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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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| Опубликовано в: : | Mol Pharmacol |
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| Главные авторы: | , , , , , , , , , |
| Формат: | Artigo |
| Язык: | Inglês |
| Опубликовано: |
The American Society for Pharmacology and Experimental Therapeutics
2017
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| Предметы: | |
| Online-ссылка: | 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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