Biased ligands in Drug Discovery - the case of TRV027
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
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Speakers
William Gowen-MacDonald Scientist, Trevena Inc.
Nicolas Pierre Global Product Manager, Cisbio.
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.
