A high-affinity peptide substrate for G protein-coupled receptor kinase 2 (GRK2)
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We synthesized a previously identified β-tubulin-derived G protein-coupled receptor kinase 2 (GKR2) peptide (GR-11-1; DEMEFTEAESNMN) and its amino-terminal extension (GR-11-1-N; GEGMDEMEFTEAESNMN) and carboxyl-terminal extension (GR-11-1-C; DEMEFTEAESNMNDLVSEYQ) peptides with the aim of finding a high-affinity peptide substrate for GRK2. GR-11-1-C showed high affinity for GRK2, but very low affinity for GKR5. Its specificity and sensitivity for GKR2 were greater than those of GR-11-1 and GR-11-1-N. These findings should be useful in designing tools for probing GKR2-mediated intracellular signaling pathways, as well as GRK2-specific drugs.
KeywordsG protein-coupled receptor kinase Amino acid residue Phosphorylation Cellular signal transduction pathway Consensus sequence
The authors thank Ms. Sigemi Terakubo and Ms. Niño Nakajima (St. Marianna University School of Medicine) for technical assistance. This work was supported by JSPS KAKENHI Grant numbers, 17K08254 and 17K01386.
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Conflict of interest
The authors declare that they have no conflict of interest.
This article does not contain any studies with human participants or animals performed by any of the authors.
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