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The potential for selective pharmacological therapies through biased receptor signaling

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 indep...

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Detalles Bibliográficos
Autor principal: Kenakin, Terry
Formato: Online Artículo Texto
Lenguaje:English
Publicado: BioMed Central 2012
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3506267/
https://www.ncbi.nlm.nih.gov/pubmed/22947056
http://dx.doi.org/10.1186/2050-6511-13-3
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author Kenakin, Terry
author_facet Kenakin, Terry
author_sort Kenakin, Terry
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description 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.
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spelling pubmed-35062672012-11-29 The potential for selective pharmacological therapies through biased receptor signaling Kenakin, Terry BMC Pharmacol Toxicol Review 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. BioMed Central 2012-08-13 /pmc/articles/PMC3506267/ /pubmed/22947056 http://dx.doi.org/10.1186/2050-6511-13-3 Text en Copyright ©2012 Kenakin; licensee BioMed Central Ltd. http://creativecommons.org/licenses/by/2.0 This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/2.0), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Review
Kenakin, Terry
The potential for selective pharmacological therapies through biased receptor signaling
title The potential for selective pharmacological therapies through biased receptor signaling
title_full The potential for selective pharmacological therapies through biased receptor signaling
title_fullStr The potential for selective pharmacological therapies through biased receptor signaling
title_full_unstemmed The potential for selective pharmacological therapies through biased receptor signaling
title_short The potential for selective pharmacological therapies through biased receptor signaling
title_sort potential for selective pharmacological therapies through biased receptor signaling
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3506267/
https://www.ncbi.nlm.nih.gov/pubmed/22947056
http://dx.doi.org/10.1186/2050-6511-13-3
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