Davis A M, Regan A C, Williams A
University Chemical Laboratories, Canterbury, England.
Biochemistry. 1988 Dec 13;27(25):9042-7. doi: 10.1021/bi00425a024.
The title esters are demonstrated to be specific substrates of bovine pancreatic ribonuclease A (EC 3.1.27.5). The Brønsted dependence of kcat/Km at pH 7.50 for the enzyme-catalyzed cyclization versus the pKa of the leaving phenol exhibits two regression lines of almost identical slope for respectively 2-chlorophenols and 2,6-unsubstituted phenols: log kcat/Km = -0.20 pKa ArOH + 5.47 (n = 5, r = 0.957); log kcat/Km = -0.17 pKa ArOH + 5.79 (n = 4, r = 0.965). Comparison of the Brønsted beta 1g's with that for the standard reaction where imidazole catalyzes the cyclization (beta 1g = -0.59) indicates considerably less development of negative charge on the leaving oxygen in the enzyme case, providing experimental evidence for the hypothesis that electrophilic assistance is involved in catalysis. The existence of two essentially parallel Brønsted correlations is not reflected in the standard reaction of substrate with imidazole. Modeling studies indicate that the phenyl ring of the substrate can take up a range of positions away from the active site; the presence of ortho chloro substituents considerably restricts the motion of the phenyl leaving group.
已证明标题酯是牛胰核糖核酸酶A(EC 3.1.27.5)的特异性底物。在pH 7.50条件下,酶催化环化反应的kcat/Km对离去酚的pKa的布朗斯特相关性显示,对于2-氯酚和2,6-未取代酚分别有两条斜率几乎相同的回归线:log kcat/Km = -0.20 pKa ArOH + 5.47(n = 5,r = 0.957);log kcat/Km = -0.17 pKa ArOH + 5.79(n = 4,r = 0.965)。将这些布朗斯特β1g值与咪唑催化环化的标准反应的β1g值(β1g = -0.59)进行比较,表明在酶催化的情况下,离去氧上负电荷的发展程度要小得多,这为亲电辅助参与催化这一假设提供了实验证据。底物与咪唑的标准反应中并未体现出两条基本平行的布朗斯特相关性的存在。模型研究表明,底物的苯环可以在远离活性位点的一系列位置占据;邻位氯取代基的存在极大地限制了苯基离去基团的运动。