Structural Basis for alpha-Helix Mimicry and Inhibition of Protein-Protein Interactions with Oligourea Foldamers
| dc.rights.license | open | en_US |
| hal.structure.identifier | Chimie et Biologie des Membranes et des Nanoobjets [CBMN] | |
| dc.contributor.author | CUSSOL, Leonie | |
| hal.structure.identifier | Chimie et Biologie des Membranes et des Nanoobjets [CBMN] | |
| dc.contributor.author | MAURAN-AMBROSINO, Laura | |
| hal.structure.identifier | Chimie et Biologie des Membranes et des Nanoobjets [CBMN] | |
| dc.contributor.author | BURATTO, Jeremie | |
| dc.contributor.author | BELORUSOVA, Anna Y. | |
| hal.structure.identifier | Chimie et Biologie des Membranes et des Nanoobjets [CBMN] | |
| dc.contributor.author | NEUVILLE, Maxime | |
| dc.contributor.author | OSZ, Judit | |
| hal.structure.identifier | Acides Nucléiques : Régulations Naturelle et Artificielle [ARNA] | |
| dc.contributor.author | FRIBOURG, Sebastien | |
| dc.contributor.author | FREMAUX, Juliette | |
| hal.structure.identifier | Chimie et Biologie des Membranes et des Nanoobjets [CBMN] | |
| dc.contributor.author | DOLAIN, Christel | |
| dc.contributor.author | GOUDREAU, Sebastien R. | |
| dc.contributor.author | ROCHEL, Natacha | |
| hal.structure.identifier | Chimie et Biologie des Membranes et des Nanoobjets [CBMN] | |
| dc.contributor.author | GUICHARD, Gilles
IDREF: 084339268 | |
| dc.date.accessioned | 2021-07-08T14:07:27Z | |
| dc.date.available | 2021-07-08T14:07:27Z | |
| dc.date.issued | 2021 | |
| dc.identifier.issn | 1433-7851 | en_US |
| dc.identifier.uri | https://oskar-bordeaux.fr/handle/20.500.12278/106475 | |
| dc.description.abstractEn | Efficient optimization of a peptide lead into a drug candidate frequently needs further transformation to augment properties such as bioavailability. Among the different options, foldamers, which are sequence-based oligomers with precise folded conformation, have emerged as a promising technology. We introduce oligourea foldamers to reduce the peptide character of inhibitors of protein-protein interactions (PPI). However, the precise design of such mimics is currently limited by the lack of structural information on how these foldamers adapt to protein surfaces. We report a collection of X-ray structures of peptide-oligourea hybrids in complex with ubiquitin ligase MDM2 and vitamin D receptor and show how such hybrid oligomers can be designed to bind with high affinity to protein targets. This work should enable the generation of more effective foldamer-based disruptors of PPIs in the context of peptide lead optimization. | |
| dc.language.iso | EN | en_US |
| dc.subject.en | Peptidomimetics | |
| dc.subject.en | Foldamers | |
| dc.subject.en | Protein-protein interactions | |
| dc.subject.en | Helical structures | |
| dc.subject.en | Structure-activity relationships | |
| dc.title.en | Structural Basis for alpha-Helix Mimicry and Inhibition of Protein-Protein Interactions with Oligourea Foldamers | |
| dc.type | Article de revue | en_US |
| dc.identifier.doi | 10.1002/anie.202008992 | en_US |
| dc.subject.hal | Chimie/Matériaux | en_US |
| bordeaux.journal | Angewandte Chemie-International Edition | en_US |
| bordeaux.page | 2296-2303 | en_US |
| bordeaux.volume | 60 | en_US |
| bordeaux.hal.laboratories | Institut de Chimie & de Biologie des Membranes & des Nano-objets (CBMN) - UMR 5248 | en_US |
| bordeaux.issue | 5 | en_US |
| bordeaux.institution | Université de Bordeaux | en_US |
| bordeaux.institution | Bordeaux INP | en_US |
| bordeaux.institution | CNRS | en_US |
| bordeaux.peerReviewed | oui | en_US |
| bordeaux.inpress | non | en_US |
| hal.identifier | hal-03039251 | |
| hal.export | false | |
| bordeaux.COinS | ctx_ver=Z39.88-2004&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.jtitle=Angewandte%20Chemie-International%20Edition&rft.date=2021&rft.volume=60&rft.issue=5&rft.spage=2296-2303&rft.epage=2296-2303&rft.eissn=1433-7851&rft.issn=1433-7851&rft.au=CUSSOL,%20Leonie&MAURAN-AMBROSINO,%20Laura&BURATTO,%20Jeremie&BELORUSOVA,%20Anna%20Y.&NEUVILLE,%20Maxime&rft.genre=article |
