Can Adding Constitutive Receptor Activity Redefine Biased Signaling Quantification?

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, constitutiv...

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Detalles Bibliográficos
Autores: Zhou, Bin, Hall, David A., Giraldo, Jesús|||0000-0001-7082-4695
Tipo de recurso: artículo
Fecha de publicación:2019
País:España
Institución:Universitat Autònoma de Barcelona
Repositorio:Dipòsit Digital de Documents de la UAB
Idioma:inglés
OAI Identifier:oai:ddd.uab.cat:306807
Acceso en línea:https://ddd.uab.cat/record/306807
https://dx.doi.org/urn:doi:10.1016/j.tips.2019.01.002
Access Level:acceso abierto
Palabra clave:Constitutive receptor activity
Biased signaling
GPCR
Inverse agonists
Descripción
Sumario: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.