Orthogonal protection of peptides and peptoids for cyclization by the thiol-ene reaction and conjugation

Cyclic peptides and peptoids were prepared using the thiol-ene Michael-type reaction. The linear precursors were provided with additional functional groups allowing for subsequent conjugation: an orthogonally protected thiol, a protected maleimide, or an alkyne. The functional group for conjugation...

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Bibliographic Details
Authors: Elduque Busquets, Xavier, Pedroso Muller, Enrique, Grandas Sagarra, Anna
Format: article
Status:Versión aceptada para publicación
Publication Date:2014
Country:España
Institution:Varias* (Consorci de Biblioteques Universitáries de Catalunya, Centre de Serveis Científics i Acadèmics de Catalunya)
Repository:Recercat. Dipósit de la Recerca de Catalunya
OAI Identifier:oai:recercat.cat:2445/53528
Online Access:https://hdl.handle.net/2445/53528
Access Level:Open access
Keyword:Pèptids
Àcids nucleics
Ciclització (Química)
Aminoàcids
Proteïnes
Peptides
Nucleic acids
Ring formation (Chemistry)
Amino acids
Proteins
Description
Summary:Cyclic peptides and peptoids were prepared using the thiol-ene Michael-type reaction. The linear precursors were provided with additional functional groups allowing for subsequent conjugation: an orthogonally protected thiol, a protected maleimide, or an alkyne. The functional group for conjugation was placed either within the cycle or in an external position. The click reactions employed for conjugation with suitably derivatized nucleoside or oligonucleotides were either cycloadditions (Diels-Alder, Cu(I)-catalyzed azide-alkyne) or the same Michael-type reaction as for cyclization.