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Effect of glycosylation on biodistribution of radiolabeled glucagon-like peptide 1

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Title: Effect of glycosylation on biodistribution of radiolabeled glucagon-like peptide 1
Authors: Watanabe, Ayahisa Browse this author
Nishijima, Ken-ichi Browse this author
Zhao, Songji Browse this author
Tanaka, Yoshikazu Browse this author
Itoh, Takeshi Browse this author
Takemoto, Hiroshi Browse this author
Tamaki, Nagara Browse this author
Kuge, Yuji Browse this author
Keywords: Noninvasive imaging
Glucagon-like peptide 1
Issue Date: Feb-2012
Publisher: Springer Japan
Journal Title: Annals of Nuclear Medicine
Volume: 26
Issue: 2
Start Page: 184
End Page: 191
Publisher DOI: 10.1007/s12149-011-0558-z
PMID: 22187312
Abstract: Objective: Glycosylation is generally applicable as a strategy for increasing the activity of bioactive proteins. In this study, we examined the effect of glycosylation on biodistribution of radiolabeled glucagon-like peptide 1 (GLP-1) as a bioactive peptide for type 2 diabetes. Methods: Noninvasive imaging studies were performed using a gamma camera after the intravenous administration of 123I-GLP-1 or 123I-α2, 6-sialyl N-acetyllactosamine (glycosylated) GLP-1 in rats. In ex vivo biodistribution studies using 125I-GLP-1 or 125I-glycosylated GLP-1, organ samples were measured for radioactivity. Plasma samples were added to 15% trichloroacetic acid (TCA) to obtain TCA-insoluble and TCA-soluble fractions. The radioactivity in the TCA-insoluble and TCA-soluble fractions was measured. Results: In the noninvasive imaging studies, a relatively high accumulation level of 123I-GLP-1 was found in the liver, which is the major organ to eliminate exogenous GLP-1. The area under the time-activity curve (AUC) of 123I-glycosylated GLP-1 in the liver was significantly lower (89%) than that of 123I-GLP-1. These results were consistent with those of ex vivo biodistribution studies using 125I-labeled peptides. The AUC of 125I-glycosylated GLP-1 in the TCA-insoluble fraction was significantly higher (1.7-fold) than that of GLP-1. Conclusions: This study demonstrated that glycosylation significantly decreased the distribution of radiolabeled GLP-1 into the liver and increased the concentration of radiolabeled GLP-1 in plasma. These results suggested that glycosylation is a useful strategy for decreasing the distribution into the liver of bioactive peptides as desirable pharmaceuticals.
Rights: The original publication is available at
Type: article (author version)
Appears in Collections:医学院・医学研究院 (Graduate School of Medicine / Faculty of Medicine) > 雑誌発表論文等 (Peer-reviewed Journal Articles, etc)

Submitter: 渡邊 郁剛

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