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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Detalhes bibliográficos
Autores: Elduque Busquets, Xavier, Pedroso Muller, Enrique, Grandas Sagarra, Anna
Formato: artículo
Estado:Versión aceptada para publicación
Fecha de publicación:2014
País:España
Recursos:Varias* (Consorci de Biblioteques Universitáries de Catalunya, Centre de Serveis Científics i Acadèmics de Catalunya)
Repositorio:Recercat. Dipósit de la Recerca de Catalunya
OAI Identifier:oai:recercat.cat:2445/53528
Acesso em linha:https://hdl.handle.net/2445/53528
Access Level:acceso abierto
Palavra-chave:Pèptids
Àcids nucleics
Ciclització (Química)
Aminoàcids
Proteïnes
Peptides
Nucleic acids
Ring formation (Chemistry)
Amino acids
Proteins
Descrição
Resumo: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.