Department of Life Sciences, Ben-Gurion University , P.O. Box 653, Beer-Sheva 84105, Israel.
Biochemistry. 2012 Oct 9;51(40):7940-52. doi: 10.1021/bi300893v. Epub 2012 Sep 25.
Glyoxylate carboligase (GCL) is a thiamin diphosphate (ThDP)-dependent enzyme, which catalyzes the decarboxylation of glyoxylate and ligation to a second molecule of glyoxylate to form tartronate semialdehyde (TSA). This enzyme is unique among ThDP enzymes in that it lacks a conserved glutamate near the N1' atom of ThDP (replaced by Val51) or any other potential acid-base side chains near ThDP. The V51D substitution shifts the pH optimum to 6.0-6.2 (pK(a) of 6.2) for TSA formation from pH 7.0-7.7 in wild-type GCL. This pK(a) is similar to the pK(a) of 6.1 for the 1',4'-iminopyrimidine (IP)-4'-aminopyrimidinium (APH(+)) protonic equilibrium, suggesting that the same groups control both ThDP protonation and TSA formation. The key covalent ThDP-bound intermediates were identified on V51D GCL by a combination of steady-state and stopped-flow circular dichroism methods, yielding rate constants for their formation and decomposition. It was demonstrated that active center variants with substitution at I393 could synthesize (S)-acetolactate from pyruvate solely, and acetylglycolate derived from pyruvate as the acetyl donor and glyoxylate as the acceptor, implying that this substitutent favored pyruvate as the donor in carboligase reactions. Consistent with these observations, the I393A GLC variants could stabilize the predecarboxylation intermediate analogues derived from acetylphosphinate, propionylphosphinate, and methyl acetylphosphonate in their IP tautomeric forms notwithstanding the absence of the conserved glutamate. The role of the residue at the position occupied typically by the conserved Glu controls the pH dependence of kinetic parameters, while the entire reaction sequence could be catalyzed by ThDP itself, once the APH(+) form is accessible.
乙醛酸 carboligase (GCL) 是一种硫胺素二磷酸 (ThDP) 依赖性酶,它催化乙醛酸的脱羧和与第二个乙醛酸分子的连接,形成琥珀酸半醛 (TSA)。该酶在 ThDP 酶中是独特的,因为它在 ThDP 的 N1' 原子附近缺乏保守的谷氨酸(被 Val51 取代)或 ThDP 附近的任何其他潜在酸碱侧链。V51D 取代将 TSA 形成的 pH 最佳值从野生型 GCL 的 pH 7.0-7.7 转移到 6.0-6.2(pK(a)为 6.2)。该 pK(a)与 1',4'-亚氨基嘧啶 (IP)-4'-氨基嘧啶鎓 (APH(+)) 质子平衡的 pK(a)相似 6.1,表明相同的基团控制 ThDP 质子化和 TSA 形成。通过稳态和停流圆二色性方法的组合,在 V51D GCL 上鉴定了关键的共价 ThDP 结合中间体,得出了它们形成和分解的速率常数。结果表明,在 I393 处取代的活性中心变体可以仅从丙酮酸合成 (S)-乙酰乳酸,并且源自丙酮酸的乙酰甘油酸作为乙酰供体和乙醛酸作为受体,这意味着该取代基有利于在 carboligase 反应中丙酮酸作为供体。与这些观察结果一致,I393A GLC 变体可以稳定源自乙酰膦酸盐、丙酰膦酸盐和甲基乙酰膦酸盐的 predecarboxylation 中间体类似物,尽管没有保守的谷氨酸。占据通常由保守 Glu 占据的位置的残基控制动力学参数的 pH 依赖性,而一旦 APH(+) 形式可及,整个反应序列可以由 ThDP 本身催化。