Discovery of the Once-Weekly Glucagon-Like Peptide-1 (GLP-1) Analogue Semaglutide.

@article{Lau2015DiscoveryOT,
  title={Discovery of the Once-Weekly Glucagon-Like Peptide-1 (GLP-1) Analogue Semaglutide.},
  author={Jesper F Lau and Paw Bloch and Lauge Sch{\"a}ffer and Ingrid Pettersson and Jane C. Spetzler and Jacob Kofoed and Kjeld Kilsgaard Madsen and Lotte Bjerre Knudsen and James Norton McGuire and Dorte Bjerre Steensgaard and Holger Martin Strauss and Dorte Xenia Gram and Sanne M\oller Knudsen and Flemming Seier Nielsen and Peter Thygesen and Steffen Reedtz-Runge and Thomas Kruse},
  journal={Journal of medicinal chemistry},
  year={2015},
  volume={58 18},
  pages={7370-80}
}
Liraglutide is an acylated glucagon-like peptide-1 (GLP-1) analogue that binds to serum albumin in vivo and is approved for once-daily treatment of diabetes as well as obesity. The aim of the present studies was to design a once weekly GLP-1 analogue by increasing albumin affinity and secure full stability against metabolic degradation. The fatty acid moiety and the linking chemistry to GLP-1 were the key features to secure high albumin affinity and GLP-1 receptor (GLP-1R) potency and in… CONTINUE READING
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