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Antagonism of the calcitonin gene‐related peptide (CGRP) receptor may be a useful approach for migraine treatment. Selective PEGylated peptide antagonists to the CGRP receptor are described, derived from CGRP(8–37) with polymer derivatization at an engineered lysine‐25 residue. Potent PEGylated peptides with improved pharmacokinetics were identified through peptide side‐chain modification to mitigate...
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