Selective Lysine Modification Enabled by Intramolecular Acyl Transfer.
Org Lett
; 22(8): 3067-3071, 2020 04 17.
Article
em En
| MEDLINE
| ID: mdl-32227899
ABSTRACT
The chemistries selectively modifying recombinant proteins are valuable for the discovery and development of biologic therapeutics. We report here a Lys modification strategy that engages a Cys residue to covalently tether the reagents to the target that facilitates a proximity-driven intramolecular O-to-N acyl-transfer process yielding desired Lys-acylated products. We utilized GLP-1 as a case study, followed by desulfurization of the Cys mutation to native Ala regenerating the native sequence in a traceless fashion.
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Base de dados:
MEDLINE
Assunto principal:
Cisteína
/
Lisina
Idioma:
En
Ano de publicação:
2020
Tipo de documento:
Article