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 RosenkildePublished 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.