2013
Peroxiredoxin-1 from the Human Hookworm Ancylostoma ceylanicum Forms a Stable Oxidized Decamer and Is Covalently Inhibited by Conoidin A
Nguyen JB, Pool CD, Wong CY, Treger RS, Williams DL, Cappello M, Lea WA, Simeonov A, Vermeire JJ, Modis Y. Peroxiredoxin-1 from the Human Hookworm Ancylostoma ceylanicum Forms a Stable Oxidized Decamer and Is Covalently Inhibited by Conoidin A. Cell Chemical Biology 2013, 20: 991-1001. PMID: 23891152, PMCID: PMC3755041, DOI: 10.1016/j.chembiol.2013.06.011.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
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 experimentsTreatment
2008
A Leishmania Ortholog of Macrophage Migration Inhibitory Factor Modulates Host Macrophage Responses
Kamir D, Zierow S, Leng L, Cho Y, Diaz Y, Griffith J, McDonald C, Merk M, Mitchell RA, Trent J, Chen Y, Kwong YK, Xiong H, Vermeire J, Cappello M, McMahon-Pratt D, Walker J, Bernhagen J, Lolis E, Bucala R. A Leishmania Ortholog of Macrophage Migration Inhibitory Factor Modulates Host Macrophage Responses. The Journal Of Immunology 2008, 180: 8250-8261. PMID: 18523291, PMCID: PMC2668862, DOI: 10.4049/jimmunol.180.12.8250.Peer-Reviewed Original ResearchMeSH KeywordsAmino Acid SequenceAnimalsAntigens, Differentiation, B-LymphocyteApoptosis Regulatory ProteinsCell LineCells, CulturedCrystallography, X-RayHistocompatibility Antigens Class IIHumansIntramolecular OxidoreductasesLeishmania majorMacrophage Migration-Inhibitory FactorsMacrophages, PeritonealMiceMice, Inbred BALB CMice, Inbred C3HMice, KnockoutMolecular Sequence DataRecombinant ProteinsStructural Homology, ProteinConceptsMacrophage migration inhibitory factorCD74-dependent mannerMigration inhibitory factorImmune defense mechanismsHuman macrophage migration inhibitory factorSmall molecule antagonistsActivation-induced apoptosisHost macrophage responseMIF receptorMIF proteinImmune destructionObligate intracellular parasitesMAP kinase activationERK1/2 MAP kinase activationInhibitory factorMacrophage responseLeishmania majorIntracellular parasitesHigh-resolution X-ray crystal structuresSpecies-specific inhibitionMacrophagesSignificant structural homologyKinase activationDefense mechanismsMammalian counterparts