Amino Acids

, Volume 51, Issue 6, pp 973–976 | Cite as

A high-affinity peptide substrate for G protein-coupled receptor kinase 2 (GRK2)

  • Daisuke AsaiEmail author
  • Masaharu Murata
  • Riki Toita
  • Takahito Kawano
  • Hideki Nakashima
  • Jeong-Hun KangEmail author
Short Communication


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.


G 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.

Compliance with ethical standards

Conflict of interest

The authors declare that they have no conflict of interest.

Ethical approval

This article does not contain any studies with human participants or animals performed by any of the authors.


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Copyright information

© Springer-Verlag GmbH Austria, part of Springer Nature 2019

Authors and Affiliations

  1. 1.Department of MicrobiologySt. Marianna University School of MedicineKawasakiJapan
  2. 2.Center for Advanced Medical Innovation, Kyushu UniversityFukuokaJapan
  3. 3.Biomedical Research InstituteNational Institute of Advanced Industrial Science and Technology (AIST)IkedaJapan
  4. 4.AIST-Osaka University Advanced Photonics and Biosensing Open Innovation Laboratory, AISTSuitaJapan
  5. 5.Division of Biopharmaceutics and PharmacokineticsNational Cerebral and Cardiovascular Center Research InstituteSuitaJapan

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