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

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

  • Amino Acids. 2019 Jun;51(6):973-976. doi: 10.1007/s00726-019-02735-0.
Daisuke Asai 1,  Masaharu Murata 2,  Riki Toita 3 4,  Takahito Kawano 2,  Hideki Nakashima 5,  Jeong-Hun Kang 6
Affiliations

Affiliations

  • 1 Department of Microbiology, St. Marianna University School of Medicine, 2-16-1 Sugao, Miyamae, Kawasaki, 216-8511, Japan. asai@marianna-u.ac.jp.
  • 2 Center for Advanced Medical Innovation, Kyushu University, 3-1-1 Maidashi, Higashi-ku, Fukuoka, 812-8582, Japan.
  • 3 Biomedical Research Institute, National Institute of Advanced Industrial Science and Technology (AIST), 1-8-31 Midorigaoka, Ikeda, Osaka, 563-8577, Japan.
  • 4 AIST-Osaka University Advanced Photonics and Biosensing Open Innovation Laboratory, AIST, 2-1 Yamadaoka, Suita, Osaka, 565-0871, Japan.
  • 5 Department of Microbiology, St. Marianna University School of Medicine, 2-16-1 Sugao, Miyamae, Kawasaki, 216-8511, Japan.
  • 6 Division of Biopharmaceutics and Pharmacokinetics, National Cerebral and Cardiovascular Center Research Institute, 5-7-1 Fujishiro-dai, Suita, Osaka, 565-8565, Japan. jrjhkang@ncvc.go.jp.
PMID: 31004228 DOI: 10.1007/s00726-019-02735-0
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.

Keywords

Amino acid residue; Cellular signal transduction pathway; Consensus sequence; G protein-coupled receptor kinase; Phosphorylation.

Figures
Products
嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z