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The Premise of the Paradox: Examining the Evidence That Motivated GIPR Agonist and Antagonist Drug Development Programs
▪ Gradual titration is essential: Opening at 2 mg weekly instead of a higher dose markedly lowers the odds of early gastrointestinal effects [4]
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Importantly, both the stalk and ECL1 of GCGR contain several β-branched residues that favor the β over α conformation, in contrast to only one β-branched residue (T207) in ECL1 and none in the stalk region in GLP-1R
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