Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 51, Issue 22, Pages 7303-7307Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm8008579
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Funding
- NIH [GM65500]
- Massachusetts Technology Transfer Center
- NSF [0320783]
- Division Of Chemistry
- Direct For Mathematical & Physical Scien [0320783] Funding Source: National Science Foundation
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The relative simplicity and high specificity of peptide therapeutics has fueled recent interest. However, peptide and protein drugs generally require injection and suffer from low metabolic stability. We report here the design, synthesis, and characterization of fluorinated analogues of the gut hormone peptide, GLP-1. Overall, fluorinated GLP-1 analogues displayed higher proteolytic stability with simultaneous retention of biological activity (efficacy). Fluorinated amino acids are useful for engineering peptide drug candidates and probing ligand-receptor interactions.
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