期刊
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
卷 136, 期 37, 页码 12848-12851出版社
AMER CHEMICAL SOC
DOI: 10.1021/ja507168t
关键词
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资金
- U.S. National Institutes of Health [GM056414, DK58037, DK56593]
- American Diabetes Association (ADA) [7-12-IN-38]
- Chemistry-Biology Interface Training Grant from NIGMS [T32 GM008505]
Glucagon-like peptide-1 (GLP-1) is a natural agonist for GLP-1R, a G protein-coupled receptor (GPCR) on the surface of pancreatic beta 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 alpha residues with conformationally constrained beta-amino acid residues. This backbone-modification approach may be useful for developing stabilized analogues of other peptide hormones.
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