Craxton A, Erneux C, Shears S B
Inositol Lipid Section, National Institute of Environmental Health Sciences, National Institutes of Health, Research Triangle Park, North Carolina 27709.
J Biol Chem. 1994 Feb 11;269(6):4337-42.
Liver homogenates phosphorylated inositol 1,4,5,6-tetrakisphosphate exclusively to inositol 1,3,4,5,6-pentakisphosphate. Approximately 30% of this phosphorylating activity was associated with the particulate fraction of the cell, in contrast to the inositol 3,4,5,6-tetrakisphosphate 1-kinase, which was 90% soluble. This soluble 1-kinase activity was resolved from the soluble activity that phosphorylated inositol 1,4,5,6-tetrakisphosphate by anion-exchange chromatography. The two phosphorylating activities were also found to be differentially inhibited by inositol 1,3,4-trisphosphate (IC50 for 3-kinase > 100 microM; IC50 for 1-kinase < 1 microM). Thus, we have demonstrated that inositol 1,4,5,6-tetrakisphosphate is phosphorylated directly by a 3-kinase, and inositol 3,4,5,6-tetrakisphosphate is not an obligatory intermediate, in contrast to one previous model (Oliver, K. G., Putney, J. W., Jr., Obie, J. F., and Shears, S. B. (1992) J. Biol. Chem. 267, 21528-21534). Inositol 1,4,5,6-tetrakisphosphate 3-kinase was inhibited by inositol 1,3,4,6-tetrakisphosphate (IC50, 1 microM). Soluble inositol 1,4,5,6-tetrakisphosphate 3-kinase and inositol 1,4,5-trisphosphate 3-kinase were resolved by anion-exchange chromatography. Furthermore, cDNA clones of two isozymes of inositol 1,4,5-trisphosphate 3-kinase from rat and human brain did not phosphorylate inositol 1,4,5,6-tetrakisphosphate. Thus, these two 3-kinase activities are performed by distinct enzymes.
肝脏匀浆仅将肌醇1,4,5,6 - 四磷酸磷酸化为肌醇1,3,4,5,6 - 五磷酸。与90%可溶的肌醇3,4,5,6 - 四磷酸1 - 激酶相反,这种磷酸化活性约30%与细胞的颗粒部分相关。通过阴离子交换色谱法,这种可溶的1 - 激酶活性与磷酸化肌醇1,4,5,6 - 四磷酸的可溶活性得以分离。还发现这两种磷酸化活性受到肌醇1,3,4 - 三磷酸的不同抑制(3 - 激酶的IC50>100微摩尔;1 - 激酶的IC50<1微摩尔)。因此,我们已经证明肌醇1,4,5,6 - 四磷酸直接由一种3 - 激酶磷酸化,并且与之前的一个模型(Oliver, K. G., Putney, J. W., Jr., Obie, J. F., and Shears, S. B. (1992) J. Biol. Chem. 267, 21528 - 21534)不同,肌醇3,4,5,6 - 四磷酸不是必需的中间体。肌醇1,4,5,6 - 四磷酸3 - 激酶受到肌醇1,3,4,6 - 四磷酸的抑制(IC50,1微摩尔)。通过阴离子交换色谱法分离了可溶的肌醇1,4,5,6 - 四磷酸3 - 激酶和肌醇1,4,5 - 三磷酸3 - 激酶。此外,来自大鼠和人类大脑的两种肌醇1,4,5 - 三磷酸3 - 激酶同工酶的cDNA克隆不能磷酸化肌醇1,4,5,6 - 四磷酸。因此,这两种3 - 激酶活性由不同的酶执行。