2025
PET Mapping of Receptor Occupancy Using Joint Direct Parametric Reconstruction
Marin T, Belov V, Chemli Y, Ouyang J, Najmaoui Y, Fakhri G, Duvvuri S, Iredale P, Guehl N, Normandin M, Petibon Y. PET Mapping of Receptor Occupancy Using Joint Direct Parametric Reconstruction. IEEE Transactions On Biomedical Engineering 2025, 72: 1057-1066. PMID: 39446540, PMCID: PMC11875991, DOI: 10.1109/tbme.2024.3486191.Peer-Reviewed Original ResearchCentral nervous systemReceptor occupancyLow-binding regionsPET scansSimulation resultsPreclinical in vivo experimentsDynamic PET scansPairs of baselineEstimation of receptor occupancyEstimation frameworkPET neuroimagingReconstruction frameworkModulating drugsTime activity curvesParametric reconstructionDevelopment of drugsVoltage-gated sodium channels in excitable cells as drug targets
Alsaloum M, Dib-Hajj S, Page D, Ruben P, Krainer A, Waxman S. Voltage-gated sodium channels in excitable cells as drug targets. Nature Reviews Drug Discovery 2025, 1-21. PMID: 39901031, DOI: 10.1038/s41573-024-01108-x.Peer-Reviewed Original ResearchSodium channelsChannel subtypesControl action potential firingDevelopment of drugsDensity of voltage-gated sodiumExcitable cellsAction potential firingSubtype-specific drugsSodium channel subtypesVoltage-gated sodium channelsExpressing high densitiesVoltage-gated sodiumCardiac myocytesNav1.1-Nav1.9Potential firingCardiac disordersAction potentialsMuscle cellsMolecular targetsDrugSubtypesDrug developmentCellsDrug targetsMyocytes
2020
Gastrointestinal tissue‐based molecular biomarkers: a practical categorisation based on the 2019 World Health Organization classification of epithelial digestive tumours
Quezada‐Marín J, Lam A, Ochiai A, Odze R, Washington K, Fukayama M, Rugge M, Klimstra D, Nagtegaal I, Tan P, Arends M, Goldblum J, Cree I, Salto‐Tellez M. Gastrointestinal tissue‐based molecular biomarkers: a practical categorisation based on the 2019 World Health Organization classification of epithelial digestive tumours. Histopathology 2020, 77: 340-350. PMID: 32320495, DOI: 10.1111/his.14120.Peer-Reviewed Original ResearchConceptsWorld Health Organization classificationWorld Health Organization Classification of TumorsMolecular biomarkersClassification of tumorsEpithelial neoplasmsDigestive tumorsRoutine diagnosticsDevelopment of drugsOncological pathologyArtificial intelligence toolsTumorIntelligence toolsBiomarkersMethod of classification
2019
Role of a patatin-like phospholipase in Plasmodium falciparum gametogenesis and malaria transmission
Singh P, Alaganan A, More K, Lorthiois A, Thiberge S, Gorgette O, Guillotte Blisnick M, Guglielmini J, Aguilera S, Touqui L, Singh S, Chitnis C. Role of a patatin-like phospholipase in Plasmodium falciparum gametogenesis and malaria transmission. Proceedings Of The National Academy Of Sciences Of The United States Of America 2019, 116: 17498-17508. PMID: 31413195, PMCID: PMC6717283, DOI: 10.1073/pnas.1900266116.Peer-Reviewed Original ResearchConceptsFemale gametesPerforin-like proteinBlood-stage growthIngestion of gametocytesProcess of gametogenesisPatatin-like phospholipaseGamete egressDiverse organismsMembrane remodelingIntracellular vesiclesVesicle secretionVesicular dischargeMale gametesOocyst formationPeripheral membraneGametocyte developmentGametogenesisExtensive membraneConditional deletionGametesBlood mealDevelopment of drugsDeletionPotential targetGenesEvaluation of 11C-LSN3172176 as a Novel PET Tracer for Imaging M1 Muscarinic Acetylcholine Receptors in Nonhuman Primates
Nabulsi NB, Holden D, Zheng MQ, Bois F, Lin SF, Najafzadeh S, Gao H, Ropchan J, Lara-Jaime T, Labaree D, Shirali A, Slieker L, Jesudason C, Barth V, Navarro A, Kant N, Carson RE, Huang Y. Evaluation of 11C-LSN3172176 as a Novel PET Tracer for Imaging M1 Muscarinic Acetylcholine Receptors in Nonhuman Primates. Journal Of Nuclear Medicine 2019, 60: 1147-1153. PMID: 30733324, DOI: 10.2967/jnumed.118.222034.Peer-Reviewed Original ResearchConceptsMuscarinic acetylcholine receptorsAcetylcholine receptorsNonhuman primatesM1 muscarinic acetylcholine receptorBrain time-activity curvesRich brain regionsArterial blood samplingNovel PET tracersSuitable reference regionRegional distribution volumesReference regionDevelopment of drugsBrain uptakeGlobus pallidusDistribution volume valuesNucleus accumbensBlood samplingPET scansTime-activity curvesCognitive impairmentAlzheimer's diseaseBrain regionsDistribution volumeSelective radiotracerRhesus monkeys
2017
Targeted drugs and diagnostic assays: Companions in the race to combat ethnic disparity.
