2023
Screening for small molecule inhibitors of SAH nucleosidase using an SAH riboswitch
Sadeeshkumar H, Balaji A, Sutherland A, Mootien S, Anthony K, Breaker R. Screening for small molecule inhibitors of SAH nucleosidase using an SAH riboswitch. Analytical Biochemistry 2023, 666: 115047. PMID: 36682579, PMCID: PMC11149561, DOI: 10.1016/j.ab.2023.115047.Peer-Reviewed Original ResearchConceptsHigh-throughput screenAutoinducer-2Reporter geneBacterial processesEssential bacterial processesGram-negative bacterial cellsQuorum sensing signalsΒ-galactosidase reporter geneSmall molecule inhibitorsAntibiotic drug discoveryNatural riboswitchesAntimicrobial drug developmentRNA elementsPhysiological signalingRiboswitchBacterial cellsMolecule inhibitorsS-adenosylmethionineEscherichia coliCritical functionsNew targetsGenesDrug discoverySmall moleculesPromising target
2022
CD55 Facilitates Immune Evasion by Borrelia crocidurae, an Agent of Relapsing Fever
Arora G, Lynn GE, Tang X, Rosen CE, Hoornstra D, Sajid A, Hovius JW, Palm NW, Ring AM, Fikrig E. CD55 Facilitates Immune Evasion by Borrelia crocidurae, an Agent of Relapsing Fever. MBio 2022, 13: e01161-22. PMID: 36036625, PMCID: PMC9600505, DOI: 10.1128/mbio.01161-22.Peer-Reviewed Original ResearchConceptsRole of CD55Fever infectionImmune evasionSurface of erythrocytesRosette formationB. crociduraeB. persicaHost factorsBorrelia crociduraeAcute febrile illnessInflammatory cytokine levelsElevated proinflammatory cytokinesExpression of CD55Causative agentErythrocyte rosette formationFacilitates Immune EvasionComplement-mediated lysisHost-pathogen interactionsCytokine levelsFebrile illnessSignificant morbidityProinflammatory cytokinesHigh-throughput screenC5a levelsCD55 expression
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
2019
High-throughput screening identifies compounds that protect RPE cells from physiological stressors present in AMD
Cai H, Gong J, Abriola L, Hoyer D, Team N, Noggle S, Paull D, Del Priore LV, Fields MA. High-throughput screening identifies compounds that protect RPE cells from physiological stressors present in AMD. Experimental Eye Research 2019, 185: 107641. PMID: 30980814, DOI: 10.1016/j.exer.2019.04.009.Peer-Reviewed Original ResearchMeSH KeywordsAntifungal AgentsApoptosisBasement MembraneCatalaseCell LineCiclopiroxCytoprotectionEpoxide HydrolasesGene Expression Regulation, EnzymologicGlutathione TransferaseHigh-Throughput Screening AssaysHumansInduced Pluripotent Stem CellsMacular DegenerationNitrosative StressOxidative StressPeroxiredoxin IIIReal-Time Polymerase Chain ReactionRetinal Pigment Epitheliumtert-ButylhydroperoxideUltraviolet RaysConceptsHigh-throughput screenHuman RPE cellsAtrophic age-related macular degenerationPrimary human RPE cellsMitochondrial functionStress-induced cell deathARPE-19Oxidative stress-induced cell deathExtracellular matrixTert-butyl hydroperoxide exposureRPE cellsOxidative damageExpression of genesInduced-pluripotent stem cellsOxidative stressSeahorse XF96 analyzerApoptosis-related genesCell viabilityGene expressionXF96 analyzerCell deathRetinal pigment epithelial cellsQuantitative reverse transcription polymerase chain reactionCiclopirox olaminePigment epithelial cells
2016
Gaucher disease: Progress and ongoing challenges
Mistry PK, Lopez G, Schiffmann R, Barton NW, Weinreb NJ, Sidransky E. Gaucher disease: Progress and ongoing challenges. Molecular Genetics And Metabolism 2016, 120: 8-21. PMID: 27916601, PMCID: PMC5425955, DOI: 10.1016/j.ymgme.2016.11.006.Peer-Reviewed Original ResearchConceptsGaucher diseaseFirst mutant allelePluripotent stem cell modelsInduced Pluripotent Stem Cell ModelStem cell modelImportant risk factorHigh-throughput screenEnzyme replacement therapyNational InstituteLysosomal enzyme glucocerebrosidaseRecombinant productionReplacement therapyMutant allelesClinical centersRisk factorsMouse modelThroughput screenIdentification of small-molecule inhibitors of Zika virus infection and induced neural cell death via a drug repurposing screen
