Show simple item record

dc.contributor.authorCollins, Patrick M
dc.contributor.authorOberg, Christopher T
dc.contributor.authorLeffler, Hakon
dc.contributor.authorNilsson, Ulf J
dc.contributor.authorBlanchard, Helen
dc.date.accessioned2017-05-03T14:15:06Z
dc.date.available2017-05-03T14:15:06Z
dc.date.issued2012
dc.date.modified2013-06-17T23:11:40Z
dc.identifier.issn1747-0277
dc.identifier.doi10.1111/j.1747-0285.2011.01283.x
dc.identifier.urihttp://hdl.handle.net/10072/48684
dc.description.abstractGalectin-1 and galectin-3 have roles in cancer and inflammation. Galectin-1 has recently emerged as a significant protein produced by tumour cells to promote tumour development, angiogenesis and metastasis and consequently represents an impor- tant target to inhibit. The design of inhibitors tar- geting the carbohydrate recognition domain that is known to recognize galactose is an important approach in the fight against cancer. Based on the analysis of crystal structures, we pursued the concept that if the galactose was replaced with talose (the C2 epimer of galactose) as a scaffold, then O2 substituents would be directed closer to the protein surface and provide opportunity to design inhibitors that are more specific towards particular galectins. Our elucidation of X-ray crys- tal structures of two of our synthesized talosides in complex with galectin-1 and galectin-3 pro- vides the first atomic information on the interac- tions of galectins, and indeed any protein, with talosides. These results have enabled a structure- based rationale for the specificity differences shown by galectin-1 and galectin-3 towards these talosides and demonstrate new opportunities for further exploitation as specific inhibitors of galectins.
dc.description.peerreviewedYes
dc.description.publicationstatusYes
dc.languageEnglish
dc.language.isoeng
dc.publisherWiley-Blackwell Publishing
dc.publisher.placeUnited States
dc.relation.ispartofstudentpublicationY
dc.relation.ispartofpagefrom339
dc.relation.ispartofpageto346
dc.relation.ispartofissue3
dc.relation.ispartofjournalChemical Biology & Drug Design
dc.relation.ispartofvolume79
dc.rights.retentionY
dc.subject.fieldofresearchBiomolecular modelling and design
dc.subject.fieldofresearchCharacterisation of biological macromolecules
dc.subject.fieldofresearchBiochemistry and cell biology
dc.subject.fieldofresearchcode340402
dc.subject.fieldofresearchcode340403
dc.subject.fieldofresearchcode3101
dc.titleTaloside Inhibitors of Galectin-1 and Galectin-3
dc.typeJournal article
dc.type.descriptionC1 - Articles
dc.type.codeC - Journal Articles
gro.facultyOffice of the Snr Dep Vice Chancellor, Institute for Glycomics
gro.date.issued2012
gro.hasfulltextNo Full Text
gro.griffith.authorCollins, Patrick
gro.griffith.authorBlanchard, Helen


Files in this item

FilesSizeFormatView

There are no files associated with this item.

This item appears in the following Collection(s)

  • Journal articles
    Contains articles published by Griffith authors in scholarly journals.

Show simple item record