Biased ligands in Drug Discovery - the case of TRV027

Watch biased ligands in drug discovery webinar

What is covered in this webinar:

  • Review of GPCR signaling
  • Introduction to concept of biased ligand quantification 
  • Utility of second messenger assays in GPCR drug discovery
  • Pre-clinical biased ligand proof-of-concept

 

Speakers

William Gowen-MacDonald

William Gowen-MacDonald 
Scientist, Trevena Inc.

Nicolas Pierre

Nicolas Pierre 
Global Product Manager, Cisbio.

Terry Kenakin

Terry Kenakin
PhD, professor, UNC School of Medicine.

Abstract

Ligand bias is a well-established concept in the GPCR research field that is beginning to emerge as a means to optimise GPCR targeted drug design. Most approved medications that target GPCRs act as either agonists or antagonists of heterotrimeric G protein and β-arrestin pathways. In many cases, this classical signalling paradigm leads to both efficacy and on-target adverse events. Biased GPCR ligands have the ability to activate or inhibit with greater selectivity one of the two downstream effector proteins and its subsequent signalling cascades. The goal of this webinar is to illustrate in vitro characterisation of GPCR ligand bias and its translation to in vivo proof-of concept using TRV027, an AT1R modulator, as an exemplar biased ligand.