Gao Meiyu, Wu Yu, Yin Huihui, Wang Qiang, Tian Yuan, Zhang Zunjian, Xu Fengguo, Zhang Pei
Department of Pharmaceutical Analysis, School of Pharmacy, China Pharmaceutical University, Nanjing, 210009, P. R. China.
Key Laboratory of Drug Quality Control and Pharmacovigilance (Ministry of Education), Nanjing, 210009, P. R. China.
Anal Bioanal Chem. 2025 Jul 5. doi: 10.1007/s00216-025-05997-8.
Phosphatidyl amino acids (p-AAs) are metabolites characterized by the phosphorylation of the hydroxyl, amino, carboxyl, and thiol groups of amino acids. Previous research has primarily focused on the phosphorylation sites within macromolecular proteins, with a particular emphasis on typical O-p-AAs. In this study, we established a prediction library of p-AAs based on existing knowledge. To improve detection rates of p-AAs in biological samples, we employed a chemical labeling-based LC-MS/MS method, utilizing p-[3,5-(dimethylamino)-2,4,6-triazine] benzene-1-sulfonyl piperazine (Tmt-PP) and its deuterated form (d12-Tmt-PP) as paired labeling reagents. A preliminary identification was performed by matching characteristic MS fragments with available standards. Additionally, strategies such as in vitro methods were implemented for further identification. The phosphatase treatment aids in identifying phosphate-modified metabolites by dephosphorylating them, while cell extract incubation helps determine if novel phosphorylated amino acids are generated in vivo. Ultimately, we identified 11 p-AAs, 6 of which are novel metabolites reported for the first time. A pseudotargeted metabolomics method covering 11 identified p-AAs was established and applied to investigate the differences between cisplatin-resistant non-small cell lung cancer (NSCLC) cells and their parental cells, as well as their derived exosomes. This approach enhances our understanding of the role of p-AAs in various health and disease conditions and contributes to the discovery of additional novel phosphatidyl metabolites.
磷脂酰氨基酸(p-AAs)是一类代谢产物,其特征在于氨基酸的羟基、氨基、羧基和硫醇基团发生磷酸化。先前的研究主要集中在大分子蛋白质中的磷酸化位点,尤其侧重于典型的O-p-AAs。在本研究中,我们基于现有知识建立了一个p-AAs预测库。为提高生物样品中p-AAs的检测率,我们采用了基于化学标记的液相色谱-串联质谱(LC-MS/MS)方法,使用对-[3,5-(二甲氨基)-2,4,6-三嗪]苯-1-磺酰哌嗪(Tmt-PP)及其氘代形式(d12-Tmt-PP)作为配对标记试剂。通过将特征性质谱碎片与现有标准进行匹配进行初步鉴定。此外,还采用了体外方法等策略进行进一步鉴定。磷酸酶处理通过使磷酸化修饰的代谢产物去磷酸化来辅助鉴定,而细胞提取物孵育有助于确定体内是否产生新的磷酸化氨基酸。最终,我们鉴定出11种p-AAs,其中6种是首次报道的新代谢产物。建立了一种覆盖11种已鉴定p-AAs的伪靶向代谢组学方法,并将其应用于研究顺铂耐药非小细胞肺癌(NSCLC)细胞与其亲本细胞及其衍生外泌体之间的差异。这种方法增强了我们对p-AAs在各种健康和疾病状况中作用的理解,并有助于发现更多新的磷脂酰代谢产物。