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维生素D受体单核苷酸多态性与维生素D类似物的分子见解:白癜风的一种新治疗途径。

Molecular insights of vitamin D receptor SNPs and vitamin D analogs: a novel therapeutic avenue for vitiligo.

作者信息

Sundaravel Sakthi Sasikala, Kuriakose Beena Briget, Alhazmi Amani Hamad, Jeyaraman Sabareeswari, Jagannathan Sushma Shruthi, Muthusamy Karthikeyan

机构信息

Pharmacogenomics and CADD Lab, Department of Bioinformatics, Alagappa University, Tamil Nadu, Karaikudi, India.

Department of Basic Medical Sciences, College of Applied Medical Sciences, King Khalid University, Khamis Mushayt, Saudi Arabia.

出版信息

Mol Divers. 2025 Mar 21. doi: 10.1007/s11030-025-11168-9.

Abstract

Vitamin D receptor (VDR) agonists play a pivotal role in modulating immune responses and promoting melanocyte survival, making them potential candidates for vitiligo treatment. The VDR gene is integral to mediating the effects of vitamin D in the immune system, and disruptions in its structure due to missense mutations may significantly contribute to the pathogenesis of vitiligo. Missense single-nucleotide polymorphisms (SNPs) can alter the amino acid sequence of the VDR protein, potentially affecting its ligand-binding affinity and downstream signaling. Investigating these missense SNPs provides critical insights into the genetic underpinnings of vitiligo and may help identify biomarkers for early detection and precision-targeted therapies. This study explored the therapeutic potential of vitamin D analogs in vitiligo management, with a particular focus on their binding interactions and molecular efficacy. Using molecular docking and virtual screening, 24 vitamin D analogs were evaluated. Calcipotriol exhibited the highest binding affinity (-11.4 kcal/mol) and unique interactions with key residues in the VDR ligand-binding domain. Additionally, an analysis of structural variations stemming from missense mutations in the VDR gene highlighted potential impacts on receptor-ligand interactions, further emphasizing the importance of genetic factors in treatment response. These findings underscore the potential of calcipotriol to promote melanogenesis and modulate pigmentation in vitiligo. A comparative analysis identified structural variations influencing the efficacy of other analogs, such as calcitriol and tacalcitol. Although the in silico methods provided valuable insights, the study acknowledges the limitations of excluding dynamic cellular environments and emphasizes the need for experimental validation. Overall, this study enhances our understanding of VDR-targeted therapies, and calcipotriol is a promising candidate for further development in the management of vitiligo.

摘要

维生素D受体(VDR)激动剂在调节免疫反应和促进黑素细胞存活方面发挥着关键作用,使其成为白癜风治疗的潜在候选药物。VDR基因对于介导维生素D在免疫系统中的作用不可或缺,由于错义突变导致其结构破坏可能显著促成白癜风的发病机制。错义单核苷酸多态性(SNP)可改变VDR蛋白的氨基酸序列,可能影响其配体结合亲和力和下游信号传导。研究这些错义SNP可为白癜风的遗传基础提供关键见解,并可能有助于识别早期检测和精准靶向治疗的生物标志物。本研究探讨了维生素D类似物在白癜风治疗中的潜在作用,特别关注它们的结合相互作用和分子疗效。通过分子对接和虚拟筛选,对24种维生素D类似物进行了评估。卡泊三醇表现出最高的结合亲和力(-11.4千卡/摩尔),并与VDR配体结合域中的关键残基有独特的相互作用。此外,对VDR基因错义突变引起的结构变异分析突出了对受体-配体相互作用的潜在影响,进一步强调了遗传因素在治疗反应中的重要性。这些发现强调了卡泊三醇在白癜风中促进黑素生成和调节色素沉着的潜力。一项比较分析确定了影响其他类似物(如骨化三醇和他卡西醇)疗效的结构变异。尽管计算机模拟方法提供了有价值的见解,但该研究承认排除动态细胞环境的局限性,并强调了实验验证的必要性。总体而言,本研究增进了我们对VDR靶向治疗的理解,卡泊三醇是白癜风管理中进一步开发的有前景的候选药物。

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