A simple method for quantifying functional selectivity and agonist bias.

  title={A simple method for quantifying functional selectivity and agonist bias.},
  author={Terry Kenakin and Christian A Watson and Vanessa Mu{\~n}iz-Medina and Arthur Christopoulos and Steven Novick},
  journal={ACS chemical neuroscience},
  volume={3 3},
Activation of seven-transmembrane (7TM) receptors by agonists does not always lead to uniform activation of all signaling pathways mediated by a given receptor. Relative to other ligands, many agonists are "biased" toward producing subsets of receptor behaviors. A hallmark of such "functional selectivity" is cell type dependence; this poses a particular problem for the profiling of agonists in whole cell test systems removed from the therapeutic one(s). Such response-specific cell-based… CONTINUE READING
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