G-protein coupled receptors (GPCRs) modulate critical cardiovascular functional parameters such as heart rate, vascular tone, contractility, and blood volume. Abnormal GPCR signaling is a major contributor to several chronic cardiovascular pathologies. Apelin and its GPCR have emerged as a key signaling pathway, which is now known to be downregulated in pulmonary arterial hypertension and heart failure.
In this webinar, Dr. Davenport will discuss strategies for exploiting orphan GPCRs recently paired with endogenous ligands, as illustrated by Apelin and Elabela/Toddler. He will also describe pharmacologically-relevant cell-based assays used to identify “functionally-selective” agonists as potential drug candidates.
