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Article

Activation of G protein-coupled receptor kinase 1 involves interactions between its N-terminal region and its kinase domain.

Biochemistry - 22 Mar 2011

Huang Chih-Chin, Orban Tivadar, Jastrzebska Beata, Palczewski Krzysztof, Tesmer John J G

Abstract excerpt

G protein-coupled receptor kinases (GRKs) phosphorylate activated G protein-coupled receptors (GPCRs) to initiate receptor desensitization. In addition to the canonical phosphoacceptor site of the kinase domain, activated receptors bind to a distinct docking site that confers higher affinity and activates GRKs allosterically. Recent mutagenesis and structural studies support a model in which receptor docking...

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Identifiers

PMID: 21265573
DOI: 10.1021/bi101606e
PMCID: PMC3069497

Genes

GRK1

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-08.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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