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Article

Crystal Structure of G Protein-coupled Receptor Kinase 5 in Complex with a Rationally Designed Inhibitor.

The Journal of biological chemistry - 21 Aug 2015

Homan Kristoff T, Waldschmidt Helen V, Glukhova Alisa, Cannavo Alessandro, Song Jianliang, Cheung Joseph Y, Koch Walter J, Larsen Scott D, Tesmer John J G

Abstract excerpt

G protein-coupled receptor kinases (GRKs) regulate cell signaling by initiating the desensitization of active G protein-coupled receptors. The two most widely expressed GRKs (GRK2 and GRK5) play a role in cardiovascular disease and thus represent important targets for the development of novel therapeutic drugs. In the course of a GRK2 structure-based drug design campaign, one inhibitor (CCG215022) exhibited...

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Source

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Identifiers

PMID: 26032411
DOI: 10.1074/jbc.M115.647370
PMCID: PMC4543626

Genes

GRK2
GRK5
GRK1
GRK6

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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