Stathopulos Peter B, Li Guang-Yao, Plevin Michael J, Ames James B, Ikura Mitsuhiko
Division of Signaling Biology and Department of Medical Biophysics, Ontario Cancer Institute and University of Toronto, Toronto M5G 1L7, Ontario, Canada.
J Biol Chem. 2006 Nov 24;281(47):35855-62. doi: 10.1074/jbc.M608247200. Epub 2006 Oct 3.
Stromal interaction molecule 1 (STIM1) has recently been identified as a key player in store-operated Ca2+ entry. Endoplasmic reticulum (ER) luminal Ca2+ depletion results in STIM1 redistribution from ER membrane homogeneity to distinctly localized aggregates near the plasma membrane; these changes precede and are linked to cytoplasmic Ca2+ influx via Ca2+ release-activated channels (CRACs). The molecular mechanisms initiating ER STIM1 redistribution and plasma membrane CRAC activity are not well understood. We recombinantly expressed the Ca2+-sensing region of STIM1 consisting of the EF-hand together with the sterile alpha-motif (SAM) domain (EF-SAM) to investigate its Ca2+-related conformational and biochemical features. We demonstrate that Ca2+-loaded EF-SAM (holo) contains high alpha-helicity, whereas EF-SAM in the absence of Ca2+ (apo) is much less compact. Accordingly, the melting temperature (Tm) of the holoform is approximately 25 degrees C higher than apoform; heat and urea-derived thermodynamic parameters indicate a Ca2+-induced stabilization of 3.2 kcal mol(-1). We show that holoEF-SAM exists as a monomer, whereas apoEF-SAM readily forms a dimer and/or oligomer, and that oligomer to monomer transitions and vice versa are at least in part mediated by changes in surface hydrophobicity. Additionally, we find that the Ca2+ binding affinity of EF-SAM is relatively low with an apparent dissociation constant (Kd) of approximately 0.2-0.6 mM and a binding stoichiometry of 1. Our results suggest that EF-SAM actively participates in and is the likely the molecular trigger initiating STIM1 punctae formation via large conformational changes. The low Ca2+ affinity of EF-SAM is reconciled with the confirmed role of STIM1 as an ER Ca2+ sensor.
基质相互作用分子1(STIM1)最近被确定为钙库操纵性钙离子内流的关键参与者。内质网(ER)腔内钙离子耗竭导致STIM1从内质网膜的均匀分布重新分布到质膜附近明显定位的聚集体;这些变化先于并与通过钙离子释放激活通道(CRACs)的细胞质钙离子内流相关。启动内质网STIM1重新分布和质膜CRAC活性的分子机制尚不清楚。我们重组表达了由EF手型结构域和无活性α基序(SAM)结构域组成的STIM1钙离子感应区域(EF-SAM),以研究其与钙离子相关的构象和生化特征。我们证明,结合钙离子的EF-SAM(全酶形式)具有高α螺旋度,而缺乏钙离子的EF-SAM(脱辅基形式)则结构松散得多。因此,全酶形式的解链温度(Tm)比脱辅基形式高约25℃;热和尿素衍生的热力学参数表明钙离子诱导的稳定性为3.2千卡/摩尔(-1)。我们表明,全酶EF-SAM以单体形式存在,而脱辅基EF-SAM容易形成二聚体和/或寡聚体,并且寡聚体到单体的转变以及反之亦然至少部分由表面疏水性的变化介导。此外,我们发现EF-SAM的钙离子结合亲和力相对较低,表观解离常数(Kd)约为0.2 - 0.6 mM,结合化学计量比为1。我们的结果表明,EF-SAM积极参与并可能是通过大的构象变化启动STIM1点状结构形成的分子触发因素。EF-SAM的低钙离子亲和力与STIM1作为内质网钙离子传感器的已证实作用相一致。