Article
Agonists and Antagonists of Protease-Activated Receptor 2 Discovered within a DNA-Encoded Chemical Library Using Mutational Stabilization of the Target.
SLAS discovery : advancing life sciences R & D - 1 Jun 2018
Brown Dean G, Brown Giles A, Centrella Paolo, Certel Kaan, Cooke Robert M, Cuozzo John W, Dekker Niek, Dumelin Christoph E, Ferguson Andrew, Fiez-Vandal Cédric, Geschwindner Stefan, Guié Marie-Aude, Habeshian Sevan, Keefe Anthony D, Schlenker Oliver, Sigel Eric A, Snijder Arjan, Soutter Holly T, Sundström Linda, Troast Dawn M, Wiggin Giselle, Zhang Jing, Zhang Ying, Clark Matthew A
Abstract excerpt
The discovery of ligands via affinity-mediated selection of DNA-encoded chemical libraries is driven by the quality and concentration of the protein target. G-protein-coupled receptors (GPCRs) and other membrane-bound targets can be difficult to isolate in their functional state and at high concentrations, and therefore have been challenging for affinity-mediated selection. Here, we report a successful selection...
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