A convenient approach to prepare topologically segregated bilayer beads for one-bead two-compound combinatorial peptide libraries

Auteur(s): Bédard, François; Girard, Anick; Biron, Éric
Résumé: One-bead one-compound (OBOC) combinatorial peptide libraries have been used to identify ligands and modulators for a wide variety of biological targets. While being very efficient with linear peptides, OBOC libraries with N-terminally blocked peptides or with unsequence-able building blocks require encoding. To fully exploit OBOC combinatorial methods with cyclic peptides and peptidomimetics, topologically segregated bilayer beads have been developed. This strategy offers the opportunity to synthesize two compounds per bead, i.e. with one compound exposed on the bead surface for screening, and the other one found within the inner layer as a tag for sequencing and compound identification. Bead segregation often involves the use of unstable derivatives or requires a series of protection–deprotection steps. In order to expedite and optimize bead segregation, the performance of various reagents has been studied. The results obtained herein show that bead segregation can be efficiently performed with commercially available reagents. Finally, in order to control outer/inner layer ratios in segregated beads, the effects of different parameters have been evaluated. We report a straightforward and efficient procedure to prepare topologically segregated bilayer beads in a wide range of controllable, predictable, and reproducible outer versus inner ratios. -- Keywords : Combinatorial chemistry - Solid phase synthesis - Peptide libraries - One-bead two-compound libraries - Cyclic peptides
Type de document: Article de recherche
Date de publication: 18 juillet 2012
Date de la mise en libre accès: Accès restreint
Version du document: VoR
Lien permanent: http://hdl.handle.net/20.500.11794/198
Ce document a été publié dans: International Journal of Peptide Research and Therapeutics, Vol. 19 (1), 13–23 (2013)
https://doi.org/10.1007/s10989-012-9316-x
Springer
Autre version disponible: 10.1007/s10989-012-9316-x
Collection :Articles publiés dans des revues avec comité de lecture

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