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Parallel Interrogation of β-Arrestin2 Recruitment for Ligand Screening on a GPCR-Wide Scale using PRESTO-Tango Assay
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G-protein-coupled receptor affinity prediction based on the use of a profiling dataset: QSAR design, synthesis, and

Catherine Rolland1, Rafael Gozalbes, Eric Nicolaï

  • 1Cerep, 128 rue Danton, 92500 Rueil-Malmaison, France, and Cerep, Le Bois l'Evêque, 86600 Celle l'Evescault, France. C.Rolland@cerep.fr

Journal of Medicinal Chemistry
|October 14, 2005
PubMed

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G Protein-coupled Receptors

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G Protein–Coupled Receptors (GPCRs) are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to various stimuli. GPCRs regulate critical physiological pathways and are excellent drug targets for treating diseases such as diabetes, cancer, obesity, depression, or Alzheimer's. Nearly 35% of approved drugs implement their therapeutic effects by selectively interacting with specific GPCRs.
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