Wright N, Rida P, Krishnamurti U, Li X, Aneja R. Targeted drugs and diagnostic assays: Companions in the race to combat ethnic disparity. Frontiers In Bioscience-Landmark 2017, 22: 193-211. PMID: 27814611, DOI: 10.2741/4481.Peer-Reviewed Original ResearchConceptsEthnic disparitiesAfrican AmericansAggressive breast cancer subtypeUnique tumor biologyBreast cancer subtypesPrecision medicine toolsDiagnostic assaysIndividualized cancer treatmentRacial health disparitiesClinical outcomesDevelopment of drugsPatient populationAncestry-associated differencesEfficacy biomarkersTargeted drugsHigh recurrenceMortality rateCentrosomal aberrationsBreast tumorsTumor biologyCancer subtypesHealth disparitiesMedicine toolsCancer treatmentPersonalized oncology
2016
Epigenetic therapy in gastrointestinal cancer: the right combination
Abdelfatah E, Kerner Z, Nanda N, Ahuja N. Epigenetic therapy in gastrointestinal cancer: the right combination. Therapeutic Advances In Gastroenterology 2016, 9: 560-579. PMID: 27366224, PMCID: PMC4913338, DOI: 10.1177/1756283x16644247.Peer-Reviewed Original ResearchDNA methyltransferaseEpigenetic dysregulationEpigenetic drugsEpigenetic therapyCpG island methylator phenotypeDeoxyribonucleic acid methylationChromatin remodelingHistone modificationsCancer epigenomeEpigenetic reprogrammingWidespread epigenetic dysregulationCancer epigeneticsEpigenetic targetsCancer stem cellsHistone deacetylase inhibitorsMolecular biologyAcid methylationStem cellsDeacetylase inhibitorsDevelopment of drugsEpigeneticsGenetic mutationsMethylator phenotypeChemo resistanceEpigenetic sensitization
2012
Unraveling the autoimmune translational research process layer by layer
Blumberg RS, Dittel B, Hafler D, von Herrath M, Nestle FO. Unraveling the autoimmune translational research process layer by layer. Nature Medicine 2012, 18: 35-41. PMID: 22227670, PMCID: PMC4592149, DOI: 10.1038/nm.2632.Peer-Reviewed Original Research
2009
Cytisine-Based Nicotinic Partial Agonists as Novel Antidepressant Compounds
Mineur YS, Eibl C, Young G, Kochevar C, Papke RL, Gündisch D, Picciotto MR. Cytisine-Based Nicotinic Partial Agonists as Novel Antidepressant Compounds. Journal Of Pharmacology And Experimental Therapeutics 2009, 329: 377-386. PMID: 19164465, PMCID: PMC2670591, DOI: 10.1124/jpet.108.149609.Peer-Reviewed Original ResearchMeSH KeywordsAlkaloidsAnimalsAntidepressive AgentsAzocinesCloning, MolecularData Interpretation, StatisticalElectrophysiologyEnvironmentFeeding BehaviorHindlimb SuspensionLaburnumMaleMiceMice, Inbred C57BLMotor ActivityNicotinic AgonistsOocytesPatch-Clamp TechniquesQuinolizinesReceptors, CholinergicSwimmingXenopus laevisConceptsAntidepressant-like effectsAntidepressant-like propertiesNicotinic partial agonistPartial agonistAntidepressant efficacyDose-dependent antidepressant-like effectNovelty-suppressed feeding testC57/BL6 miceBeta2 nAChRsAntidepressant-like activityTail suspension testBlood-brain barrierSelective partial agonistNicotinic acetylcholine receptorsNovel antidepressantsDevelopment of drugsBL6 miceAlpha3/beta4Alpha7 nAChRsAgonist effectsMood disordersRodent modelsSuspension testTail suspensionMouse model
2005
Phosphoproteomics for oncology discovery and treatment
