Protected maleimide building blocks for the decoration of peptides, peptoids and peptide nucleic acids

Monomers allowing for the introduction of [2,5-dimethylfuran]-protected maleimides into polyamides such as peptides, peptide nucleic acids, and peptoids were prepared, as well as the corresponding oligomers. Suitable maleimide deprotection conditions were established in each case. The stability of t...

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Detalles Bibliográficos
Autores: Elduque Busquets, Xavier, Sánchez-Moya, Albert, Sharma, Kapil, Pedroso Muller, Enrique, Grandas Sagarra, Anna
Tipo de recurso: artículo
Estado:Versión aceptada para publicación
Fecha de publicación:2013
País:España
Institución:Universidad de Barcelona
Repositorio:Dipòsit Digital de la UB
OAI Identifier:oai:diposit.ub.edu:2445/49423
Acceso en línea:https://hdl.handle.net/2445/49423
Access Level:acceso abierto
Palabra clave:Pèptids
Àcids nucleics
Oligòmers
Síntesi orgànica
Biotecnologia
Aminoàcids
Proteïnes
Peptides
Nucleic acids
Oligomers
Organic synthesis
Biotechnology
Amino acids
Proteins
Descripción
Sumario:Monomers allowing for the introduction of [2,5-dimethylfuran]-protected maleimides into polyamides such as peptides, peptide nucleic acids, and peptoids were prepared, as well as the corresponding oligomers. Suitable maleimide deprotection conditions were established in each case. The stability of the adducts generated by Michael-type maleimide-thiol reaction and Diels-Alder cycloaddition to maleimide deprotection conditions was exploited to prepare a variety of conjugates from peptide and PNA scaffolds incorporating one free and one protected maleimide. The target molecules were synthesized by using two subsequent maleimide-involving click reactions separated by a maleimide deprotection step. Carrying out maleimide deprotection and conjugation simultaneously gave better results than performing the two reactions subsequently.