Microwave-assisted solid phase synthesis, PEGylation, and biological activity studies of glucagon-like peptide-1(7–36) amide

The insulinotropic hormone glucagon-like peptide-1 (GLP-1) is rapidly inactivated in the body. In order to improve its stability, we replaced the enzymatic hydrolyzation position Ala8with Gly and replaced Ala30 with Cys firstly. Then the modified peptide was further PEGylated at thiol group of Cys30. Biological activity studies showed that the resulting mPEG-MAL-Gly8-Cys30-GLP-1(7–36)-NH2 exhibited long-lasting effect while maintaining moderate glucose-lowering activity.

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