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dc.rights.licenseopenen_US
dc.contributor.authorFREMAUX, Juliette
dc.contributor.authorVENIN, Claire
dc.contributor.authorMAURAN, Laura
dc.contributor.authorZIMMER, Robert H.
dc.contributor.authorGUICHARD, Gilles
IDREF: 084339268
dc.contributor.authorGOUDREAU, Sébastien R.
dc.date.accessioned2019
dc.date.available2019
dc.date.issued2019
dc.identifier.issn2041-1723en_US
dc.identifier.otherhttps://static-content.springer.com/esm/art%3A10.1038%2Fs41467-019-08793-y/MediaObjects/41467_2019_8793_MOESM4_ESM.xlsxen_US
dc.identifier.urihttps://oskar-bordeaux.fr/handle/20.500.12278/3814
dc.description.abstractEnPeptides have gained so much attention in the last decade that they are now part of the main strategies, with small molecules and biologics, for developing new medicines. Despite substantial progress, the successful development of peptides as drugs still requires a number of limitations to be addressed, including short in vivo half-lives and poor membrane permeability. Here, we describe the use of oligourea foldamers as tool to improve the pharmaceutical properties of GLP-1, a 31 amino acid peptide hormone involved in metabolism and glycemic control. Our strategy consists in replacing four consecutive amino acids of GLP-1 by three consecutive ureido residues by capitalizing on the structural resemblance of oligourea and α-peptide helices. The efficacy of the approach is demonstrated with three GLP-1-oligourea hybrids showing prolonged activity in vivo. Our findings should enable the use of oligoureas in other peptides to improve their pharmaceutical properties and may provide new therapeutic applications.
dc.language.isoENen_US
dc.title.enPeptide-oligourea hybrids analogue of GLP-1 with improved action in vivo
dc.title.alternativeNat Communen_US
dc.typeArticle de revueen_US
dc.identifier.doi10.1038/s41467-019-08793-y
dc.subject.halChimie/Matériauxen_US
bordeaux.journalNature Communicationsen_US
bordeaux.page924en_US
bordeaux.volume10en_US
bordeaux.hal.laboratoriesInstitut de Chimie & de Biologie des Membranes & des Nano-objets (CBMN) - UMR 5248
bordeaux.issue1en_US
bordeaux.institutionBordeaux INPen_US
bordeaux.institutionUniversité de Bordeauxen_US
bordeaux.peerReviewedouien_US
bordeaux.inpressnonen_US
hal.identifierhal-03181410
hal.version1
hal.date.transferred2021-03-25T14:42:39Z
hal.exporttrue
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