Perkins S N, Eipper B A, Mains R E
Department of Neuroscience, Johns Hopkins University School of Medicine, Baltimore, Maryland 21205.
Mol Endocrinol. 1990 Jan;4(1):132-9. doi: 10.1210/mend-4-1-132.
Peptidylglycine alpha-amidating monooxygenase (PAM; EC 1.14.17.3) catalyzes the production of alpha-amidated peptides from their glycine-extended precursors, a posttranslational modification often required for full biological activity. We have previously cloned cDNAs encoding a 108-kDa bovine PAM precursor. To confirm that this cDNA encodes a functional alpha-amidating enzyme and to begin to examine the structural requirements for the biosynthesis of an active PAM enzyme, we constructed expression vectors that placed the cDNA for either the full-sized enzyme or a form truncated at the carboxyl-terminal (and thus lacking the transmembrane domain) under the control of the mouse metallothionein-1 promoter. We used the resultant plasmids to transfect AtT-20 mouse anterior pituitary corticotrope cells and selected stable lines that expressed increased levels of PAM activity. Transfected cells in which expression from the metallothionein promoter had been induced had up to 15-fold higher levels of PAM mRNA and up to 7.5-fold higher levels of PAM activity than wild-type cells. The PAM activity in the transfected cells shared many enzymatic characteristics with PAM-B, a 38-kDa soluble form of PAM purified from bovine neurointermediate pituitary. These included copper- and ascorbate-dependent activity, an alkaline pH optimum for the peptide substrate D-Tyr-Val-Gly, similar affinities for several other synthetic substrates, and comparable apparent size during gel filtration. Compared to extracts of wild-type cells, extracts from transfected cells showed increased production of five different amino acid alpha-amides. These data indicate that a single enzyme can act on a variety of peptide substrates, and that the full structure of the PAM precursor is not necessary during biosynthesis for expression of active PAM enzyme.
肽基甘氨酸α-酰胺化单加氧酶(PAM;EC 1.14.17.3)催化从其甘氨酸延伸前体产生α-酰胺化肽,这是一种通常对充分生物活性而言必需的翻译后修饰。我们先前已克隆了编码108 kDa牛PAM前体的cDNA。为了证实该cDNA编码一种功能性α-酰胺化酶,并开始研究活性PAM酶生物合成的结构要求,我们构建了表达载体,将全长酶或羧基末端截短(因此缺乏跨膜结构域)形式的cDNA置于小鼠金属硫蛋白-1启动子的控制之下。我们使用所得质粒转染AtT-20小鼠垂体前叶促肾上腺皮质激素细胞,并筛选出表达PAM活性水平升高的稳定细胞系。与野生型细胞相比,诱导金属硫蛋白启动子表达的转染细胞中PAM mRNA水平高达15倍,PAM活性水平高达7.5倍。转染细胞中的PAM活性与从牛神经垂体中间叶纯化的38 kDa可溶性PAM形式PAM-B具有许多酶学特征。这些特征包括铜和抗坏血酸依赖性活性、对肽底物D-Tyr-Val-Gly的最适碱性pH、对其他几种合成底物的相似亲和力以及凝胶过滤过程中可比的表观大小。与野生型细胞提取物相比,转染细胞提取物显示出五种不同氨基酸α-酰胺的产量增加。这些数据表明,单一酶可作用于多种肽底物,并且在生物合成过程中,活性PAM酶的表达不需要PAM前体的完整结构。