Department of Biology, University of Utah, 257 South 1400 East, Salt Lake City, UT 84112, USA.
Toxicon. 2013 Nov;74:215-24. doi: 10.1016/j.toxicon.2013.08.054. Epub 2013 Aug 29.
Cone snails, genus Conus, are predatory marine snails that use venom to capture their prey. This venom contains a diverse array of peptide toxins, known as conotoxins, which undergo a diverse set of posttranslational modifications. Amidating enzymes modify peptides and proteins containing a C-terminal glycine residue, resulting in loss of the glycine residue and amidation of the preceding residue. A significant fraction of peptides present in the venom of cone snails contain C-terminal amidated residues, which are important for optimizing biological activity. This study describes the characterization of the amidating enzyme, peptidylglycine α-amidating monooxygenase (PAM), present in the venom duct of cone snails, Conus bullatus and Conus geographus. PAM is known to carry out two functions, peptidyl α-hydroxylating monooxygenase (PHM) and peptidylamido-glycolate lyase (PAL). In some animals, such as Drosophila melanogaster, these two functions are present in separate polypeptides, working as individual enzymes. In other animals, such as mammals and in Aplysia californica, PAM activity resides in a single, bifunctional polypeptide. Using specific oligonucleotide primers and reverse transcription-polymerase chain reaction we have identified and cloned from the venom duct cDNA library, a cDNA with 49% homology to PAM from A. californica. We have determined that both the PHM and PAL activities are encoded in one mRNA polynucleotide in both C. bullatus and C. geographus. We have directly demonstrated enzymatic activity catalyzing the conversion of dansyl-YVG-COOH to dansyl-YV-NH2 in cloned cDNA expressed in Drosophila S2 cells.
圆锥蜗牛,属 Conus,是掠食性海洋蜗牛,它们使用毒液来捕获猎物。这种毒液含有多种肽毒素,称为 conotoxin,它们经历了多种翻译后修饰。酰胺化酶修饰含有 C 末端甘氨酸残基的肽和蛋白质,导致甘氨酸残基的丢失和前一个残基的酰胺化。在圆锥蜗牛毒液中存在的显著比例的肽含有 C 末端酰胺化残基,这对于优化生物活性非常重要。本研究描述了存在于圆锥蜗牛 Conus bullatus 和 Conus geographus 的毒管中的酰胺化酶,肽基甘氨酰 α-酰胺化单加氧酶(PAM)的特征。PAM 已知具有两种功能,即肽基 α-羟化单加氧酶(PHM)和肽基酰胺基-甘氨酸裂合酶(PAL)。在一些动物中,如黑腹果蝇,这两种功能存在于不同的多肽中,作为单独的酶起作用。在其他动物中,如哺乳动物和加利福尼亚海兔,PAM 活性存在于单个双功能多肽中。使用特定的寡核苷酸引物和逆转录-聚合酶链反应,我们从毒管 cDNA 文库中鉴定并克隆了一个 cDNA,其与加利福尼亚海兔的 PAM 具有 49%的同源性。我们已经确定,在 C. bullatus 和 C. geographus 中,PHM 和 PAL 两种活性都编码在一个 mRNA 多核苷酸中。我们直接证明了在克隆 cDNA 表达的果蝇 S2 细胞中催化 dansyl-YVG-COOH 转化为 dansyl-YV-NH2 的酶促活性。