Hormonal
GIP receptor antagonism, specifically via the peptide GIP(3-30)NH2, increases GIP receptor surface expression and prevents internalization, thereby resensitizing the receptor for subsequent activation by endogenous or exogenous agonists.
Blocking the GIP receptor with specific antagonists like GIP(3-30)NH2 doesn't just turn off the signal; it keeps the receptors on the cell surface ready to receive signals. This resensitization may help overcome the impaired GIP response often seen in type 2 diabetes and obesity, potentially enhancing the effects of other treatments like GLP-1 agonists.
exposure to the antagonist GIP(3-30)NH2 results in enhanced GIPR surface expression due to an inhibition of GIPR internalization [51]; hence, the antagonist resensitizes the receptor for subsequent agonist activation (Fig. 1D).
Why this rating
Supported by multiple in vitro and in vivo studies cited in the review, including human studies with GIP(3-30)NH2.
Source
GIP-derived GIP receptor antagonists – a review of their role in GIP receptor pharmacology
Mette M. Rosenkilde et al. · Peptides · 2024
DOI 10.1016/j.peptides.2024.171212
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