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微粒体羟化酶与葡糖醛酸基转移酶之间的关系。

Relationship between microsomal hydroxylase and glucuronyltransferase.

作者信息

Remmer H, Bock K W, Rexer B

出版信息

Adv Exp Med Biol. 1975;58(00):335-41. doi: 10.1007/978-1-4615-9026-2_23.

Abstract

These experiments did not answer the question of whether one or several UDG-glucuronyltransferases are present in endoplasmic membranes of the liver. However, they present results which indicate that the glucuronlytransferase (s) have several properties in common with the hydroxylating cytochrome P-450 dependent enzyme system: the inducibility (which differs considerably after pretreatment with phenobarbital or 3-methylcholanthrene), the sex specificity, and the inhibition by the same compounds. The most obvious difference between the systems is the alteration of the enzyme activities after solubilization of the membranes by sonication or use of detergents.. On solubilization, the activity of the glucuronyltransferase (s) increases, whereas the opposite is true for the hydroxylating system which may lose one or several components essential for its activity (such as the NADPH dependent reductase). Our experiments can best be interpreted by assuming a common micro-environment around the enzymes produced by lipids and proteins which modulate both the rate of hydroxylation and that of glucuronyl-conjugation of drugs.

摘要

这些实验并未回答肝脏内质膜中存在一种还是几种尿苷二磷酸葡糖醛酸基转移酶的问题。然而,实验结果表明,葡糖醛酸基转移酶与依赖细胞色素P-450的羟化酶系统有几个共同特性:可诱导性(苯巴比妥或3-甲基胆蒽预处理后差异很大)、性别特异性以及被相同化合物抑制。这两个系统最明显的差异在于通过超声处理或使用去污剂使膜溶解后酶活性的变化。溶解后,葡糖醛酸基转移酶的活性增加,而羟化系统则相反,其可能会失去一种或几种对其活性至关重要的成分(如依赖烟酰胺腺嘌呤二核苷酸磷酸的还原酶)。假设脂质和蛋白质产生的围绕酶的共同微环境调节药物的羟化速率和葡糖醛酸基结合速率,能最好地解释我们的实验结果。

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