药物代谢酶,特别是CYP450酶的活性调节一直是药物代谢的研究热点,大多数现有的研究都集中在转录和翻译水平上探讨化合物对其基因表达和蛋白水平的影响。但是随着研究的深入,发现在翻译后水平的修饰作用也可能对代谢酶的活性有重要影响。近年来,翻译后修饰作用对酶活性的影响越来越受到重视,并发现了一些对代谢酶活性有重要影响的修饰方式,如磷酸化、硝基化、泛素化等。本文对近年来翻译后修饰对CYP450酶活性影响的研究进行综述。
Regulation of the activity of CYP450 has always been research focus of drug metabolism. The effect of compounds on the mRNA and protein expression level of CYP450 is the main purpose of most of the existing reports. In recent years, the protein modification in the posttranslation level has been found to participate in maintaining the proper function of CYP450, thus effect of posttranslational modification on the enzyme activity has been paid more and more attention. Posttranslational modifications including phosphorylation, nitration, and ubiquitination have been described to regulate the activity of CYP450. In this paper, recent developments in the effects of posttranslational modifications on the activity of CYP450 have been reviewed.