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Webinar: From Chemistry to Clinic: Discovery of Biased Apelin Receptor Agonists and Action in the Cardiovascular System

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Wednesday, April 5, 2017


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Presenter:
Dr. Anthony Davenport
Director, Human Receptor Research Group,
Department of Medicine, University of Cambridge, UK
 

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.

What will be covered?

  • Role of GPCRs in human cardiovascular system
  • Strategies for exploiting orphan GPCRs recently paired with endogenous ligands illustrated by Apelin and Elabela/Toddler
  • Identifying biased agonists using pharmacologically-relevant functional cell based assays
  • Validating assays and minimizing inter-assay variation

Who should attend?

  • Scientists working in GPCR research and drug discovery
  • Scientists with focus on defining role of GPCRs in diseases and developing drug candidates
  • Assay development scientists