Prof. Terry HĂ©bert at McGill University, to talk on, "Assessing Bias and Allostery in GPCRs using Conformational Biosensors" at GPCR Meeting
Online PR News – 26-August-2016 – California – Terry HĂ©bert, Professor of Pharmacology and Therapeuticsat at McGill University, will give a presentation on, "Assessing Bias and Allostery in GPCRs using Conformational Biosensors" at GTCbio's 4th GPCR in Drug Discovery Conference to be held on September 14-15, 2016 in Boston, MA.
Ligand-biased signaling could have a significant impact on drug discovery programs in the pharmaceutical industry. As such, many investigators and screening campaigns are now being directed at a larger section of the signaling responses downstream of an individual G protein-coupled receptor. Biosensor-based platforms have been developed to capture signaling signatures. Despite the ability to use such signaling signatures, they may still be particular to an individual cell type and thus such platforms may not be portable from cell to cell, necessitating further cell-specific biosensor development. We have developed a complementary strategy based on capturing receptor-proximal conformational profiles using intra-molecular BRET-based sensors composed of a Renilla luciferase donor engineered into the carboxy-terminus and CCPGCC motifs which bind fluorescent hairpin arsenical dyes engineered into different positions in the AT1 angiotensin II receptor and the PGF2α receptor. Terry HĂ©bert will discuss the design and optimization of such sensors to capture ligand bias and receptor dimerization-specific conformational crosstalk.
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