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Using the SNAP-tag system, in which the GLP-1R N-terminus contains a small genetically encoded tag to allow specific labeling of surface receptors, we measured the dose responses for the agonist-induced cell surface loss of human GLP-1R in CHO-K1 cells, identifying the analogs with different net internalization efficacy than the reference compound exendin-4 (Supplementary Fig
The higher dose carries a higher incidence of gastrointestinal side effects, particularly nausea and vomiting, and a newly identified effect: dysaesthesia (tingling or burning sensations affecting the skin) occurred in approximately 23% of patients on 7.2 mg versus 6% at 2.4 mg
