2023
Updates on risk stratification and management of lower-risk myelodysplastic syndromes/neoplasms
Badar T, Madanat Y, Zeidan A. Updates on risk stratification and management of lower-risk myelodysplastic syndromes/neoplasms. Future Oncology 2023, 19: 1877-1889. PMID: 37750305, DOI: 10.2217/fon-2023-0454.Peer-Reviewed Reviews, Practice Guidelines, Standards, and Consensus StatementsErythropoiesis-stimulating agentsTreatment-naive patientsHigh-risk patientsMeaningful efficacyIndolent courseDismal prognosisRandomized trialsRisk stratificationNeoplasm patientsSerial monitoringClinical trialsNovel therapiesPatientsAppropriate managementModest responseGood responseNeoplasmsTrialsNovel compoundsLuspaterceptLenalidomidePrognosisAnemiaTherapyMore needs
2021
Wet-dry-wet drug screen leads to the synthesis of TS1, a novel compound reversing lung fibrosis through inhibition of myofibroblast differentiation
Ring NAR, Volpe MC, Stepišnik T, Mamolo MG, Panov P, Kocev D, Vodret S, Fortuna S, Calabretti A, Rehman M, Colliva A, Marchesan P, Camparini L, Marcuzzo T, Bussani R, Scarabellotto S, Confalonieri M, Pham TX, Ligresti G, Caporarello N, Loffredo FS, Zampieri D, Džeroski S, Zacchigna S. Wet-dry-wet drug screen leads to the synthesis of TS1, a novel compound reversing lung fibrosis through inhibition of myofibroblast differentiation. Cell Death & Disease 2021, 13: 2. PMID: 34916483, PMCID: PMC8677786, DOI: 10.1038/s41419-021-04439-4.Peer-Reviewed Original ResearchConceptsAnti-fibrotic effectsDopamine receptor 3Lung fibrosisMyofibroblast activationReceptor 3Idiopathic pulmonary fibrosis patientsMyofibroblast differentiationPulmonary fibrosis patientsProgression of fibrosisTransforming Growth Factor-β PathwayGrowth factor β pathwayHigh-throughput screenDisease progressionMurine modelFibrosisFibrosis patientsFibrotic diseasesDrug screensLung fibroblastsNovel compoundsProgressionΒ pathwayImportant targetDopaminePrimary fibroblasts
2015
Polysulfated Trehalose as a Novel Anticoagulant Agent with Dual Mode of Action
Rashid Q, Abid M, Gupta N, Tyagi T, Ashraf M, Jairajpuri M. Polysulfated Trehalose as a Novel Anticoagulant Agent with Dual Mode of Action. BioMed Research International 2015, 2015: 630482. PMID: 25866798, PMCID: PMC4381846, DOI: 10.1155/2015/630482.Peer-Reviewed Original ResearchConceptsFavorable safety profileNovel anticoagulant agentsForm of heparinAnticoagulant administrationSafety profileAntithrombotic agentsAnticoagulant agentsAnticoagulant factorsHemostatic balanceAntithrombotic potentialLow doseAntiplatelet mechanismFibrinolytic systemPlatelet aggregationThrombotic ratsFirst lineHeparinCoagulation timeRatsBlood plasmaNovel compoundsThromboembolismComplicationsAnticoagulantsTherapy
2005
A Close Structural Analog of 2-Methyl-6-(phenylethynyl)-pyridine Acts as a Neutral Allosteric Site Ligand on Metabotropic Glutamate Receptor Subtype 5 and Blocks the Effects of Multiple Allosteric Modulators
Rodriguez A, Nong Y, Sekaran N, Alagille D, Tamagnan G, Conn P. A Close Structural Analog of 2-Methyl-6-(phenylethynyl)-pyridine Acts as a Neutral Allosteric Site Ligand on Metabotropic Glutamate Receptor Subtype 5 and Blocks the Effects of Multiple Allosteric Modulators. Molecular Pharmacology 2005, 68: 1793-1802. PMID: 16155210, DOI: 10.1124/mol.105.016139.Peer-Reviewed Original ResearchConceptsMetabotropic glutamate receptor subtype 5Subtype 5Allosteric siteG protein-coupled receptorsProtein-coupled receptorsMajor excitatory neurotransmitterCentral nervous systemMPEP siteAntagonist MPEPBinding of glutamateOnly partial inhibitionExcitatory neurotransmitterSubthalamic nucleusCalcium mobilizationNervous systemSite ligandsAllosteric modulatorsPartial antagonistValuable new toolNovel compoundsValuable new insightsOrthosteric ligandsAllosteric modulationFunctional effectsNative systemsGABA and glutamate systems as therapeutic targets in depression and mood disorders
Kendell SF, Krystal JH, Sanacora G. GABA and glutamate systems as therapeutic targets in depression and mood disorders. Expert Opinion On Therapeutic Targets 2005, 9: 153-168. PMID: 15757488, DOI: 10.1517/14728222.9.1.153.Peer-Reviewed Original Research
2004
Report from the Society for Biological Therapy and Vascular Biology Faculty of the NCI Workshop on Angiogenesis Monitoring
McDonald DM, Teicher BA, Stetler-Stevenson W, Ng SS, Figg WD, Folkman J, Hanahan D, Auerbach R, O’Reilly M, Herbst R, Cheresh D, Gordon M, Eggermont A, Libutti SK. Report from the Society for Biological Therapy and Vascular Biology Faculty of the NCI Workshop on Angiogenesis Monitoring. Journal Of Immunotherapy 2004, 27: 161-175. PMID: 14770088, DOI: 10.1097/00002371-200403000-00010.Peer-Reviewed Original Research
2002
Synthesis, Receptor Potency, and Selectivity of Halogenated Diphenylpiperidines as Serotonin 5-HT2A Ligands for PET or SPECT Brain Imaging
Fu X, Tan P, Kula N, Baldessarini R, Tamagnan G, Innis R, Baldwin R. Synthesis, Receptor Potency, and Selectivity of Halogenated Diphenylpiperidines as Serotonin 5-HT2A Ligands for PET or SPECT Brain Imaging. Journal Of Medicinal Chemistry 2002, 45: 2319-2324. PMID: 12014970, DOI: 10.1021/jm0200411.Peer-Reviewed Original ResearchMeSH KeywordsAnimalsCOS CellsHumansIn Vitro TechniquesLigandsPiperidinesProsencephalonRadioligand AssayRatsReceptor, Serotonin, 5-HT2AReceptor, Serotonin, 5-HT2CReceptors, Adrenergic, alpha-1Receptors, Adrenergic, alpha-2Receptors, Dopamine D2Receptors, SerotoninStructure-Activity RelationshipTomography, Emission-ComputedTomography, Emission-Computed, Single-Photon
1988
Triticone A: A novel bioactive lactam with potential as a molecular probe
Kenfield D, Strobel S, Sugawara F, Berglund D, Strobel G. Triticone A: A novel bioactive lactam with potential as a molecular probe. Biochemical And Biophysical Research Communications 1988, 157: 174-182. PMID: 3196330, DOI: 10.1016/s0006-291x(88)80029-9.Peer-Reviewed Original ResearchConceptsPlant pathogenic fungiMolecular probesProtoplast assaysSH functional groupsCO2 fixation reactionWheat cellsPathogenic fungiPhysiological functionsSpirocyclic lactamsFunctional groupsActive siteEnantiomeric mixturesNovel compoundsFluorescein diacetateBiological activityFixation reactionBiological systemsAccurate quantitationLactamsPhotosynthesisProtoplastsChlorosisFungiPlantsWheat
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