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Can Adding Constitutive Receptor Activity Redefine Biased Signaling Quantification?

Zhou, Bin; Hall, David A.; Giraldo, Jesus

TRENDS IN PHARMACOLOGICAL SCIENCES
2019
VL / 40 - BP / 156 - EP / 160
abstract
Biased signaling, the differential activation of distinct signaling pathways, is currently at the center of pharmacology. Reliable characterization of biased ligands requires robust scales applicable to all ligand classes: agonists, neutral antagonists, and inverse agonists. To this end, constitutive receptor activity should be included in the models.

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