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ABSTRACT:
SUBMITTER: Neubacher S
PROVIDER: S-EPMC7011175 | biostudies-literature | 2020 Feb
REPOSITORIES: biostudies-literature
Neubacher Saskia S Saya Jordy M JM Amore Alessia A Grossmann Tom N TN
The Journal of organic chemistry 20191216 3
Protein macrocyclization represents a very efficient strategy to increase the stability of protein tertiary structures. Here, we describe a panel of novel C3-symmetric tris-electrophilic agents and their use for the cyclization of proteins. These electrophiles are reacted with a protein domain harboring three solvent-exposed cysteine residues, resulting in the in situ cyclization of the protein (INCYPRO). We observe a clear dependency of cross-linking rates on the electrophilicity. All nine obta ...[more]