Abstract
Abstract Preclinical Research Glucagon‐like peptide‐1 (GLP‐1) is an attractive lead for antidiabetic drug development but its utility is limited due to poor in vivo stability. In this study, we developed a C‐terminal site‐specific PEGylated analog of GLP‐1 based on the structure‐activity relationship of GLP‐1. Using three steps of chromatography, we obtained the conjugate with a high purity. Polyethylene glycol (PEG) conjugation greatly enhanced GLP‐1 potency in vivo without changing its original conformation. In streptozotosin diabetic mice, this conjugate had an improved antidiabetic effect, as measured by fasting glucose/insulin/glycosylated serum protein, oral glucose tolerance test, and histochemical studies. Additionally, this PEG‐conjugated peptide delayed gastric emptying without significant effects on body weight gain. Our data indicate that this conjugate may be a promising lead for the development of antidiabetic drugs.
Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
