For compound 2, truncation of a large portion (28-48 residues) of the N-terminal -helix resulted in a dramatic efficacy decrease of compound 2, implying the role of the tip of N-terminal -helix in the ago-allosterism
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N Engl J Med 392(6):612615 Rosenstock J, Frias J, Jastreboff AM, Du Y, Lou J, Gurbuz S, Thomas MK, Hartman ML, Haupt A, Milicevic Z, Coskun T (2023) Retatrutide, a GIP, GLP-1 and glucagon receptor agonist, for people with type 2 diabetes: a randomised, double-blind, placebo and active-controlled, parallel-group, phase 2 trial conducted in the USA
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