From the Vascular Biology Research Centre, Institute of Molecular and Clinical Sciences, St George's University of London, United Kingdom.
Arterioscler Thromb Vasc Biol. 2018 Sep;38(9):2091-2102. doi: 10.1161/ATVBAHA.118.311360.
Objective- In renal arteries, inhibitors of G protein βγ subunits (Gβγ) reduce Kv7 activity and inhibit Kv7-dependent receptor-mediated vasorelaxations. However, the mechanisms underlying receptor-mediated relaxation are artery specific. Consequently, the aim of this study was to ascertain the role of Gβγ in Kv7-dependent vasorelaxations of the rat vasculature. Approach and Results- Isometric tension recording was performed in isolated rat renal, mesenteric, and cerebral arteries to study isoproterenol and calcitonin gene-related peptide relaxations. Kv7.4 was knocked down via morpholino transfection while inhibition of Gβγ was investigated with gallein and M119K. Proximity ligation assay was performed on isolated myocytes to study the association between Kv7.4 and G protein β subunits or signaling intermediaries. Isoproterenol or calcitonin gene-related peptide-induced relaxations were attenuated by Kv7.4 knockdown in all arteries studied. Inhibition of Gβγ with gallein or M119K had no effect on isoproterenol-mediated relaxations in mesenteric artery but had a marked effect on calcitonin gene-related peptide-induced responses in mesenteric artery and cerebral artery and isoproterenol responses in renal artery. Isoproterenol increased association with Kv7.4 and Rap1a in mesenteric artery which were not sensitive to gallein, whereas in renal artery, isoproterenol increased Kv7.4-AKAP (A-kinase anchoring protein) associations in a gallein-sensitive manner. Conclusions- The Gβγ-Kv7 relationship differs between vessels and is an essential requirement for AKAP, but not Rap-mediated regulation of the channel.
在肾动脉中,G 蛋白 βγ 亚基(Gβγ)抑制剂可降低 Kv7 活性并抑制 Kv7 依赖性受体介导的血管舒张。然而,受体介导的舒张机制是动脉特异性的。因此,本研究的目的是确定 Gβγ 在大鼠血管中 Kv7 依赖性血管舒张中的作用。
在分离的大鼠肾、肠系膜和脑动脉中进行等长张力记录,以研究异丙肾上腺素和降钙素基因相关肽的舒张作用。通过 morpholino 转染敲低 Kv7.4,并用 gallein 和 M119K 抑制 Gβγ。在分离的心肌细胞上进行接近连接测定,以研究 Kv7.4 与 G 蛋白 β 亚基或信号中间物的关联。异丙肾上腺素或降钙素基因相关肽诱导的舒张作用在所有研究的动脉中均被 Kv7.4 敲低所减弱。Gallein 或 M119K 抑制 Gβγ对肠系膜动脉中异丙肾上腺素介导的舒张没有影响,但对肠系膜动脉和脑动脉中降钙素基因相关肽诱导的反应以及肾动脉中异丙肾上腺素的反应有显著影响。异丙肾上腺素增加了与肠系膜动脉中 Kv7.4 和 Rap1a 的关联,而这些关联对 gallein 不敏感,而在肾动脉中,异丙肾上腺素以 gallein 敏感的方式增加了 Kv7.4-AKAP(蛋白激酶 A 锚定蛋白)的关联。
Gβγ-Kv7 关系在血管之间存在差异,是 AKAP 但不是 Rap 调节通道的必需条件。