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)
复制标题
G 蛋白偶联受体激酶 2 (GRK2) 的高亲和力肽底物
DOI：
10.1007/s00726-019-02735-0
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发表时间：
2019
期刊：
影响因子：
3.5
通讯作者：
Jeong-Hun Kang
中科院分区：
文献类型：
--
作者：
Daisuke Asai;Masaharu Murata;Riki Toita;Takahito Kawano;Hideki Nakashima;Jeong-Hun Kang
我们合成了先前鉴定的β-微管蛋白衍生的G蛋白偶联受体激酶2（GKR 2）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，目的是寻找GRK 2的高亲和力肽底物。GR-11-1-C对GRK 2表现出高亲和力，但对GKR 5表现出非常低的亲和力。GKR 2的特异性和敏感性均高于GR-11-1和GR-11-1-N。这些发现将有助于设计探测GKR 2介导的细胞内信号通路的工具，以及GRK 2特异性药物。
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.