Pigment epithelium-derived factor engineered to increase glycosaminoglycan affinity while maintaining bioactivity
Chu H, Rebustini I, Becerra S, Wang Y. Pigment epithelium-derived factor engineered to increase glycosaminoglycan affinity while maintaining bioactivity. Biochemical And Biophysical Research Communications 2022, 605: 148-153. PMID: 35334413, PMCID: PMC11371396, DOI: 10.1016/j.bbrc.2022.03.079.Peer-Reviewed Original ResearchConceptsPigment epithelium-derived factorEpithelium-derived factorNegatively charged extracellular matrixInhibit endothelial cell proliferationAmino acid sequenceHyaluronic acidEndothelial cell proliferationExtracellular matrixRetinal degenerationRetinal diseasesRetinal microenvironmentProtect photoreceptorsTherapeutic effectVitreous humorProtein engineeringGlycosaminoglycan affinitySecreted proteinsTherapeutic drugsTube formationTissue homeostasisCell deathCell proliferationEfficient therapeutic drugsCationic residuesBinding assays
2017
Pathological correlations of [F‐18]‐AV‐1451 imaging in non‐alzheimer tauopathies
Marquié M, Normandin M, Meltzer A, Chong M, Andrea N, Antón‐Fernández A, Klunk W, Mathis C, Ikonomovic M, Debnath M, Bien E, Vanderburg C, Costantino I, Makaretz S, DeVos S, Oakley D, Gomperts S, Growdon J, Domoto‐Reilly K, Lucente D, Dickerson B, Frosch M, Hyman B, Johnson K, Gómez‐Isla T. Pathological correlations of [F‐18]‐AV‐1451 imaging in non‐alzheimer tauopathies. Annals Of Neurology 2017, 81: 117-128. PMID: 27997036, PMCID: PMC5319193, DOI: 10.1002/ana.24844.Peer-Reviewed Original ResearchConceptsNon-Alzheimer tauopathiesTau lesionsDetection of tau aggregatesBinding to tau lesionsTau measuresPositron emission tomographyMutation carriersTau filamentsProgressive supranuclear palsyTau aggregationPostmortem brain samplesAlzheimer brainsTauopathiesAV-1451Atypical tauopathyBrain regionsOff-target bindingBinding patternsBinding assaysBasal gangliaEntorhinal cortexSubstantia nigraTauMAPT
2016
Aedes aegypti D7 Saliva Protein Inhibits Dengue Virus Infection
Conway MJ, Londono-Renteria B, Troupin A, Watson AM, Klimstra WB, Fikrig E, Colpitts TM. Aedes aegypti D7 Saliva Protein Inhibits Dengue Virus Infection. PLOS Neglected Tropical Diseases 2016, 10: e0004941. PMID: 27632170, PMCID: PMC5025043, DOI: 10.1371/journal.pntd.0004941.Peer-Reviewed Original ResearchConceptsSalivary gland extractsDengue virus infectionD7 proteinDengue virus type 1Virus type 1DENV envelope proteinAegypti salivaLymph nodesDENV infectionDENV virionsVirus infectionRelevant arbovirusesType 1InfectionHost skinBlood feedingEnvelope proteinNovel roleBinding assaysSalivaAedes aegyptiGland extractsPrimary vectorHPLC fractionsFeeding
2015
Validating novel tau positron emission tomography tracer [F‐18]‐AV‐1451 (T807) on postmortem brain tissue
Marquié M, Normandin M, Vanderburg C, Costantino I, Bien E, Rycyna L, Klunk W, Mathis C, Ikonomovic M, Debnath M, Vasdev N, Dickerson B, Gomperts S, Growdon J, Johnson K, Frosch M, Hyman B, Gómez-Isla T. Validating novel tau positron emission tomography tracer [F‐18]‐AV‐1451 (T807) on postmortem brain tissue. Annals Of Neurology 2015, 78: 787-800. PMID: 26344059, PMCID: PMC4900162, DOI: 10.1002/ana.24517.Peer-Reviewed Original ResearchConceptsTau filamentsAlzheimer brainsTDP-43Paired helical filamentsDNA-binding proteinsIn vitro binding assaysFrontotemporal lobar degeneration-tauBinding to tau lesionsDNA-binding protein 43Tauopathy brainsHelical filamentsBrain tau pathologyTau pathologyTau lesionsSubstrate-specificBinding proteinPostmortem brain tissueCerebral amyloid angiopathyPhosphor-screen autoradiographyOff-target bindingB-amyloidAlzheimer's diseaseBinding assaysTauProtein 43
2013
The common hereditary elliptocytosis-associated α-spectrin L260P mutation perturbs erythrocyte membranes by stabilizing spectrin in the closed dimer conformation
