丙烯醛，一种脱氧核糖5 - 磷酸醛缩酶的不可逆活性位点导向抑制剂？
Acrolein, an irreversible active-site-directed inhibitor of deoxyribose 5-phosphate aldolase?
作者信息
Wilton D C
出版信息
Biochem J. 1976 Feb 1;153(2):495-7. doi: 10.1042/bj1530495.
Abstract
The enzyme deoxyribose 5-phosphate aldolase was irreversibly inactivated by the substrate analogue acrolein with a pseudo-first-order rate constant of 0.324 min-1 and a Ki (apparent) of 2.7 x 10(-4) m. No inactivation was observed after prolonged incubation with the epoxide analogues glycidol phosphate and glycidaldehyde. It is suggested that the acrolein is first activated by forming a Schiff base with the enzyme active-site lysine residue and it is the activated inhibitor that reacts with a suitable-active-site nucleophile.
摘要
脱氧核糖5 - 磷酸醛缩酶被底物类似物丙烯醛不可逆地失活，其假一级反应速率常数为0.324 min⁻¹，表观抑制常数Ki为2.7×10⁻⁴ m。与环氧类似物甘油磷酸酯和甘油醛长时间孵育后未观察到失活现象。有人提出，丙烯醛首先通过与酶活性位点的赖氨酸残基形成席夫碱而被激活，正是这种活化的抑制剂与合适的活性位点亲核试剂发生反应。
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