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Utilizing a Structure-Based Docking Approach to Develop Potent G Protein-Coupled Receptor Kinase (GRK) 2 and 5 Inhibitors

G protein-coupled receptor (GPCR) kinases (GRKs) regulate the desensitization and internalization of GPCRs. Two of these, GRK2 and GRK5, are upregulated in heart failure and are promising targets for heart failure treatment. Although there have been several reports of potent and selective inhibitors...

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Pubblicato in:Bioorg Med Chem Lett
Autori principali: Waldschmidt, Helen V., Bouley, Renee, Kirchhoff, Paul D., Lee, Pil, Tesmer, John J. G., Larsen, Scott D.
Natura: Artigo
Lingua:Inglês
Pubblicazione: 2018
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Accesso online:https://ncbi.nlm.nih.gov/pmc/articles/PMC5916850/
https://ncbi.nlm.nih.gov/pubmed/29627263
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2018.03.082
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