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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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Bibliografski detalji
Izdano u:J Med Chem
Glavni autori: Rowlands, Rachel A., Chen, Qiuyan, Bouley, Renee A., Avramova, Larisa V., Tesmer, John J. G., White, Andrew D.
Format: Artigo
Jezik:Inglês
Izdano: 2021
Teme:
Online pristup: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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