A Scale of Agonism and Allosteric Modulation for Assessment of Selectivity, Bias, and Receptor Mutation
Abstract
An index of agonism is described that can be used to quantify agonist receptor selectivity, bias, cell-based agonism, and the effects of receptor mutation on signaling. The parameter is derived from agonist concentration-response curves and comprises the maximal response to the agonist (max) and the EC50 in the form of Δlog(max/EC50). This parameter is derived from equations describing agonists as positive allosteric facilitators of...
Paper Details
Title
A Scale of Agonism and Allosteric Modulation for Assessment of Selectivity, Bias, and Receptor Mutation
Published Date
Jul 5, 2017
Journal
Volume
92
Issue
4
Pages
414 - 424
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