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Updated: Jan 26, 2026

Identification of Kinase-substrate Pairs Using High Throughput Screening
Published on: August 29, 2015
A high-affinity peptide substrate for G protein-coupled receptor kinase 2 (GRK2)
Daisuke Asai1, Masaharu Murata2, Riki Toita3,4
1Department of Microbiology, St. Marianna University School of Medicine, 2-16-1 Sugao, Miyamae, Kawasaki, 216-8511, Japan. asai@marianna-u.ac.jp.
Abstract:
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.
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