Biological and functional characteristics of a novel low-molecular weight antagonist of glucose-dependent insulinotropic polypeptide receptor, SKL-14959, in vitro and in vivo.

@article{Nakamura2012BiologicalAF,
  title={Biological and functional characteristics of a novel low-molecular weight antagonist of glucose-dependent insulinotropic polypeptide receptor, SKL-14959, in vitro and in vivo.},
  author={T Nakamura and Hidenori Tanimoto and Yuki Mizuno and Y Tsubamoto and H Noda},
  journal={Diabetes, obesity & metabolism},
  year={2012},
  volume={14 6},
  pages={511-7}
}
AIM We recently discovered a glucose-dependent insulinotropic polypeptide (GIP) receptor antagonist, SKL-14959. GIP plays a role in the glucose and lipid metabolism, and is associated with obesity and insulin resistance. Therefore, we aimed to ascertain the inhibitory potency and glucose and lipid metabolism of SKL-14959. METHODS SKL-14959 was evaluated for its binding affinity to each GIP, glucagon-like peptide-1 (GLP-1) and glucagon receptors by each labelled and non-labelled ligand; GIP… CONTINUE READING
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