Title : Structural and functional analysis of g protein-coupled receptor kinase inhibition by paroxetine and a rationally designed analog.

Pub. Date : 2014 Feb

PMID : 24220010






5 Functional Relationships(s)
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1 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 G protein-coupled receptor kinase 2 Homo sapiens
2 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 G protein-coupled receptor kinase 2 Homo sapiens
3 Paroxetine exhibits up to 50-fold selectivity for GRK2 versus other GRKs. Paroxetine G protein-coupled receptor kinase 2 Homo sapiens
4 Our results suggest that the selectivity of paroxetine for GRK2 largely reflects its lower affinity for adenine nucleotides. Paroxetine G protein-coupled receptor kinase 2 Homo sapiens
5 Next, we designed a benzolactam derivative of paroxetine that has optimized interactions with the hinge of the GRK2 kinase domain. Paroxetine G protein-coupled receptor kinase 2 Homo sapiens