Astbury Centre for Structural Molecular Biology and Institute of Molecular and Cellular Biology, Faculty of Biological Sciences, University of Leeds, Leeds LS2 9JT, UK.
Biochemistry. 2010 Feb 16;49(6):1268-80. doi: 10.1021/bi901738k.
To investigate the role of the active site copper in Escherichia coli copper amine oxidase (ECAO), we initiated a metal-substitution study. Copper reconstitution of ECAO (Cu-ECAO) restored only approximately 12% wild-type activity as measured by k(cat(amine)). Treatment with EDTA, to remove exogenous divalent metals, increased Cu-ECAO activity but reduced the activity of wild-type ECAO. Subsequent addition of calcium restored wild-type ECAO and further enhanced Cu-ECAO activities. Cobalt-reconstituted ECAO (Co-ECAO) showed lower but significant activity. These initial results are consistent with a direct electron transfer from TPQ to oxygen stabilized by the metal. If a Cu(I)-TPQ semiquinone mechanism operates, then an alternative outer-sphere electron transfer must also exist to account for the catalytic activity of Co-ECAO. The positive effect of calcium on ECAO activity led us to investigate the peripheral calcium binding sites of ECAO. Crystallographic analysis of wild-type ECAO structures, determined in the presence and absence of EDTA, confirmed that calcium is the normal ligand of these peripheral sites. The more solvent exposed calcium can be easily displaced by mono- and divalent cations with no effect on activity, whereas removal of the more buried calcium ion with EDTA resulted in a 60-90% reduction in ECAO activity and the presence of a lag phase, which could be overcome under oxygen saturation or by reoccupying the buried site with various divalent cations. Our studies indicate that binding of metal ions in the peripheral sites, while not essential, is important for maximal enzymatic activity in the mature enzyme.
为了研究大肠杆菌铜胺氧化酶(ECAO)活性部位铜的作用,我们启动了一项金属取代研究。铜再生成 ECAO(Cu-ECAO)仅恢复了约 12%的野生型活性,这是通过 k(cat(amine))测量得出的。用 EDTA(乙二胺四乙酸)处理以去除外源二价金属,增加了 Cu-ECAO 的活性,但降低了野生型 ECAO 的活性。随后添加钙恢复了野生型 ECAO,并进一步增强了 Cu-ECAO 的活性。钴再生成的 ECAO(Co-ECAO)表现出较低但仍具有显著活性。这些初步结果与 TPQ 与金属稳定的氧之间直接电子转移一致。如果 Cu(I)-TPQ 半醌机制起作用,那么必须存在替代的外层电子转移,以解释 Co-ECAO 的催化活性。钙对 ECAO 活性的积极影响促使我们研究 ECAO 的外围钙结合位点。在存在和不存在 EDTA 的情况下确定的野生型 ECAO 结构的晶体学分析证实,钙是这些外围位点的正常配体。更暴露在溶剂中的钙可以很容易地被单价和二价阳离子取代,而不会对活性产生影响,而 EDTA 去除更埋在里面的钙离子会导致 ECAO 活性降低 60-90%,并且存在滞后期,在氧气饱和或用各种二价阳离子重新占据埋置位点的情况下,该滞后期可以克服。我们的研究表明,外围位点金属离子的结合虽然不是必需的,但对于成熟酶的最大酶活性很重要。