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Altered desensitization and internalization patterns of rodent versus human glucose-dependent insulinotropic polypeptide (GIP) receptors. An important drug discovery challenge.

Laerke Smidt GasbjergRasmus Syberg RasmussenAdrian DraganPeter LindquistJosefine Ulrikke MelchiorsenTomasz Maciej StepniewskiSine SchiellerupEsther Karen TordrupSarina GadgaardHüsün Sheyma KizilkayaSabine WillemsYi ZhongYi WangShane C WrightVolker M LauschkeBolette HartmannJens Juul HolstJana SelentMette Marie Rosenkilde
Published in: British journal of pharmacology (2024)
Desensitization of the human GIPR is dependent on the C-terminal tail. The species-dependent functionality of the C-terminal tail and the different species-dependent internalization patterns, especially between human and mouse GIPRs, are important factors influencing the preclinical evaluation of GIPR-targeting therapeutic compounds.
Keyphrases
  • endothelial cells
  • induced pluripotent stem cells
  • pluripotent stem cells
  • stem cells
  • drug delivery
  • adipose tissue
  • cancer therapy