G protein-coupled receptors (GPCRs), the single largest class of druggable targets in therapeutic drug discovery, signal via canonical pathways involving heterotrimeric G proteins, and also via G protein–independent interactions with other signaling proteins, including β-arrestins, a process known as functional selectivity. Discovering ligands with the desired signaling bias at GPCRs will yield molecules with novel activities, and could lead to significantly improved therapeutics by enabling beneficial efficacy while reducing undesirable adverse effects. This symposium examines perspectives from academic and industrial scientists, highlighting basic and translational research. Researchers will discuss molecular and structural mechanisms underlying ligand bias and demonstrate how they quantify, design and develop functionally selective GPCR ligands for potential use in cardiovascular and central nervous system diseases.
*Reception to follow.
|Nonmember (Student / Postdoc / Resident / Fellow)
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