A More Integrated Approach To Looking At GPCR Signaling
This article was originally published in Start Up
Executive Summary
G protein-coupled receptors are the most prolific initiators of cell signaling pathways. The largest class of drug targets, they are also, unfortunately, the most intractable to drug development. Three research papers shows how combining different techniques -- crystallography, hydrogen exchange, and electron microscopy -- can shed new light on the nuances of GPCR signaling and how this kind of integrated approach could help identify new drug targets.
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The hydrogen/deuterium-exchange (H/D-Ex) phenomenon is well established as a method for measuring binding interactions between a drug target and a ligand. ExSAR Corp. has developed an automated, rapid, and sensitive H/D-Ex system to rapidly map drug-target interactions in solution, for use in small-molecule drug discovery and also to assist in the stabilization and design of new protein therapeutics.