Mackenzie P I
Department of Clinical Pharmacology, Flinders Medical Centre, Bedford Park, South Australia.
J Biol Chem. 1990 May 25;265(15):8699-703.
The cDNA encoding a member of a family of steroid UDP-glucuronosyltransferases has been cloned and sequenced. The 1871-base pair (bp) cDNA, designated UDPGTr-5, contains an open reading frame of 1590 bp flanked by 43 and 238 bp of 5'- and 3'-untranslated regions, respectively. The 530-amino acid protein encoded by the open reading frame is 93% and 84% similar in sequence to UDPGTr-3 and UDPGTr-4, which are other members of this multigene family. In common with these forms, the encoded protein contains regions characteristic of a signal peptide and a transmembrane-anchoring domain at the carboxyl terminus. Potential asparagine-linked glycosylation sites are not present in the encoded protein. Expression of UDPGTr-5 cDNA in COS cells demonstrated that the encoded enzyme has a subunit size of 50 kDa as determined by sodium dodecyl sulfate-polyacrylamide gel electrophoresis. The expressed enzyme glucuronidates testosterone and dihydrotestosterone, although its activity towards these two substrates is about 30-fold less than that of UDPGTr-3. This low activity appeared to be a bone fide property of the enzyme and was not due to lower amounts of protein synthesized or increased rates of protein degradation. Northern analysis and cDNA sequencing demonstrated that UDPGTr-5 is encoded by two mRNA species which differed in the lengths of their 3'-untranslated regions. The cDNA to the longer transcript has a 1768-bp 3'-untranslated region which contains a segment that is 80% similar to the rat identifier sequence (ID) family of repetitive DNA elements. These data indicate that UDPGTr-5 is another 17 beta-hydroxysteroid UDP-glucuronosyltransferase that is encoded by two mRNAs transcribed from a single gene.
编码类固醇UDP-葡萄糖醛酸基转移酶家族成员的cDNA已被克隆和测序。这个1871个碱基对(bp)的cDNA,命名为UDPGTr-5,包含一个1590 bp的开放阅读框,其两侧分别是43 bp和238 bp的5'-和3'-非翻译区。开放阅读框编码的530个氨基酸的蛋白质与该多基因家族的其他成员UDPGTr-3和UDPGTr-4在序列上分别有93%和84%的相似性。与这些形式一样,编码的蛋白质含有信号肽的特征区域和羧基末端的跨膜锚定结构域。编码的蛋白质中不存在潜在的天冬酰胺连接的糖基化位点。UDPGTr-5 cDNA在COS细胞中的表达表明,通过十二烷基硫酸钠-聚丙烯酰胺凝胶电泳测定,编码的酶的亚基大小为50 kDa。表达的酶能使睾酮和二氢睾酮葡萄糖醛酸化,尽管它对这两种底物的活性比UDPGTr-3低约30倍。这种低活性似乎是该酶的真实特性,并非由于合成的蛋白质数量减少或蛋白质降解速率增加所致。Northern分析和cDNA测序表明,UDPGTr-5由两种mRNA编码,它们的3'-非翻译区长度不同。较长转录本的cDNA有一个1768 bp的3'-非翻译区,其中包含一个与大鼠重复DNA元件识别序列(ID)家族80%相似的片段。这些数据表明,UDPGTr-5是另一种17β-羟基类固醇UDP-葡萄糖醛酸基转移酶,由从单个基因转录的两种mRNA编码。