Department of Physiology, Wayne State University, School of Medicine, Detroit, MI 48201, USA.
Biochem J. 2012 Apr 1;443(1):249-58. doi: 10.1042/BJ20111398.
Kidney plasma membranes, which contain a single α-1 isoform of Na+/K+-ATPase, simultaneously contain two sub-conformations of E2P, differing in their rate of digoxin release in response to Na+ and ATP. Treating cells with Ang II (angiotensin II) somehow changes the conformation of both, because it differentially inhibits the rate of digoxin release. In the present study we tested whether Ang II regulates release by increasing phosphorylation at Ser11/Ser18 and Ser938. Opossum kidney cells co-expressing the AT1a receptor and either α-1.wild-type, α-1.S11A/S18A or α-1.S938A were treated with or without 10 nM Ang II for 5 min, increasing phosphorylation at the three sites. Na+/K+-ATPase was bound to digoxin-affinity columns in the presence of Na+, ATP and Mg2+. A solution containing 30 mM NaCl and 3 mM ATP eluted ~20% of bound untreated Na+/K+-ATPase (Population #1). Pre-treating cells with Ang II slowed the elution of Population #1 in α-1.wild-type and α-1.S938A, but not α-1.S11A/S18A cells. Another 50% of bound Na+/K+-ATPase (Population #2) was subsequently eluted in two phases by a solution containing 150 mM NaCl and 3 mM ATP. Ang II increased the initial rate and slowed the second phase in α-1.wild-type, but not α-1.S938A, cells. Thus Ang II changes the conformation of two forms of EP2 via differential phosphorylation.
肾血浆膜含有单一的α-1 同工型 Na+/K+-ATP 酶,同时含有两种 E2P 亚构象,它们在响应 Na+和 ATP 时的地高辛释放速率不同。用血管紧张素 II(Ang II)处理细胞会改变这两种构象,因为它会差异抑制地高辛的释放速率。在本研究中,我们测试了 Ang II 是否通过增加 Ser11/Ser18 和 Ser938 的磷酸化来调节释放。同时表达 AT1a 受体和α-1.野生型、α-1.S11A/S18A 或α-1.S938A 的负鼠肾细胞用或不用 10 nM Ang II 处理 5 分钟,增加了这三个位点的磷酸化。Na+/K+-ATP 酶在存在 Na+、ATP 和 Mg2+的情况下结合到地高辛亲和柱上。含有 30 mM NaCl 和 3 mM ATP 的溶液洗脱约 20%未处理的结合 Na+/K+-ATP 酶(#1 群体)。用 Ang II 预处理细胞会减缓α-1.野生型和α-1.S938A 细胞中#1 群体的洗脱,但不会减缓α-1.S11A/S18A 细胞的洗脱。随后,用含有 150 mM NaCl 和 3 mM ATP 的溶液分两阶段洗脱另 50%的结合 Na+/K+-ATP 酶(#2 群体)。Ang II 增加了α-1.野生型细胞的初始洗脱速率,并减缓了第二阶段,但在α-1.S938A 细胞中则没有。因此,Ang II 通过差异磷酸化改变了两种 EP2 构象。