将网络药理学与分子对接和动力学相结合,揭示维生素D3在帕金森病中的治疗靶点和信号机制。

IF 3.9 2区 化学 Q2 CHEMISTRY, APPLIED Molecular Diversity Pub Date : 2025-01-17 DOI:10.1007/s11030-024-11090-6
Cheng Wang, Yi-Ling Wang, Qiu-Han Xu
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引用次数: 0

摘要

帕金森病(PD)是一种以黑质多巴胺能神经元变性为特征的慢性神经退行性疾病。越来越多的证据表明维生素D3 (VD)在PD中起治疗作用,但其确切的分子机制尚不清楚。本研究采用网络药理学和生物信息学方法鉴定VD的中枢靶点和相关通路。我们确定了24个VD的抗pd靶点,其中雌激素受体1、雌激素受体2 (ESR2)、钠依赖性去甲肾上腺素转运蛋白和胰岛素样生长因子1受体是中心靶点。基因富集分析表明,VD的抗pd机制与雌激素信号通路密切相关。此外,双样本孟德尔随机化表明25-羟基维生素D和体内雌激素水平之间存在正因果关系。为了验证VD与枢纽药物靶点之间的相互作用,我们进行了分子对接和动力学模拟,发现VD与ESR2之间的相互作用最强。药物靶点的进一步孟德尔随机化分析证实了ESR2药物靶点对PD风险的显著影响。多巴胺能神经元单细胞核测序结合GSEA分析表明,ESR2激活可上调神经活性配体-受体相互作用信号通路,下调帕金森病通路,从而发挥神经保护作用。综上所述,我们的研究结果表明,补充VD不仅可以提高人类雌二醇水平,还可以直接激活ESR2,从而调节PD患者的雌激素信号通路,提供神经保护。这些预测性生物学靶点为未来帕金森病的临床应用提供了有希望的途径。
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Integrating network pharmacology with molecular docking and dynamics to uncover therapeutic targets and signaling mechanisms of vitamin D3 in Parkinson's disease.

Parkinson's disease (PD) is a chronic neurodegenerative disorder marked by dopaminergic neuron degeneration in the substantia nigra. Emerging evidence suggests vitamin D3 (VD) plays a therapeutic role in PD, but its precise molecular mechanisms remain unclear. This study employed network pharmacology and bioinformatics to identify VD's hub targets and related pathways. We identified 24 VD's anti-PD targets, with estrogen receptor 1, estrogen receptor 2 (ESR2), sodium-dependent norepinephrine transporter, and insulin-like growth factor 1 receptor emerging as hub targets. Gene enrichment analysis elucidated that VD's anti-PD mechanism is closely related to the estrogen signaling pathway. Additionally, two-sample Mendelian randomization suggested a positive causal relationship between 25-hydroxyvitamin D and estrogen levels in vivo. To verify the interaction between VD and the hub drug targets, we performed molecular docking and kinetic simulations, finding the strongest interaction between VD and ESR2. Further Mendelian randomization analysis of drug targets confirmed the significant effect of the ESR2 drug target on PD risk. Single-cell nuclear sequencing of dopaminergic neurons, coupled with GSEA analysis, indicated that ESR2 activation upregulates the neuroactive ligand-receptor interaction signaling pathway and downregulates the Parkinson's disease pathway, thereby exerting a neuroprotective effect. In summary, our findings suggest that VD supplementation can not only elevate estradiol levels in humans but also directly activate ESR2, thereby modulating the estrogen signaling pathway in PD patients and providing neuroprotection. These predictive biological targets offer promising avenues for future clinical applications in Parkinson's disease treatment.

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来源期刊
Molecular Diversity
Molecular Diversity 化学-化学综合
CiteScore
7.30
自引率
7.90%
发文量
219
审稿时长
2.7 months
期刊介绍: Molecular Diversity is a new publication forum for the rapid publication of refereed papers dedicated to describing the development, application and theory of molecular diversity and combinatorial chemistry in basic and applied research and drug discovery. The journal publishes both short and full papers, perspectives, news and reviews dealing with all aspects of the generation of molecular diversity, application of diversity for screening against alternative targets of all types (biological, biophysical, technological), analysis of results obtained and their application in various scientific disciplines/approaches including: combinatorial chemistry and parallel synthesis; small molecule libraries; microwave synthesis; flow synthesis; fluorous synthesis; diversity oriented synthesis (DOS); nanoreactors; click chemistry; multiplex technologies; fragment- and ligand-based design; structure/function/SAR; computational chemistry and molecular design; chemoinformatics; screening techniques and screening interfaces; analytical and purification methods; robotics, automation and miniaturization; targeted libraries; display libraries; peptides and peptoids; proteins; oligonucleotides; carbohydrates; natural diversity; new methods of library formulation and deconvolution; directed evolution, origin of life and recombination; search techniques, landscapes, random chemistry and more;
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