Julien T, Betakis E, Zaki L
Max-Planck-Institut für Biophysik, Frankfurt am Main, F.R.G.
Biochim Biophys Acta. 1990 Jul 9;1026(1):43-50. doi: 10.1016/0005-2736(90)90330-q.
A series of arginine-specific reagents with different size and polarity have been synthesized and their inhibitory potency on sulfate exchange in resealed ghosts has been investigated. The synthesized phenylglyoxal derivatives p-nitro-, p-methyl-, p-hydroxy-, p-carboxy-, p-sulfo-, and p-azido-phenylglyoxal are found to be potent inhibitors of anion transport. The reaction between the cells and azidophenylglyoxal was performed in the dark. Exposure of the modified cells to the light was not followed by an increase in the inhibition. No cross-linking products were visible after gel electrophoresis. The rate of inactivation of sulfate flux with these reagents obeyed pseudo-first-order kinetics and increases with increasing reagents concentration and pH. Prolonged incubation of the cells with these reagents results in almost complete inhibition of the transport system. The positively charged phenylglyoxal derivative 4-(trimethylammonioacetylamido)phenylglyoxal was not able to inhibit the transport system. The hydrophobic character and the electronic properties of these reagents do not correlate with their inhibitory potency. Their electrostatic and steric effects seem to play the major role in their action.
已经合成了一系列具有不同大小和极性的精氨酸特异性试剂，并研究了它们对重封膜泡中硫酸盐交换的抑制效力。发现合成的苯乙二醛衍生物对硝基、对甲基、对羟基、对羧基、对磺基和对叠氮基苯乙二醛是阴离子转运的有效抑制剂。细胞与叠氮基苯乙二醛之间的反应在黑暗中进行。将修饰后的细胞暴露于光下后，抑制作用并未增强。凝胶电泳后未可见交联产物。这些试剂使硫酸盐通量失活的速率符合假一级动力学，且随试剂浓度和pH值的增加而增加。用这些试剂长时间孵育细胞会导致转运系统几乎完全被抑制。带正电荷的苯乙二醛衍生物4-(三甲基铵乙酰氨基)苯乙二醛不能抑制转运系统。这些试剂的疏水特性和电子性质与其抑制效力无关。它们的静电和空间效应似乎在其作用中起主要作用。
