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Bioconjug Chem ; 34(6): 1014-1018, 2023 06 21.
Artigo em Inglês | MEDLINE | ID: mdl-37192432

RESUMO

Exenatide was the first marketed GLP-1 receptor agonist for the treatment of type 2 diabetes. Modification to the chemical structure or the formulation has the potential to increase the stability of exenatide. We introduced human complex-type sialyloligosaccharide to exenatide at the native Asn28 position. The synthesis was achieved using both solid phase peptide synthesis (SPPS) and Omniligase-1-mediated chemoenzymatic ligation. The results demonstrate that glycosylation increases the proteolytic stability of exenatide while retaining its full biological activity.


Assuntos
Diabetes Mellitus Tipo 2 , Humanos , Exenatida , Diabetes Mellitus Tipo 2/tratamento farmacológico , Hipoglicemiantes , Glicosilação , Peptídeo Hidrolases , Receptor do Peptídeo Semelhante ao Glucagon 1/agonistas , Peçonhas
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