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dc.contributor.authorRajput, Vishal K
dc.contributor.authorMacKinnon, Alison
dc.contributor.authorMandal, Santanu
dc.contributor.authorCollins, Patrick
dc.contributor.authorBlanchard, Helen
dc.contributor.authorLeffler, Hakon
dc.contributor.authorSethi, Tariq
dc.contributor.authorSchambye, Hans
dc.contributor.authorMukhopadhyay, Balaram
dc.contributor.authorNilsson, Ulf J
dc.date.accessioned2017-11-27T04:45:46Z
dc.date.available2017-11-27T04:45:46Z
dc.date.issued2016
dc.identifier.issn0022-2623
dc.identifier.doi10.1021/acs.jmedchem.6b00957
dc.identifier.urihttp://hdl.handle.net/10072/100256
dc.description.abstractSynthesis of doubly 3-O-coumarylmethyl-substituted thiodigalactosides from bis-3-O-propargyl-thiodigalactoside resulted in highly selective and high affinity galectin-3 inhibitors. Mutant studies, structural analysis, and molecular modeling revealed that the coumaryl substituents stack onto arginine side chains. One inhibitor displayed efficacy in a murine model of bleomycin-induced lung fibrosis similar to that of a known nonselective galectin-1/galectin-3 inhibitor, which strongly suggests that blocking galectin-3 glycan recognition is an important antifibrotic drug target.
dc.description.peerreviewedYes
dc.languageEnglish
dc.language.isoeng
dc.publisherAmerican Chemical Society
dc.relation.ispartofpagefrom8141
dc.relation.ispartofpageto8147
dc.relation.ispartofjournalJournal of Medicinal Chemistry
dc.relation.ispartofvolume59
dc.subject.fieldofresearchMedicinal and Biomolecular Chemistry not elsewhere classified
dc.subject.fieldofresearchMedicinal and Biomolecular Chemistry
dc.subject.fieldofresearchOrganic Chemistry
dc.subject.fieldofresearchPharmacology and Pharmaceutical Sciences
dc.subject.fieldofresearchcode030499
dc.subject.fieldofresearchcode0304
dc.subject.fieldofresearchcode0305
dc.subject.fieldofresearchcode1115
dc.titleA Selective Galactose–Coumarin-Derived Galectin-3 Inhibitor Demonstrates Involvement of Galectin-3-glycan Interactions in a Pulmonary Fibrosis Model
dc.typeJournal article
dc.type.descriptionC1 - Articles
dc.type.codeC - Journal Articles
gro.hasfulltextNo Full Text
gro.griffith.authorCollins, Patrick
gro.griffith.authorBlanchard, Helen


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