A novel human-based receptor antagonist of sustained action reveals body weight control by endogenous GLP-1.

@article{Patterson2011ANH,
  title={A novel human-based receptor antagonist of sustained action reveals body weight control by endogenous GLP-1.},
  author={James T. Patterson and Nickki L Ottaway and Vasily M Gelfanov and David L. Smiley and Diego P{\'e}rez-Tilve and Paul T Pfluger and Matthias H Tsch{\"o}p and Richard D DiMarchi},
  journal={ACS chemical biology},
  year={2011},
  volume={6 2},
  pages={135-45}
}
Ex-4 (9-39)a is a well characterized GLP-1 receptor antagonist that suffers from two notable limitations, its nonhuman amino acid sequence and its relatively short in vivo duration of action. Comparable N-terminal shortening of human GLP-1 lessens agonism but does not provide a high potency antagonist. Through a series of GLP-1/Ex-4 hybrid peptides, the minimal structural changes required to generate a pure GLP-1-based antagonist were identified as Glu16, Val19, and Arg20, yielding an… CONTINUE READING

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