Butcher Neville J, Arulpragasam Ajanthy, Pope Catherine, Minchin Rodney F
Centre for Medical Research, University of Western Australia, Nedlands, Western Australia, Australia.
Biochem J. 2003 Dec 1;376(Pt 2):441-8. doi: 10.1042/BJ20030650.
Human N -acetyltransferase Type I (NAT1) catalyses the acetylation of many aromatic amine and hydrazine compounds and it has been implicated in the catabolism of folic acid. The enzyme is widely expressed in the body, although there are considerable differences in the level of activity between tissues. A search of the mRNA databases revealed the presence of several NAT1 transcripts in human tissue that appear to be derived from different promoters. Because little is known about NAT1 gene regulation, the present study was undertaken to characterize one of the putative promoter sequences of the NAT1 gene located just upstream of the coding region. We show with reverse-transcriptase PCR that mRNA transcribed from this promoter (Promoter I) is present in a variety of human cell-lines, but not in quiescent peripheral blood mononuclear cells. Using deletion mutant constructs, we identified a 20 bp sequence located 245 bases upstream of the translation start site which was sufficient for basal NAT1 expression. It comprised an AP-1 (activator protein 1)-binding site, flanked on either side by a TCATT motif. Mutational analysis showed that the AP-1 site and the 3' TCATT sequence were necessary for gene expression, whereas the 5' TCATT appeared to attenuate promoter activity. Electromobility shift assays revealed two specific bands made up by complexes of c-Fos/Fra, c-Jun, YY-1 (Yin and Yang 1) and possibly Oct-1. PMA treatment enhanced expression from the NAT1 promoter via the AP-1-binding site. Furthermore, in peripheral blood mononuclear cells, PMA increased endogenous NAT1 activity and induced mRNA expression from Promoter I, suggesting that it is functional in vivo.
人I型N - 乙酰基转移酶(NAT1)催化多种芳香胺和肼类化合物的乙酰化反应,并且参与叶酸的分解代谢。该酶在体内广泛表达,尽管不同组织之间的活性水平存在显著差异。对mRNA数据库的搜索显示,人体组织中存在几种NAT1转录本,它们似乎来自不同的启动子。由于对NAT1基因调控了解甚少,本研究旨在对位于编码区上游的NAT1基因的一个推定启动子序列进行表征。我们通过逆转录PCR表明,从该启动子(启动子I)转录的mRNA存在于多种人类细胞系中,但不存在于静止的外周血单核细胞中。使用缺失突变体构建体,我们确定了位于翻译起始位点上游245个碱基处的一个20 bp序列,该序列足以实现NAT1的基础表达。它包含一个AP-1(激活蛋白1)结合位点,两侧各有一个TCATT基序。突变分析表明,AP-1位点和3' TCATT序列对于基因表达是必需的,而5' TCATT似乎会减弱启动子活性。电泳迁移率变动分析揭示了由c-Fos/Fra、c-Jun、YY-1(阴阳1)以及可能的Oct-1复合物组成的两条特异性条带。佛波酯(PMA)处理通过AP-1结合位点增强了NAT1启动子的表达。此外,在外周血单核细胞中,PMA增加了内源性NAT1活性并诱导了启动子I的mRNA表达,表明它在体内具有功能。