the potential for selective pharmacological therapies through biased receptor signaling潜在的选择性药物疗法通过偏见受体信号.pdfVIP
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the potential for selective pharmacological therapies through biased receptor signaling潜在的选择性药物疗法通过偏见受体信号
Kenakin BMC Pharmacology and Toxicology 2012, 13:3
/2050-6511/13/1/3
REVIEW Open Access
The potential for selective pharmacological
therapies through biased receptor signaling
Terry Kenakin
Abstract
The discovery that not all agonists uniformly activate cellular signaling pathways (biased signaling) has greatly
changed the drug discovery process for agonists and the strategy for treatment of disease with agonists.
Technological advances have enabled complex receptor behaviors to be viewed independently and through these
assays, the bias for an agonist can be quantified. It is predicted that therapeutic phenotypes will be linked, through
translational studies, to quantified scales of bias to guide medicinal chemists in the drug discovery process.
Introduction agonist-receptor complex) and τ (where τ is the agonist
Agonists constitute a major class of therapeutic drug intrinsic efficacy and sensitivity to agonist of the tissue-
and pose special problems with respect to the drug dis- vide infra) [1]. Thus estimates of τ and KA become the
covery process. Specifically, agonist activity is intimately system independent measures of agonism.
tied to the sensitivity of the tissue in which the activity The use of these techniques to compare whole cell
is measured therefore the obvious measures of agonist activity for drug discovery depends on an important
activity (i.e. potency and maximal response) can be assumption, namely that the function linking receptor
complex and certainly are system dependent. As in most occupancy and tissue response be monotonic (i.e. that
cases, new therapeutic entities are discovered, optimized
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