van der Wijk Thea, Blanchetot Christophe, Overvoorde John, den Hertog Jeroen
Hubrecht Laboratory, Netherland Institute for Developmental Biology, Uppsalalaan 8, Utrecht, 3584 CT, The Netherlands.
J Biol Chem. 2003 Apr 18;278(16):13968-74. doi: 10.1074/jbc.M300632200. Epub 2003 Feb 11.
Receptor protein-tyrosine phosphatase alpha (RPTP alpha) constitutively forms dimers in the membrane, and activity studies with forced dimer mutants of RPTP alpha revealed that rotational coupling of the dimer defines its activity. The hemagglutinin (HA) tag of wild type RPTP alpha and of constitutively dimeric, active RPTP alpha-F135C with a disulfide bond in the extracellular domain was not accessible for antibody, whereas the HA tag of constitutively dimeric, inactive RPTP alpha-P137C was. All three proteins were expressed on the plasma membrane to a similar extent, and the accessibility of their extracellular domains did not differ as determined by biotinylation studies. Dimerization was required for masking the HA tag, and we identified a region in the N terminus of RPTP alpha that was essential for the effect. Oxidative stress has been shown to induce a conformational change of the membrane distal PTP domain (RPTP alpha-D2). Here we report that H(2)O(2) treatment of cells induced a change in rotational coupling in RPTP alpha dimers as detected using accessibility of an HA tag in the extracellular domain as a read-out. The catalytic site Cys(723) in RPTP alpha-D2, which was required for the conformational change of RPTP alpha-D2 upon H(2)O(2) treatment, was essential for the H(2)O(2)-induced increase in accessibility. These results show for the first time that a conformational change in the intracellular domain of RPTP alpha led to a change in conformation of the extracellular domains, indicating that RPTPs have the capacity for inside-out signaling.
受体蛋白酪氨酸磷酸酶α(RPTPα)在膜中组成性地形成二聚体,对RPTPα的强制二聚体突变体进行的活性研究表明,二聚体的旋转偶联决定了其活性。野生型RPTPα以及细胞外结构域带有二硫键的组成性二聚体、活性RPTPα - F135C的血凝素(HA)标签不能被抗体识别,而组成性二聚体、无活性的RPTPα - P137C的HA标签则可以被识别。这三种蛋白在质膜上的表达程度相似,通过生物素化研究确定它们细胞外结构域的可及性没有差异。二聚化是掩盖HA标签所必需的,并且我们在RPTPα的N末端鉴定出一个对该效应至关重要的区域。氧化应激已被证明可诱导膜远端PTP结构域(RPTPα - D2)的构象变化。在此我们报告,以细胞外结构域中HA标签的可及性作为读出指标,用H₂O₂处理细胞可诱导RPTPα二聚体的旋转偶联发生变化。RPTPα - D2中催化位点Cys⁷²³是H₂O₂处理后RPTPα - D2构象变化所必需的,它对于H₂O₂诱导的可及性增加至关重要。这些结果首次表明,RPTPα细胞内结构域的构象变化导致了细胞外结构域的构象变化,这表明RPTP具有从内向外信号传导的能力。