Article ID Journal Published Year Pages File Type
8410683 Drug Discovery Today 2013 7 Pages PDF
Abstract
► The operational model is extended by including a ligand-induced receptor conformation. ► It is proposed that the system maximum effect depends on receptor conformation. ► The model links receptor active conformations to agonist affinity and efficacy. ► The model can explain the activity of superagonists and allosteric modulators.
Related Topics
Life Sciences Biochemistry, Genetics and Molecular Biology Biotechnology
Preview
Multiple active receptor conformation, agonist efficacy and maximum effect of the system: the conformation-based operational model of agonism
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