Woo K M, Chung W J, Ha D B, Goldberg A L, Chung C H
Department of Zoology, College of Natural Sciences, Seoul National University, Korea.
J Biol Chem. 1989 Feb 5;264(4):2088-91.
Protease Ti, a new ATP-dependent protease in Escherichia coli, degrades proteins and ATP in a linked process, but these two hydrolytic functions are catalyzed by distinct components of the enzyme. To clarify the enzyme's specificity and the role of ATP, a variety of fluorogenic peptides were tested as possible substrates for protease Ti or its two components. Protease Ti rapidly hydrolyzed N-succinyl(Suc)-Leu-Tyr-amidomethylcoumarin (AMC) (Km = 1.3 mM) which is not degraded by protease La, the other ATP-dependent protease in E. coli. Protease Ti also hydrolyzed, but slowly, Suc-Ala-Ala-Phe-AMC and Suc-Leu-Leu-Val-Tyr-AMC. However, it showed little or no activity against basic or other hydrophobic peptides, including ones degraded rapidly by protease La. Component P, which contains the serine-active site, by itself rapidly degrades the same peptides as the intact enzyme. Addition of component A, which contains the ATP-hydrolyzing site and is necessary for protein degradation, had little or no effect on peptide hydrolysis. N-Ethylmaleimide, which inactivates the ATPase, did not inhibit peptide hydrolysis. In addition, this peptide did not stimulate the ATPase activity of component A (unlike protein substrates). Thus, although the serine-active site on component P is unable to degrade proteins, it is fully functional against small peptides in the absence of ATP. At high concentrations, Suc-Leu-Tyr-AMC caused a complete inhibition of casein breakdown, and diisopropylfluorophosphate blocked similarly the hydrolysis of both protein and peptide substrates. Thus, both substrates seem to be hydrolyzed at the same active site on component P, and ATP hydrolysis by component A either unmasks or enlarges this proteolytic site such that large proteins can gain access to it.
蛋白酶Ti是大肠杆菌中一种新的ATP依赖性蛋白酶,在一个相关过程中降解蛋白质和ATP,但这两种水解功能由该酶的不同组分催化。为了阐明该酶的特异性和ATP的作用,测试了多种荧光肽作为蛋白酶Ti或其两个组分的可能底物。蛋白酶Ti能快速水解N-琥珀酰(Suc)-亮氨酸-酪氨酸-氨基甲基香豆素(AMC)(Km = 1.3 mM),而大肠杆菌中的另一种ATP依赖性蛋白酶蛋白酶La不能降解该底物。蛋白酶Ti也能水解Suc-丙氨酸-丙氨酸-苯丙氨酸-AMC和Suc-亮氨酸-亮氨酸-缬氨酸-酪氨酸-AMC,但速度较慢。然而,它对碱性或其他疏水肽几乎没有活性,包括那些被蛋白酶La快速降解的肽。含有丝氨酸活性位点的组分P自身就能快速降解与完整酶相同的肽。添加含有ATP水解位点且是蛋白质降解所必需的组分A,对肽水解几乎没有影响。使ATP酶失活的N-乙基马来酰亚胺不抑制肽水解。此外,这种肽不会刺激组分A的ATP酶活性(与蛋白质底物不同)。因此,尽管组分P上的丝氨酸活性位点不能降解蛋白质,但在没有ATP的情况下,它对小肽具有完全功能。在高浓度下,Suc-亮氨酸-酪氨酸-AMC会完全抑制酪蛋白的分解,二异丙基氟磷酸酯同样会阻断蛋白质和肽底物的水解。因此,两种底物似乎在组分P上的同一活性位点被水解,组分A的ATP水解要么暴露要么扩大了这个蛋白水解位点,使得大蛋白质能够接近它。