Harper SL, Sriswasdi S, Tang HY, Gaetani M, Gallagher PG, Speicher DW. The common hereditary elliptocytosis-associated α-spectrin L260P mutation perturbs erythrocyte membranes by stabilizing spectrin in the closed dimer conformation. Blood 2013, 122: 3045-3053. PMID: 23974198, PMCID: PMC3811177, DOI: 10.1182/blood-2013-02-487702.Peer-Reviewed Original ResearchMeSH KeywordsAmino Acid SequenceBinding SitesCross-Linking ReagentsElliptocytosis, HereditaryErythrocyte MembraneHumansModels, MolecularMolecular Sequence DataMutationProtein BindingProtein MultimerizationProtein StabilityProtein Structure, SecondaryProtein Structure, TertiaryRecombinant ProteinsSpectrinConceptsHereditary elliptocytosisMembrane destabilizationLarge conformational rearrangementsGel filtration analysisMembrane proteinsTetramer assemblyHereditary pyropoikilocytosisBiophysical analysisCommon hereditary elliptocytosisConformational rearrangementsDimer conformationHelical contentTetramerization siteFiltration analysisSpectrin tetramersNovel mechanismUnknown mechanismMutationsBinding assaysSpectrinChemical crosslinkingErythrocyte shapeTetramerErythrocyte membranesMembrane
2012
Claudin-6: a novel receptor for CPE-mediated cytotoxicity in ovarian cancer
Lal-Nag M, Battis M, Santin AD, Morin PJ. Claudin-6: a novel receptor for CPE-mediated cytotoxicity in ovarian cancer. Oncogenesis 2012, 1: e33-e33. PMID: 23552466, PMCID: PMC3511677, DOI: 10.1038/oncsis.2012.32.Peer-Reviewed Original ResearchClostridium perfringens enterotoxinClaudin-6Claudin-3Ovarian cancer cell linesNovel receptorCell linesTight junction proteinsOvarian cell linesCancer cell linesOvarian cancerNovel functional receptorMouse modelCPE cytotoxicityClaudin-4Functional receptorsCancerEpithelial cell architecturePerfringens enterotoxinUCI 101Different cancersJunction proteinsReceptorsRapid cell lysisBinding assaysIntegral tight junction proteinsSynthesis and evaluation of 4-(substituted styryl/alkenyl)-3,5-bis(4-hydroxyphenyl)-isoxazoles as ligands for the estrogen receptor
Haddad T, Gershman R, Dilis R, Labaree D, Hochberg RB, Hanson RN. Synthesis and evaluation of 4-(substituted styryl/alkenyl)-3,5-bis(4-hydroxyphenyl)-isoxazoles as ligands for the estrogen receptor. Bioorganic & Medicinal Chemistry Letters 2012, 22: 5999-6003. PMID: 22906893, PMCID: PMC3444814, DOI: 10.1016/j.bmcl.2012.06.097.Peer-Reviewed Original Research
2011
Interaction of Recombinant Myocilin with the Matricellular Protein SPARC: Functional Implications
Aroca-Aguilar JD, Sánchez-Sánchez F, Ghosh S, Fernández-Navarro A, Coca-Prados M, Escribano J. Interaction of Recombinant Myocilin with the Matricellular Protein SPARC: Functional Implications. Investigative Ophthalmology & Visual Science 2011, 52: 179-189. PMID: 20926826, PMCID: PMC3053273, DOI: 10.1167/iovs.09-4866.Peer-Reviewed Original ResearchMeSH KeywordsAmino Acid SequenceBlotting, WesternCalcium-Binding ProteinsCell LineChromatography, High Pressure LiquidCytoskeletal ProteinsExtracellular Matrix ProteinsEye ProteinsGene Expression ProfilingGlycoproteinsHumansKidneyMicroscopy, FluorescenceMolecular Sequence DataOsteonectinPolymerase Chain ReactionProtein BindingRecombinant Fusion ProteinsRecombinant ProteinsTwo-Hybrid System TechniquesConceptsHEK 293T cellsSolid-phase binding assaysInteraction of myocilinRecombinant proteinsRecombinant myocilinMatricellular proteinEC domainTerminal olfactomedin domainTwo-hybrid analysisTwo-hybrid systemProtein-protein interactionsFull-length myocilinC-terminal domainN-terminal domainC-terminal regionCalcium binding domainsBinding assaysOlfactomedin domainC-terminal fragmentBinding domainsLinker regionUnknown functionExtracellular glycoproteinIntracellular interactionsSPARC family
2010
Optimization of N-benzyl-benzoxazol-2-ones as receptor antagonists of macrophage migration inhibitory factor (MIF)
