G protein-coupled receptor kinase 4: role in hypertension.
G protein-coupled receptor kinase 4: role in hypertension.
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DOI：
10.1161/hypertensionaha.115.05189
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发表时间：
2015-06
期刊：
影响因子：
--
通讯作者：
Zeng C
中科院分区：
文献类型：
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作者：
Yang J;Villar VA;Jones JE;Jose PA;Zeng C
在人类基因组中有超过800种已知的GPCR，但只有7种GRK被确定。所有GRK具有相似的一般结构：高度保守的中心蛋白激酶结构域，插入在G蛋白信号传导同源结构域的调节子中，其保持激酶结构域磷酸化活化的GPCR的能力。GRK的前20个左右的氨基酸是高度保守的，而羧基尾区是GRK亚型特异性的：在GRK 1亚家族中被异戊二烯化;在GRK 2亚家族中与Gβγ结合并含有普列克底物蛋白同源结构域;在GRK 4亚家族中具有C末端螺旋/棕榈酰化位点。GRK 1亚家族（视蛋白激酶家族）由GRK 1和GRK 7组成; GRK 2样亚家族（β-肾上腺素能受体激酶家族）由GRK 2和GRK 3组成; GRK 4样亚家族由GRK 4、GRK 5和GRK 6组成。GRK 1和GRK 7几乎只存在于视网膜中并调节视蛋白。GRK 2、GRK 3、GRK 5和GRK 6普遍表达，而GRK 4仅在少数器官中表达（参见下文）。20–22
There are over 800 known GPCRs in the human genome, but only 7 GRKs have been identified. All GRKs have a similar general structure: a highly conserved central protein kinase domain, inserted in the regulator of G protein signaling homology domain that keeps the ability of the kinase domain to phosphorylate activated GPCRs. The first 20 or so amino acids of GRKs are highly conserved, whereas the carboxy tail region is GRK subtype-specific: prenylated in the GRK1 subfamily; binds to Gβγ and contains a pleckstrin homology domain in the GRK2 subfamily; and has a C-terminal helix/palmitoylation site in the GRK4 subfamily. 19 The GRK1 subfamily (opsin kinase family) consists of GRK1 and GRK7; GRK2-like subfamily (β-adrenergic receptor kinase family) consists of GRK2 and GRK3; and the GRK4-like subfamily consists of GRK4, GRK5, and GRK6. GRK1 and GRK7 are found almost exclusively in the retina and modulate opsins. GRK2, GRK3, GRK5, and GRK6 are ubiquitously expressed, whereas GRK4 is expressed in only a few organs (vide infra). 20–22