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Structural and Functional Analysis of G Protein–Coupled Receptor Kinase Inhibition by Paroxetine and a Rationally Designed Analog

Recently we identified the serotonin reuptake inhibitor paroxetine as an inhibitor of G protein–coupled receptor kinase 2 (GRK2) that improves cardiac performance in live animals. Paroxetine exhibits up to 50-fold selectivity for GRK2 versus other GRKs. A better understanding of the molecular basis...

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Detalhes bibliográficos
Main Authors: Homan, Kristoff T., Wu, Emily, Wilson, Michael W., Singh, Puja, Larsen, Scott D., Tesmer, John J. G.
Formato: Artigo
Idioma:Inglês
Publicado em: The American Society for Pharmacology and Experimental Therapeutics 2014
Assuntos:
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC3913355/
https://ncbi.nlm.nih.gov/pubmed/24220010
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1124/mol.113.089631
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