Perturbation of the interactions of calmodulin with GRK5 using a natural product chemical probe

G protein-coupled receptor (GPCR) kinases (GRKs) are responsible for initiating desensitization of activated GPCRs. GRK5 is potently inhibited by the calcium-sensing protein calmodulin (CaM), which leads to nuclear translocation of GRK5 and promotion of cardiac hypertrophy. Herein, we report the arc...

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Veröffentlicht in:	Proceedings of the National Academy of Sciences - PNAS 2019-08, Vol.116 (32), p.15895-15900
Hauptverfasser:	Beyett, Tyler S., Fraley, Amy E., Labudde, Emily, Patra, Dhabaleswar, Coleman, Ryan C., Eguchi, Akito, Glukhova, Alisa, Chen, Qiuyan, Williams, Robert M., Koch, Walter J., Sherman, David H., Tesmer, John J. G.
Format:	Artikel
Sprache:	eng
Schlagworte:	Biological Products - chemistry Biological Sciences Calcium - metabolism Calcium ions Calcium-binding protein Calmodulin Calmodulin - metabolism Cell activation Cell Nucleus - drug effects Cell Nucleus - metabolism Desensitization Electron microscopy Enzyme Activation - drug effects Eutrophication G protein-coupled receptor kinase 5 G protein-coupled receptors G-Protein-Coupled Receptor Kinase 5 - chemistry G-Protein-Coupled Receptor Kinase 5 - metabolism Hypertrophy Indole Alkaloids - chemistry Indole Alkaloids - pharmacology INORGANIC, ORGANIC, PHYSICAL, AND ANALYTICAL CHEMISTRY Kinases malbrancheamide Models, Biological Myocytes, Cardiac - drug effects Myocytes, Cardiac - metabolism Myocytes, Cardiac - pathology Natural products Nuclear transport Organic chemistry Perturbation Phosphorylation Phosphorylation - drug effects Physical Sciences Protein Domains Protein Transport - drug effects Proteins Small angle X ray scattering Substrate Specificity - drug effects Substrates Translocation X-ray scattering
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