Supra-physiological efficacy at GPCRs: superstition or super agonists?

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Abstract

The concept of super agonism has been described since the discovery of peptide hormone analogues that yielded greater functional responses than the endogenous agonists, in the early 1980s. It has remained an area of debate as to whether such compounds can really display greater efficacy than an endogenous agonist. However, recent pharmacological data, combined with crystal structures of different GPCR conformations and improved analytical methods for quantifying drug action, are starting to shed light on this phenomenon and indicate that super agonists may be more than superstition.
Original languageEnglish
Pages (from-to)353 - 356
Number of pages4
JournalBritish Journal of Pharmacology
Volume169
Issue number2
DOIs
Publication statusPublished - 2013

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