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Generation of Highly Selective, Potent, and Covalent G Protein-Coupled Receptor Kinase 5 Inhibitors

The ability of G protein-coupled receptor (GPCR) kinases (GRKs) to regulate the desensitization of GPCRs has made GRK2 and GRK5 attractive targets for treating diseases such as heart failure and cancer. Previously, our work showed that Cys474, a GRK5 subfamily-specific residue located on a flexible...

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Detalhes bibliográficos
Publicado no:J Med Chem
Main Authors: Rowlands, Rachel A., Chen, Qiuyan, Bouley, Renee A., Avramova, Larisa V., Tesmer, John J. G., White, Andrew D.
Formato: Artigo
Idioma:Inglês
Publicado em: 2021
Assuntos:
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC7909074/
https://ncbi.nlm.nih.gov/pubmed/33393767
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.0c01522
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