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
2010
Allosteric inhibition of macrophage migration inhibitory factor revealed by ibudilast
Cho Y, Crichlow GV, Vermeire JJ, Leng L, Du X, Hodsdon ME, Bucala R, Cappello M, Gross M, Gaeta F, Johnson K, Lolis EJ. Allosteric inhibition of macrophage migration inhibitory factor revealed by ibudilast. Proceedings Of The National Academy Of Sciences Of The United States Of America 2010, 107: 11313-11318. PMID: 20534506, PMCID: PMC2895110, DOI: 10.1073/pnas.1002716107.Peer-Reviewed Original ResearchConceptsMacrophage migration inhibitory factorMigration inhibitory factorInhibitory factorPeripheral blood mononuclear cellsBlood mononuclear cellsNeuropathic painOpioid withdrawalMIF receptorBronchial asthmaOcular indicationsMononuclear cellsProinflammatory proteinsAntiinflammatory drugsGlial cellsPossible therapeuticsAntiinflammatory activityChemotactic functionNonselective inhibitorAV411Major receptorTautomerase activityReceptorsAllosteric binding siteAntibody experimentsTreatmentAV411 (Ibudilast) and AV1013 are non-competitive inhibitors of macrophage migration inhibitory factor: a novel induced-fit allosteric inhibition mechanism (133.11)
Cho Y, Crichlow G, Vermeire J, Leng L, Du X, Hodsdon M, Bucala R, Cappello M, Gross M, Gaeta F, Johnson K, Lolis E. AV411 (Ibudilast) and AV1013 are non-competitive inhibitors of macrophage migration inhibitory factor: a novel induced-fit allosteric inhibition mechanism (133.11). The Journal Of Immunology 2010, 184: 133.11-133.11. DOI: 10.4049/jimmunol.184.supp.133.11.Peer-Reviewed Original ResearchMacrophage migration inhibitory factorMigration inhibitory factorInhibitory factorPro-inflammatory proteinsAnti-inflammatory activityAnti-inflammatory drugsNon-selective inhibitorPDE inhibitor rolipramNeuropathic painOpioid withdrawalBronchial asthmaOcular indicationsGlial cellsNon-competitive inhibitorPossible therapeuticsInhibitor rolipramChemotactic functionAV411Tautomerase activityInhibitorsAllosteric binding siteIsobutylmethylxanthineTreatmentAsthmaPain
2007
Structural and Functional Characterization of a Secreted Hookworm Macrophage Migration Inhibitory Factor (MIF) That Interacts with the Human MIF Receptor CD74*
Cho Y, Jones BF, Vermeire JJ, Leng L, DiFedele L, Harrison LM, Xiong H, Kwong YK, Chen Y, Bucala R, Lolis E, Cappello M. Structural and Functional Characterization of a Secreted Hookworm Macrophage Migration Inhibitory Factor (MIF) That Interacts with the Human MIF Receptor CD74*. Journal Of Biological Chemistry 2007, 282: 23447-23456. PMID: 17567581, PMCID: PMC3707627, DOI: 10.1074/jbc.m702950200.Peer-Reviewed Original ResearchMeSH KeywordsAmino Acid SequenceAncylostomaAnimalsAntigens, Differentiation, B-LymphocyteCricetinaeCytokinesHistocompatibility Antigens Class IIHumansIntestinal MucosaMacrophage Migration-Inhibitory FactorsMesocricetusMolecular Sequence DataProtein BindingRabbitsRecombinant ProteinsSequence Homology, Amino AcidConceptsMacrophage migration inhibitory factorMIF receptor CD74Migration inhibitory factorReceptor CD74Inhibitory factorHost immune responseHuman macrophage migration inhibitory factorMIF proteinHookworm Ancylostoma ceylanicumImmune responseDisease pathogenesisHuman cytokinesMacrophage migrationAncylostoma ceylanicumMajor causeWorm survivalParasite survivalISO-1Significant differencesTautomerase activityHookworm proteinsCytokinesCD74HookwormRelative bioactivity