Hare AA, Leng L, Gandavadi S, Du X, Cournia Z, Bucala R, Jorgensen WL. Optimization of N-benzyl-benzoxazol-2-ones as receptor antagonists of macrophage migration inhibitory factor (MIF). Bioorganic & Medicinal Chemistry Letters 2010, 20: 5811-5814. PMID: 20728358, PMCID: PMC2939296, DOI: 10.1016/j.bmcl.2010.07.129.Peer-Reviewed Original ResearchConceptsMacrophage migration inhibitory factorCytokine macrophage migration inhibitory factorMigration inhibitory factorHuman synovial fibroblastsReceptor CD74Receptor antagonistSynovial fibroblastsInhibitory factorAdditional studiesERK1/2 phosphorylationCell proliferationTautomerase activityAntagonistPotent inhibitorBinding assaysInhibitorsAssaysInflammationCD74
2003
Molecular determinants of ligand interaction with the capsaicin receptor
Jordt S, Julius D. Molecular determinants of ligand interaction with the capsaicin receptor. Journal Of Neurochemistry 2003, 85: 4-4. DOI: 10.1046/j.1471-4159.85.s2.4_3.x.Peer-Reviewed Original ResearchReceptor homologPutative transmembrane regionsTransmembrane regionChemical modification studiesChimeric analysisPlasma membraneReceptor orthologsTransmembrane moietyStructural domainsMolecular determinantsChemical labelingIntracellular sideLigand binding assaysStructural determinantsLigand interactionsHomologPain-producing effectsBinding assaysModification studiesEndogenous ligandCapsaicin receptorReceptorsOrthologsMutagenesisBirds
1999
Relative cytotoxic activity of immunotoxins reactive with different epitopes on the extracellular domain of the c‐erbB‐2 (HER‐2/neu) gene product p185
Boyer C, Pusztai L, Wiener J, Xu F, Dean G, Bast B, O'Briant K, Greenwald M, DeSombre K, Bast R. Relative cytotoxic activity of immunotoxins reactive with different epitopes on the extracellular domain of the c‐erbB‐2 (HER‐2/neu) gene product p185. International Journal Of Cancer 1999, 82: 525-531. PMID: 10404066, DOI: 10.1002/(sici)1097-0215(19990812)82:4<525::aid-ijc10>3.0.co;2-j.Peer-Reviewed Original ResearchConceptsDifferent epitopesHER-2 receptorBreast cancer cell linesHER-2/neu geneRelative cytotoxic activityCytotoxic activityCancer cell linesEpitope targetsImmunotoxin therapyC-erbBImmunoglobulin isotypesUnconjugated antibodyEffective immunotoxinsExtracellular domainClonogenic assayImmunotoxinEpitope expressionNeu geneCompetitive binding assaysAntibodiesEpitopesAntibody bindingCell linesReceptorsBinding assaysCharacterization of the Neuronal Targeting Protein Spinophilin and Its Interactions with Protein Phosphatase-1 †
Hsieh-Wilson L, Allen P, Watanabe T, Nairn A, Greengard P. Characterization of the Neuronal Targeting Protein Spinophilin and Its Interactions with Protein Phosphatase-1 †. Biochemistry 1999, 38: 4365-4373. PMID: 10194355, DOI: 10.1021/bi982900m.Peer-Reviewed Original ResearchMeSH KeywordsAnimalsBinding SitesCell LineDopamine and cAMP-Regulated Phosphoprotein 32HumansMicrofilament ProteinsNerve Tissue ProteinsNeuronsPeptide FragmentsPeptidesPhosphoprotein PhosphatasesPhosphoproteinsProtein Phosphatase 1Protein Structure, TertiaryProteinsRabbitsSequence Homology, Amino AcidConceptsProtein phosphatase 1Ability of spinophilinPhosphatase 1PP1 regulatory subunitClass of proteinsAmino acids 447Cell cycle progressionPP1 activityPentapeptide motifRegulatory subunitCellular processesDeletion analysisDistinct subdomainsSubstrate specificityBinding domainsPhysiological substratesMutational analysisNeuronal proteinsProtein spinophilinCompetition binding assaysHigh-affinity binding domainsDARPP-32SpinophilinPostsynaptic densityBinding assays
1996
Rabies virus binding to the nicotinic acetylcholine receptor α subunit demonstrated by virus overlay protein binding assay
Gastka M, Horvath J, Lentz T. Rabies virus binding to the nicotinic acetylcholine receptor α subunit demonstrated by virus overlay protein binding assay. Journal Of General Virology 1996, 77: 2437-2440. PMID: 8887475, DOI: 10.1099/0022-1317-77-10-2437.Peer-Reviewed Original ResearchConceptsAlpha subunitNicotinic acetylcholine receptor α subunitAcetylcholine receptor α subunitElectric organ membranesVirus overlay proteinVirus overlay protein binding assaysTransfer of proteinsReceptor α subunitProtein binding assaysAChR alpha subunitOverlay proteinRabies virusΑ-subunitSubunitsGel electrophoresisAcetylcholine receptorsBinding assaysCuraremimetic neurotoxinsProteinMembraneVirusBindingAChRBlot
