Chirgwin J M, Parsons T F, Noltmann E A
J Biol Chem. 1975 Sep 25;250(18):7277-9.
In contrast to the strongly pH-dependent inhibition of phosphoglucose isomerase by substrate analogues with a free carboxyl group, inhibition of this enzyme by neutral sugar phosphates is essentially invariant between pH 7 and 9. Competitive inhibition constants for glucitol 6-phosphate (40 muM), arabinose 5-phosphate (50 muM), and erythritol 4-phosphate (100 muM) were found to be of the same order of magnitude as that reported previously for substrate binding constants (50 to 240 muM). The unique exception is erythrose 4-phosphate whose Ki (0.7 muM, independent of pH) reflects a tightness of binding similar to that found at pH values near or below neutrality for the transition state analogue 5-phosphorarabinonate. The pH independence of inhibition by erythrose 4-phosphate and other neutral sugar phosphates may reflect a mode and locus of binding to phosphoglucose isomerase different from that of the aldonate inhibitors.
与具有游离羧基的底物类似物对磷酸葡萄糖异构酶的强烈pH依赖性抑制相反,中性糖磷酸酯对该酶的抑制在pH 7至9之间基本不变。发现磷酸葡萄糖醇(40 μM)、磷酸阿拉伯糖(50 μM)和磷酸赤藓醇(100 μM)的竞争性抑制常数与先前报道的底物结合常数(50至240 μM)处于同一数量级。唯一的例外是磷酸赤藓糖,其Ki(0.7 μM,与pH无关)反映出与过渡态类似物5-磷酸阿拉伯糖酸在接近或低于中性的pH值下所发现的结合紧密程度相似。磷酸赤藓糖和其他中性糖磷酸酯抑制作用的pH独立性可能反映了与醛糖酸抑制剂不同的与磷酸葡萄糖异构酶结合的方式和位点。