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However, given that large peptides like GLP-1 interact with both the extracellular and transmembrane domains of the GLP-1R ( 32 ), and that our small molecules were unlikely to recapitulate this complex binding mode, it was unclear whether the competition binding experiments with radiolabeled GLP-1 were providing an accurate measure of affinity ( 25 )

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Marcinkiewicz et al., 2002