The DOI matches its Crossref record; 12 of the 12 references it cites were found in a registry or an index.
Development and Characterization of a Glucagon-Like Peptide 1-Albumin Conjugate
Abstract
The rapid degradation of native glucagon-like peptide 1 (GLP-1) by dipeptidyl peptidase-IV (DPP-IV) has fostered new approaches for generation of degradation-resistant GLP-1 analogues. We examined the biological activity of CJC-1131, a DPP-IV-resistant drug affinity complex (DAC) GLP-1 compound that conjugates to albumin in vivo. The CJC-1131 albumin conjugate bound to the GLP-1 receptor (GLP-1R) and activated cAMP formation in heterologous fibroblasts expressing a GLP-1R. CJC-1131 lowered glucose in wild-type mice, but not in GLP-1R−/− mice. Basal glucose and glycemic excursion following glucose challenge remained significantly reduced 10–12 h following a single injection of CJC-1131. Twice daily administration of CJC-1131 to db/db mice significantly reduced glycemic excursion following oral and IP glucose challenge (P < 0.01 to 0.05) but did not significantly lower body weight during the 4-week study period. Levels of random fed glucose were significantly lower in CJC-1131-treated +/+ and db/db mice and remained significantly lower even 1 week following discontinuation of CJC-1131 administration. CJC-1131 increased levels of pancreatic proinsulin mRNA transcripts, percent islet area, and the number of bromodeoxyuridine-positive islet cells. These findings demonstrate that an albumin-conjugated DAC:GLP-1 mimics the action of native GLP-1 and represents a new approach for prolonged activation of GLP-1R signaling.
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Self-citationAlbumin as a drug carrier: Design of prodrugs, drug conjugates and nanoparticles
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Metadata
- Authors
- Kim, J.-G., Baggio, L. L., Bridon, D. P., Castaigne, J.-P., Robitaille, M. F., Jetté, L., Benquet, C., & Drucker, D. J.
- Venue
- Diabetes
- Publisher
- American Diabetes Association
- Published
- 2003-03-01
- Volume
- 52
- Issue
- 3
- Pages
- 751-759
- ISSN
- 0012-1797 (ISSN-L)
- 1939-327X
- OpenAlex
- W2124182221
- Cited by
- 210
- References
- 12
- FWCI
- 14.08
- Type
- journal article
- Language
- en
- Open access
- closed
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- Kim, J.-G., Baggio, L. L., Bridon, D. P., Castaigne, J.-P., Robitaille, M. F., Jetté, L., Benquet, C., & Drucker, D. J. (2003). Development and Characterization of a Glucagon-Like Peptide 1-Albumin Conjugate. Diabetes. https://doi.org/10.2337/diabetes.52.3.751
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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