Discovery of β2 adrenergic receptor ligands using biosensor fragment screening of tagged wild-type receptor

…, LM Wingler, X Zhu, P Tripathi-Shukla…

Index: Aristotelous, Tonia; Ahn, Seungkirl; Shukla, Arun K.; Gawron, Sylwia; Sassano, Maria F.; Kahsai, Alem W.; Wingler, Laura M.; Zhu, Xiao; Tripathi-Shukla, Prachi; Huang, Xi-Ping; Riley, Jennifer; Besnard, Jeremy; Read, Kevin D.; Roth, Bryan L.; Gilbert, Ian H.; Hopkins, Andrew L.; Lefkowitz, Robert J.; Navratilova, Iva ACS Medicinal Chemistry Letters, 2013 , vol. 4, # 10 p. 1005 - 1010

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Citation Number: 30

Abstract

G-protein coupled receptors (GPCRs) are the primary target class of currently marketed drugs, accounting for about a quarter of all drug targets of approved medicines. However, almost all the screening efforts for novel ligand discovery rely exclusively on cellular systems overexpressing the receptors. An alternative ligand discovery strategy is a fragment-based drug discovery, where low molecular weight compounds, known as fragments, are ...