Institute of Biological Chemistry, Academia Sinica, Taipei, 11529, Taiwan.
Center for Infectious Disease and Cancer Research (CICAR), Kaohsiung Medical University, Kaohsiung 80708, Taiwan.
J Food Drug Anal. 2019 Apr;27(2):603-609. doi: 10.1016/j.jfda.2018.12.007. Epub 2019 Jan 8.
Glycine N-methyltransferase (GNMT) protein is highly expressed in certain tissues, such as liver, pancreas, and prostate. GNMT serves multiple roles which include a methyl group transfer enzyme and a liver tumor suppressor. Benzo(a)pyrene (BaP), a family member of polycyclic aromatic hydrocarbon (PAH), is a known environmental carcinogen found in coal tar, tobacco smoke, barbecued food and incomplete combustion of auto fuel. BaP recruits cytochrome P450 to transform itself into benzo(a)pyrene-7,8-diol-9,10-epoxide (B(a)PDE), which covalently interacts with DNA causing tumorigenesis. BaP can be detoxified through GNMT and induces GNMT translocation into the cellular nucleus. GNMT translocation is accompanied by phosphorylation, but the role of phosphorylation in GNMT remains to be explored. Using liquid chromatography coupled with tandem mass spectrometry, this study identified serine 9 of GNMT as the phosphorylation site upon BaP treatment. When serine 9 was mutated and lost the capability to be phosphorylated, the occurrence of BaP-induced GNMT nuclear translocation was dramatically decreased. Also, this mutant from of GNMT lost the ability of phosphorylation and increased cytochrome P450 1A1 (Cyp1a) expression upon BaP treatment. In addition, protein kinase C (PKC) and c-Jun NH2-terminal kinase (JNK) may be required for such phosphorylation. Further characterization of phosphorylated GNMT for its link to BaP may bring new insights into chemical detoxification.
甘氨酸 N-甲基转移酶 (GNMT) 蛋白在某些组织中高度表达,如肝脏、胰腺和前列腺。GNMT 具有多种功能,包括甲基转移酶和肝肿瘤抑制因子。苯并(a)芘 (BaP) 是多环芳烃 (PAH) 的一种成员,是一种已知的环境致癌物,存在于煤焦油、烟草烟雾、烧烤食品和汽车燃料不完全燃烧中。BaP 招募细胞色素 P450 将自身转化为苯并(a)芘-7,8-二醇-9,10-环氧化物 (B(a)PDE),与 DNA 发生共价相互作用导致肿瘤发生。BaP 可以通过 GNMT 解毒,并诱导 GNMT 向细胞核转移。GNMT 转移伴随着磷酸化,但磷酸化在 GNMT 中的作用仍有待探索。本研究使用液相色谱串联质谱法鉴定出 BaP 处理后 GNMT 的丝氨酸 9 为磷酸化位点。当丝氨酸 9 突变并失去磷酸化能力时,BaP 诱导的 GNMT 核转移发生显著减少。此外,这种突变形式的 GNMT 失去了磷酸化能力,并在 BaP 处理时增加了细胞色素 P450 1A1 (Cyp1a) 的表达。此外,蛋白激酶 C (PKC) 和 c-Jun NH2-末端激酶 (JNK) 可能是这种磷酸化所必需的。进一步研究磷酸化 GNMT 与 BaP 的关系可能为化学解毒带来新的见解。