Structural Determinants Influencing the Potency and Selectivity of Indazole-Paroxetine Hybrid G Protein–Coupled Receptor Kinase 2 Inhibitors

G protein–coupled receptor kinases (GRKs) phosphorylate activated receptors to promote arrestin binding, decoupling from heterotrimeric G proteins, and internalization. GRK2 and GRK5 are overexpressed in the failing heart and thus have become therapeutic targets. Previously, we discovered two classe...

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Foilsithe in:Mol Pharmacol
Main Authors: Bouley, Renee, Waldschmidt, Helen V., Cato, M. Claire, Cannavo, Alessandro, Song, Jianliang, Cheung, Joseph Y., Yao, Xin-Qiu, Koch, Walter J., Larsen, Scott D., Tesmer, John J. G.
Formáid: Artigo
Teanga:Inglês
Foilsithe: The American Society for Pharmacology and Experimental Therapeutics 2017
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Articles
Rochtain Ar Líne:https://ncbi.nlm.nih.gov/pmc/articles/PMC5691592/
https://ncbi.nlm.nih.gov/pubmed/29070696
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1124/mol.117.110130
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