Peptide agonists of class B G protein–coupled receptors have separate segments for binding and activation. Synthesizing peptidic analogs that can be 'clicked' together allows for rapid optimization of agonist activity—as well as providing some surprises about receptor pharmacology.
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Sakmar, T. Clicking class B GPCR ligands. Nat Chem Biol 7, 500–501 (2011). https://doi.org/10.1038/nchembio.621
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DOI: https://doi.org/10.1038/nchembio.621
