Department of Microbiology, St. Marianna University School of Medicine, 2-16-1 Sugao, Miyamae, Kawasaki, 216-8511, Japan.
Center for Advanced Medical Innovation, Kyushu University, 3-1-1 Maidashi, Higashi-ku, Fukuoka, 812-8582, Japan.
Amino Acids. 2019 Jun;51(6):973-976. doi: 10.1007/s00726-019-02735-0. Epub 2019 Apr 19.
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.
我们合成了之前鉴定出的β-微管蛋白衍生的 G 蛋白偶联受体激酶 2（GKR2）肽（GR-11-1；DEMEFTEAESNMN）及其氨基末端延伸（GR-11-1-N；GEGMDEMEFTEAESNMN）和羧基末端延伸（GR-11-1-C；DEMEFTEAESNMNDLVSEYQ）肽，旨在寻找高亲和力的 GRK2 肽底物。GR-11-1-C 对 GRK2 具有高亲和力，但对 GKR5 的亲和力非常低。它对 GKR2 的特异性和敏感性大于 GR-11-1 和 GR-11-1-N。这些发现对于设计用于探测 GKR2 介导的细胞内信号通路的工具以及 GRK2 特异性药物应该是有用的。
