Heterochiral peptides reshaping class B1 GPCR agonism

A α-helical conformation within Class B1 G protein-coupled receptors agonists has been thought necessary for receptor activation. Gellman et al. suggested that selective replacement of L-amino acids with D-enantiomers could yield biased agonists. The new strategy helical would broaden the tools available for investigating agonist conformations and therapeutic potentials.