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Supra‐physiological efficacy at GPCRs : superstition or super agonists?
Author(s) -
Langmead Christopher J,
Christopoulos Arthur
Publication year - 2013
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/bph.12142
Subject(s) - agonist , g protein coupled receptor , superstition , endogeny , pharmacology , drug discovery , medicine , receptor , neuroscience , chemistry , bioinformatics , biology , philosophy , theology
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.