A Potent α/β-Peptide Analogue of GLP-1 with Prolonged Action in Vivo
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Author
Johnson, Lisa M.
Barrick, Stacey
Hager, Marlies
V.
McFedries, Amanda
Homan, Edwin A.
Rabaglia, Mary E.
Keller, Mark P.
Attie, Alan D.
Saghatelian, Alan
Bisello, Alessandro
Gellman, Samuel H.
Note: Order does not necessarily reflect citation order of authors.
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https://doi.org/10.1021/ja507168tMetadata
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Johnson, L. M., S. Barrick, M. Hager, A. McFedries, E. A. Homan, M. E. Rabaglia, M. P. Keller, et al. 2014. “A Potent α/β-Peptide Analogue of GLP-1 with Prolonged Action in Vivo.” Journal of the American Chemical Society 136 (37): 12848-12851. doi:10.1021/ja507168t. http://dx.doi.org/10.1021/ja507168t.Abstract
Glucagon-like peptide-1 (GLP-1) is a natural agonist for GLP-1R, a G protein-coupled receptor (GPCR) on the surface of pancreatic β cells. GLP-1R agoinsts are attractive for treatment of type 2 diabetes, but GLP-1 itself is rapidly degraded by peptidases in vivo. We describe a design strategy for retaining GLP-1-like activity while engendering prolonged activity in vivo, based on strategic replacement of native α residues with conformationally constrained β-amino acid residues. This backbone-modification approach may be useful for developing stabilized analogues of other peptide hormones.Other Sources
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4183665/pdf/Terms of Use
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