INHIBITION OF PHOSPHATASE AND SULFATASE BY TRANSITION-STATE ANALOGS
INHIBITION OF PHOSPHATASE AND SULFATASE BY TRANSITION-STATE ANALOGS
复制标题
DOI：
10.1021/bi00401a031
复制
发表时间：
1988-01-12
期刊：
影响因子：
2.9
通讯作者：
GRESSER, MJ
中科院分区：
文献类型：
--
作者：
STANKIEWICZ, PJ;GRESSER, MJ
钒酸盐，铬酸盐，草酸盐和钨酸盐的抑制常数已被确定与大肠杆菌碱性磷酸酶，马铃薯酸性磷酸酶，和黑果芸香芳基硫酸酯酶。钒酸盐是所有三种酶的有效抑制剂。两种磷酸酶的抑制作用顺序为WO 42- > MoO 42- > CrO 42-。马铃薯酸性磷酸酶的Ki值比碱性磷酸酶低约3个数量级。芳基硫酸酯酶抑制组VI含氧阴离子的反向顺序。苯酚增强钒酸盐和铬酸盐对碱性磷酸酶的抑制作用，但不影响酸性磷酸酶的抑制作用。苯酚增强金属含氧阴离子对芳基硫酸酯酶的抑制作用，其顺序为H_2VO_4- > CrO_（42）- > MoO_（42）- > WO_（42）-，N-乙酰酪氨酸乙酯增强H_2VO_4-和CrO_（42）-对芳基硫酸酯酶的抑制作用比苯酚强。很明显，金属含氧阴离子作为磷酸酶和硫酸酯酶抑制剂的有效性可以在其他溶质存在下选择性地增强。这些obervations过渡含氧阴离子对蛋白磷酸酶在体内的影响的相关性进行了讨论。
The inhibition constants for vanadate, chromate, molybdate, and tungstate have been determined with Escherichia coli alkaline phosphatase, potato acid phosphatase, and Helix pomatia aryl sulfatase. Vanadate was a potent inhibitor of all three enzymes. Inhibition of both phosphatases followed the order WO42- > MoO42- > CrO42-. The Ki values for potato acid phosphatase were about 3 orders of magnitude lower than those for alkaline phosphatase. Aryl sulfatase followed the reverse order of inhibition by group VI oxyanions. Phenol enhanced inhibition of alkaline phosphatase by vanadate and chromate but did not affect inhibition of acid phosphatase. Phenol enhanced inhibition of aryl sulfatase by metal oxyanions in all cases following the order H2VO4- > CrO42- > MoO42- > WO42-, and N-acetyltyrosine ethyl ester enhanced inhibition of aryl sulfatase by H2VO4- and CrO42- more strongly than did phenol. It is apparent that the effectiveness of metal oxyanions as inhibitors of phosphatases and sulfatases can be selectively enhanced in the presence of other solutes. The relevance of these obervations to the effects of transition oxyanions on protein phosphatases in vivo is discussed.