Stern DF. Phosphoproteomics for oncology discovery and treatment. Expert Opinion On Therapeutic Targets 2005, 9: 851-860. PMID: 16083347, DOI: 10.1517/14728222.9.4.851.Peer-Reviewed Original ResearchConceptsPhosphoproteomic analysisProtein phosphorylationReversible protein phosphorylationSignal transduction pathwaysCellular regulationProtein kinaseTransduction pathwaysHuman cancersDevelopment of drugsPathwayPhosphorylationGood targetImportant insightsCancer therapyCancer drugsPhosphoproteomicsCellsIndividual tumorsPowerful toolKinaseRegulationIntermediary levelDiscoveryTargetIdentificationKv1.3 potassium channel blockade as an approach to insulin resistance
Desir GV. Kv1.3 potassium channel blockade as an approach to insulin resistance. Expert Opinion On Therapeutic Targets 2005, 9: 571-579. PMID: 15948674, DOI: 10.1517/14728222.9.3.571.Peer-Reviewed Original ResearchConceptsInsulin resistanceInsulin sensitivityKv1.3 channel inhibitionPotassium channel blockadePeripheral insulin sensitivityPotential therapeutic targetDevastating metabolic diseaseType II diabetesVoltage-gated potassium channelsAbnormal glucoseDiabetes mellitusInsulin deficiencyDevelopment of drugsInflammatory cytokinesChannel blockadeGlucose metabolismTherapeutic targetCardinal featuresMetabolic diseasesChannel inhibitionII diabetesLipid metabolismHealthcare expendituresPotassium channelsPromising target
2000
Selective Inhibition of NF-κB Activation by a Peptide That Blocks the Interaction of NEMO with the IκB Kinase Complex
May M, D'Acquisto F, Madge L, Glöckner J, Pober J, Ghosh S. Selective Inhibition of NF-κB Activation by a Peptide That Blocks the Interaction of NEMO with the IκB Kinase Complex. Science 2000, 289: 1550-1554. PMID: 10968790, DOI: 10.1126/science.289.5484.1550.Peer-Reviewed Original ResearchMeSH KeywordsAmino Acid SequenceAnimalsAnti-Inflammatory Agents, Non-SteroidalCells, CulturedCOS CellsEndothelium, VascularE-SelectinGene Expression RegulationHeLa CellsHumansI-kappa B KinaseInflammationMiceMice, Inbred C57BLMolecular Sequence DataMutationNF-kappa BPeptidesPoint MutationProtein Serine-Threonine KinasesProtein Structure, TertiaryRecombinant Fusion ProteinsConceptsNF-kappaBBasal NF-kappaB activityExperimental mouse modelTranscription factor nuclear factorCytokine-induced NF-kappaB activationCell-permeable NBD peptideInhibitor of kappaBNF-κB activationNF-kappaB activityNF-kappaB activationAssociation of NEMOIKK complexAcute inflammationDevelopment of drugsProinflammatory activationInflammatory responseNBD peptideMouse modelProinflammatory stimuliIκB kinase (IKK) complexNuclear factorRegulatory protein NEMOInflammationSelective inhibitionExpression of genes
1993
The Therapeutic Potential of Neurotrophic Factors in the Treatment of Parkinson's Disease
Lindsay R, Altar C, Cedarbaum J, Hyman C, Wiegand S. The Therapeutic Potential of Neurotrophic Factors in the Treatment of Parkinson's Disease. Experimental Neurology 1993, 124: 103-118. PMID: 8282068, DOI: 10.1006/exnr.1993.1181.Peer-Reviewed Original ResearchConceptsNeurotrophic factorParkinson's diseaseNeurodegenerative disordersTherapeutic agentsNeurodegenerative diseasesFetal nigral graftsTransplantation of neuronsDopamine neurotrophic factorPartial symptomatic reliefDopamine receptor agonistsNeurotrophic growth factorsPotential clinical useHuman neurodegenerative disordersAppropriate neurotransmittersObvious therapeutic strategyNeuronal lossNigral graftsSymptomatic reliefDevelopment of drugsDopaminergic neuronsNeuroprotective agentsSubstantia nigraNeuronal degenerationNeurotrophin familyDopamine neurons
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