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This dual mechanism of action is why tirzepatide is classified as a GIP/GLP-1 receptor agonist rather than simply a GLP-1 receptor agonist
Phase II Clinical Trials: Efinopegdutide (Merck/Johnson & Johnson/Hanmi Hanma), VK2735 (Viking Therapeutics), BGM0504 (BrightGene), Pemvidutide (Altimmune/Spitfire Pharma), AMG133 (Amgen), Dapiglutide (Zealand Pharma), etc
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Importantly, the ECD of GLP-1R undergoes a remarkable orientation change from the closed TMD-interacting conformation to the extended active conformation during peptide binding and activation
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Ozeki Y, Masaki T, Kamata A, Miyamoto S, Yoshida Y, Okamoto M, et al
