Facile synthesis of insulin fusion derivatives through sortase A ligation
Acta Pharmaceutica Sinica B
; (6): 2719-2725, 2021.
Article
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| WPRIM
| ID: wpr-888883
Biblioteca responsable:
WPRO
ABSTRACT
Insulin derivatives such as insulin detemir and insulin degludec are U.S. Food and Drug Administration (FDA)-approved long-acting insulin currently used by millions of people with diabetes. These derivatives are modified in C-terminal B29 lysine to retain insulin bioactivity. New and efficient methods for facile synthesis of insulin derivatives may lead to new discovery of therapeutic insulin. Herein, we report a new method using sortase A (SrtA)-mediated ligation for the synthesis of insulin derivatives with high efficiency and functional group tolerance in the C-terminal B chain. This new insulin molecule (Ins-SA) with an SrtA-recognizing motif can be conjugated to diverse groups with N-terminal oligoglycines to generate new insulin derivatives. We further demonstrated that a new insulin derivative synthesized by this SrtA-mediated ligation shows strong cellular and
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Base de datos:
WPRIM
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En
Revista:
Acta Pharmaceutica Sinica B
Año:
2021
Tipo del documento:
Article