1995
Downregulation of Lck-mediated signal transduction by tip of herpesvirus saimiri
Jung J, Lang S, Jun T, Roberts T, Veillette A, Desrosiers R. Downregulation of Lck-mediated signal transduction by tip of herpesvirus saimiri. Journal Of Virology 1995, 69: 7814-7822. PMID: 7494293, PMCID: PMC189725, DOI: 10.1128/jvi.69.12.7814-7822.1995.Peer-Reviewed Original ResearchMeSH KeywordsBase SequenceCell LineCell Line, TransformedCloning, MolecularDNA PrimersElectrophoresis, Polyacrylamide GelGene ExpressionHerpesvirus 2, SaimiriineHumansLymphocyte Specific Protein Tyrosine Kinase p56(lck)Molecular Sequence DataMolecular WeightPhosphoproteinsPlasmidsPolymerase Chain ReactionRecombinant Fusion ProteinsSignal Transductionsrc-Family KinasesT-LymphocytesTumor Cells, CulturedViral ProteinsConceptsExpression of tipSignal transductionTyrosine phosphorylationT cell signal transductionCellular signal transductionCellular tyrosine phosphorylationHuman Jurkat T cell lineJurkat T cell lineJurkat T cellsInhibition of LckSH3 domainLckTransductionHerpesvirus saimiriFibroblast cellsPhosphorylationStable complexesSurface expressionBinding assaysComplex formationExpressionCellsAnti-CD3 stimulationT cellsB cellsAn astrocytic binding site for neuronal Thy-1 and its effect on neurite outgrowth.
Dreyer E, Leifer D, Heng J, McConnell J, Gorla M, Levin L, Barnstable C, Lipton S. An astrocytic binding site for neuronal Thy-1 and its effect on neurite outgrowth. Proceedings Of The National Academy Of Sciences Of The United States Of America 1995, 92: 11195-11199. PMID: 7479964, PMCID: PMC40598, DOI: 10.1073/pnas.92.24.11195.Peer-Reviewed Original ResearchConceptsNeurite outgrowthThy-1 functionsNeuronal Thy-1Thy-1Abundant glycoproteinMammalian neuronsNervous systemAnti-idiotype monoclonal antibodyCentral nervous system neuronsMonoclonal antibodiesBinding sitesCentral nervous systemAnti-idiotype antibodiesCertain monoclonal antibodiesBinding assaysCompetitive binding assaysProteinOutgrowthSystem neuronsDendritic developmentAntibodiesNeuronsSitesGlycoproteinCells
1994
The combinatorial synthesis and chemical and biological evaluation of a 1,4-benzodiazepine library.
Bunin B, Plunkett M, Ellman J. The combinatorial synthesis and chemical and biological evaluation of a 1,4-benzodiazepine library. Proceedings Of The National Academy Of Sciences Of The United States Of America 1994, 91: 4708-4712. PMID: 8197123, PMCID: PMC43857, DOI: 10.1073/pnas.91.11.4708.Peer-Reviewed Original ResearchConceptsLarge-scale synthesisLibrary of derivativesChemical functionalityBenzodiazepine derivativesCombinatorial synthesisChemical integrityBiological evaluationCarboxylic acidsActivity relationshipsDiverse derivativesDerivativesSynthesisDetailed structureAcidAminesRadio-ligand binding assayAmidesAmino acidsIndolePhenolBinding assaysChemicalsYieldStructure
1987
Characterization of protective and non-protective surface membrane carbohydrate epitopes of Schistosoma mansoni
Ko A, Harn D. Characterization of protective and non-protective surface membrane carbohydrate epitopes of Schistosoma mansoni. Memórias Do Instituto Oswaldo Cruz 1987, 82: 115-119. PMID: 2474123, DOI: 10.1590/s0074-02761987000800019.Peer-Reviewed Original ResearchConceptsKeyhole limpet hemocyaninNon-protective antibodiesMonoclonal antibodiesCarbohydrate epitopesProtective monoclonal antibodyEpitope mapping studiesDifferent carbohydrate epitopesLimpet hemocyaninSchistosomula antigensDifferent epitopesSchistosoma mansoniAntibodiesAntigenEpitopesImmunoprecipitation studiesBinding assaysInhibition studiesVaccineMansoni
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