Scalable synthesis and coupling of quaternary α-arylated amino acids: α-aryl substituents are tolerated in α-helical peptides.


Journal

Chemical science
ISSN: 2041-6520
Titre abrégé: Chem Sci
Pays: England
ID NLM: 101545951

Informations de publication

Date de publication:
14 Jul 2021
Historique:
received: 08 03 2021
accepted: 08 06 2021
entrez: 5 8 2021
pubmed: 6 8 2021
medline: 6 8 2021
Statut: epublish

Résumé

Quaternary amino acids are important tools for the modification and stabilisation of peptide secondary structures. Here we describe a practical and scalable synthesis applicable to quaternary alpha-arylated amino acids (Q4As), and the development of solid-phase synthesis conditions for their incorporation into peptides. Monomeric and dimeric α-helical peptides are synthesised with varying degrees of Q4A substitution and their structures examined using biophysical methods. Both enantiomers of the Q4As are tolerated in folded monomeric and oligomeric α-helical peptides, with the (

Identifiants

pubmed: 34349911
doi: 10.1039/d1sc01378e
pii: d1sc01378e
pmc: PMC8278958
doi:

Types de publication

Journal Article

Langues

eng

Pagination

9386-9390

Subventions

Organisme : Biotechnology and Biological Sciences Research Council
ID : BB/L01386X/1
Pays : United Kingdom

Informations de copyright

This journal is © The Royal Society of Chemistry.

Déclaration de conflit d'intérêts

There are no conflicts to declare.

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Auteurs

Daniel J Leonard (DJ)

School of Chemistry, University of Bristol Cantock's Close Bristol BS8 1TS UK D.N.Woolfson@bristol.ac.uk j.clayden@bristol.ac.uk.

Francis Zieleniewski (F)

School of Chemistry, University of Bristol Cantock's Close Bristol BS8 1TS UK D.N.Woolfson@bristol.ac.uk j.clayden@bristol.ac.uk.

Isabelle Wellhöfer (I)

School of Chemistry, University of Bristol Cantock's Close Bristol BS8 1TS UK D.N.Woolfson@bristol.ac.uk j.clayden@bristol.ac.uk.

Emily G Baker (EG)

School of Chemistry, University of Bristol Cantock's Close Bristol BS8 1TS UK D.N.Woolfson@bristol.ac.uk j.clayden@bristol.ac.uk.
School of Biochemistry, University of Bristol, Medical Sciences Building, University Walk Bristol BS8 1TS UK.
Bristol BioDesign Institute, University of Bristol, Life Sciences Building Tyndall Avenue Bristol BS8 1TQ UK.

John W Ward (JW)

School of Chemistry, University of Bristol Cantock's Close Bristol BS8 1TS UK D.N.Woolfson@bristol.ac.uk j.clayden@bristol.ac.uk.

Derek N Woolfson (DN)

School of Chemistry, University of Bristol Cantock's Close Bristol BS8 1TS UK D.N.Woolfson@bristol.ac.uk j.clayden@bristol.ac.uk.
School of Biochemistry, University of Bristol, Medical Sciences Building, University Walk Bristol BS8 1TS UK.
Bristol BioDesign Institute, University of Bristol, Life Sciences Building Tyndall Avenue Bristol BS8 1TQ UK.

Jonathan Clayden (J)

School of Chemistry, University of Bristol Cantock's Close Bristol BS8 1TS UK D.N.Woolfson@bristol.ac.uk j.clayden@bristol.ac.uk.

Classifications MeSH