On-Resin Peptide Cyclization Using the 3-Amino-4-(Methylamino)Benzoic Acid MeDbz Linker

Publikation: Bidrag til bog/antologi/rapportBidrag til bog/antologiForskningfagfællebedømt

Cyclic peptides are becoming increasingly important in drug discovery due to their specific binding properties, larger surface area compared to small molecules, and their ready and modular synthetic accessibility. In this protocol, we describe an on-resin, cleavage-inducing cyclization methodology for the synthesis of cyclic thiodepsipeptides and cyclic homodetic peptides using the 3-amino-4-(methylamino)benzoic acid (MeDbz) linker. We further describe three post-cyclization one-pot procedures, which include desulfurization, disulfide bond formation, and S-alkylation of cysteine residues.

OriginalsprogEngelsk
TitelMethods in Molecular Biology
ForlagHumana Press
Publikationsdato2022
Sider101-115
ISBN (Trykt)978-1-0716-1688-8
ISBN (Elektronisk)978-1-0716-1689-5
DOI
StatusUdgivet - 2022
NavnMethods in Molecular Biology
Vol/bind2371
ISSN1064-3745

Bibliografisk note

Publisher Copyright:
© 2022, Springer Science+Business Media, LLC, part of Springer Nature.

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