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Functional Selectivity of GPCR Ligand Stereoisomers: New Pharmacological Opportunities

Seifert, Roland ; Dove, Stefan



Abstract

It is now well established that any given ligand for a G-protein coupled receptor (GPCR) does not simply possess a single defined efficacy. Rather, a ligand possesses multiple efficacies, depending on the specific down-stream signal transduction pathway analyzed. This diversity may be based on ligand-specific GPCR conformations and is often referred to as “Functional Selectivity”. It has been ...

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