Xu M, Lee E, Wen Z, Cheng Y, Huang W, Qian X, TCW J, Kouznetsova J, Ogden S, Hammack C, Jacob F, Nguyen H, Itkin M, Hanna C, Shinn P, Allen C, Michael S, Simeonov A, Huang W, Christian K, Goate A, Brennand K, Huang R, Xia M, Ming G, Zheng W, Song H, Tang H. Identification of small-molecule inhibitors of Zika virus infection and induced neural cell death via a drug repurposing screen. Nature Medicine 2016, 22: 1101-1107. PMID: 27571349, PMCID: PMC5386783, DOI: 10.1038/nm.4184.Peer-Reviewed Original Research
2011
Drug Repositioning and Pharmacophore Identification in the Discovery of Hookworm MIF Inhibitors
Cho Y, Vermeire JJ, Merkel JS, Leng L, Du X, Bucala R, Cappello M, Lolis E. Drug Repositioning and Pharmacophore Identification in the Discovery of Hookworm MIF Inhibitors. Cell Chemical Biology 2011, 18: 1089-1101. PMID: 21944748, PMCID: PMC3294498, DOI: 10.1016/j.chembiol.2011.07.011.Peer-Reviewed Original ResearchMeSH KeywordsAncylostomatoideaAnimalsAnti-Inflammatory Agents, Non-SteroidalBinding SitesCatalytic DomainCrystallography, X-RayDiureticsDrug RepositioningFurosemideHigh-Throughput Screening AssaysHookworm InfectionsHumansKineticsMacrophage Migration-Inhibitory FactorsMeclofenamic AcidSmall Molecule LibrariesConceptsNonsteroidal anti-inflammatory drugsMacrophage migration inhibitory factorMigration inhibitory factorAnti-inflammatory drugsIntestinal nematode parasitesSodium meclofenamateHigh-throughput screenMIF inhibitorsAnimal modelsTherapeutic efficacyBioactive compound librariesInhibitory factorHookworm diseaseDiuretic activityPartial protectionTautomerase activityFurosemideDiseaseDrugsFDADrug repositioningSubmicromolar inhibitionInhibitorsNew pharmacophoreDiuretics
2009
Chemical modifier screen identifies HDAC inhibitors as suppressors of PKD models
Cao Y, Semanchik N, Lee SH, Somlo S, Barbano PE, Coifman R, Sun Z. Chemical modifier screen identifies HDAC inhibitors as suppressors of PKD models. Proceedings Of The National Academy Of Sciences Of The United States Of America 2009, 106: 21819-21824. PMID: 19966229, PMCID: PMC2799791, DOI: 10.1073/pnas.0911987106.Peer-Reviewed Original ResearchConceptsKidney cyst formationCommon human genetic diseasesLarge-scale high-throughput screensHDAC inhibitorsBody curvatureChemical modifier screensHuman genetic diseasesPolycystic kidney diseaseHigh-throughput screenModifier screenSpecific HDAC inhibitorsCyst formationClass I HDACsCausal genesKnockdown animalsCiliary signalsPKD pathogenesisPan-HDAC inhibitorsPKD modelLaterality defectsGenetic diseasesPKD treatmentZebrafishAutosomal dominant polycystic kidney diseaseDrug candidatesAn AlphaScreen™-Based High-Throughput Screen to Identify Inhibitors of Hsp90-Cochaperone Interaction
Yi F, Zhu P, Southall N, Inglese J, Austin CP, Zheng W, Regan L. An AlphaScreen™-Based High-Throughput Screen to Identify Inhibitors of Hsp90-Cochaperone Interaction. SLAS DISCOVERY 2009, 14: 273-281. PMID: 19211782, PMCID: PMC3066041, DOI: 10.1177/1087057108330114.Peer-Reviewed Original ResearchConceptsImportant anticancer drug targetFirst high-throughput screenHigh-throughput screenChemical probesNovel anticancer drugsAnticancer drug targetSuch moleculesAnticancer drugsTPR2A domainDifferent interactionsCompoundsSmall molecule Hsp90 inhibitorsNovel typeSynthetic peptidesFurther optimizationDrug targetsC-terminal peptideAlphaScreen technologyPeptidesDMSOReported valuesMoleculesInteractionHsp90 inhibitorsBackground ratio
2002
Evolutionary Rate in the Protein Interaction Network
Fraser HB, Hirsh AE, Steinmetz LM, Scharfe C, Feldman MW. Evolutionary Rate in the Protein Interaction Network. Science 2002, 296: 750-752. PMID: 11976460, DOI: 10.1126/science.1068696.Peer-Reviewed Original ResearchConceptsProtein interaction networksInteraction networksMost cellular functionsRate of evolutionHigh-throughput screenMolecular evolutionEvolutionary ratesYeast SaccharomycesCellular functionsEvolutionary changeSelection pressureProtein resultsProteinMore interactorsInteractorsFundamental questionsSaccharomycesCoevolutionEvolutionOrganismsReciprocal changesFunctionSimilar ratesGreater proportionScreen
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