Highly biased agonism for GPCR ligands via nanobody tethering
Shivani Sachdev,
Brendan A. Creemer,
Thomas J. Gardella
et al.
Abstract:Ligand-induced activation of G protein-coupled receptors (GPCRs) can initiate signaling through multiple distinct pathways with differing biological and physiological outcomes. There is intense interest in understanding how variation in GPCR ligand structure can be used to promote pathway selective signaling (“biased agonism”) with the goal of promoting desirable responses and avoiding deleterious side effects. Here we present a new approach in which a conventional peptide ligand for the type 1 parathyroid hor… Show more
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