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Influence of selective fluorination on the biological activity and proteolytic stability of glucagon-like peptide-1.

Abstract：

: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.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Meng H,Krishnaji ST,Beinborn M,Kumar K

doi

10.1021/jm8008579

subject

Has Abstract

pub_date

2008-11-27 00:00:00

pages

7303-7

issue

22

eissn

0022-2623

issn

1520-4804

journal_volume

51

pub_type

杂志文章

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