Jia Tianqi, Liu Wenbin, Keller Arturo A, Gao Lirong, Xu Xiaotian, Wu Wenqi, Wang Xiaoxia, Yu Yang, Zhao Guang, Li Baohui, Deng Jinglin, Mao Tianao, Chen Chunci
Research Center for Eco-Environmental Sciences, Chinese Academy of Sciences, Beijing 100085, China; College of Resources and Environment, University of Chinese Academy of Sciences, Beijing 101408, China; Bren School of Environmental Science and Management, University of California, Santa Barbara, CA 93106, USA.
College of Resources and Environment, University of Chinese Academy of Sciences, Beijing 101408, China; Hangzhou Institute for Advanced Study, University of Chinese Academy of Sciences, Hangzhou 310024, China..
Sci Total Environ. 2024 Dec 20;957:177835. doi: 10.1016/j.scitotenv.2024.177835. Epub 2024 Dec 3.
Organophosphate esters (OPEs) are widely used as flame retardants and plasticizers in daily commodities and building materials. Some OPEs, acting as agonists of the thyroid-stimulating hormone receptor (TSHR), may contribute to the development of thyroid eye disease (TED). This study analyzes the serum and urine of patients and control groups, using machine learning and molecular docking to investigate the potential impact of OPEs on TED. Results indicate significantly higher concentrations of OPEs and di-OPEs of TED patients compared to controls (Mann-Whitney U test, p < 0.05). Aryl OPEs exhibit the strongest binding affinity with TSHR. We developed a predictive model for OPE-TSHR affinity to explore the impact of OPE structural features on TSHR activity and effectively capture the complex relationships between changes in OPE side chains and their effects on TSHR. Predictions from the USEPA's database indicate that 28 % of 1011 OPEs have a tendency to bind with TSHR. Furthermore, a high-accuracy classification model successfully identified key substructures associated with high affinity for TSHR. This study not only enhances our understanding of the complex relationship between the structural diversity of OPEs and their thyroid impact but also offers molecular design insights to prevent releasing OPEs with high thyroid harm potential into the environment.
有机磷酸酯(OPEs)作为阻燃剂和增塑剂广泛应用于日常用品和建筑材料中。一些OPEs作为促甲状腺激素受体(TSHR)的激动剂,可能会导致甲状腺眼病(TED)的发展。本研究分析了患者组和对照组的血清和尿液,运用机器学习和分子对接技术来探究OPEs对TED的潜在影响。结果表明,与对照组相比,TED患者的OPEs和二-OPEs浓度显著更高(曼-惠特尼U检验,p < 0.05)。芳基OPEs与TSHR表现出最强的结合亲和力。我们建立了一个OPE-TSHR亲和力预测模型,以探索OPE结构特征对TSHR活性的影响,并有效捕捉OPE侧链变化与其对TSHR影响之间的复杂关系。美国环境保护局数据库的预测表明,1011种OPEs中有28%倾向于与TSHR结合。此外,一个高精度分类模型成功识别出了与TSHR高亲和力相关的关键亚结构。本研究不仅加深了我们对OPEs结构多样性与其甲状腺影响之间复杂关系的理解,还为防止将具有高甲状腺危害潜力的OPEs释放到环境中提供了分子设计方面的见解。