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用于银屑病治疗的新型芳烃受体调节剂的计算发现。

Computational discovery of novel aryl hydrocarbon receptor modulators for psoriasis therapy.

作者信息

Santini Gianluca, Bonati Laura, Motta Stefano

机构信息

Department of Earth and Environmental Sciences, University of Milano-Bicocca, Milan, 20126, Italy.

Inter-University Center for the Promotion of the 3Rs Principles in Teaching & Research (Centro 3R), Pisa, 56122, Italy.

出版信息

Sci Rep. 2025 Jun 6;15(1):19963. doi: 10.1038/s41598-025-03626-z.

DOI:10.1038/s41598-025-03626-z
PMID:40481006
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12144160/
Abstract

The aryl hydrocarbon receptor (AhR) is a ligand-dependent transcription factor involved in the regulation of many pathophysiological processes. Among these, immune system modulation, as well as regulation of skin homeostasis and inflammation, make it a promising target for psoriasis therapy. Tapinarof, an AhR agonist recently approved for psoriasis treatment, exerts its action through antioxidant, anti-inflammatory and barrier-restoring effects. In this study, we employed a computational drug-discovery approach to identify novel AhR modulators with psoriasis therapeutic potential. We performed a multi-step similarity-based screening in PubChem. Molecular docking led to the identification of diverse chemical scaffolds with high docking scores and potential AhR activity, some belonging to chemical classes with known pharmacological relevance. The stability of the binding geometries of the most promising compounds of each family was then verified through molecular dynamics simulations and pharmacokinetic characteristics were predicted using ADMETlab 2.0 and SwissADME. Notably, several identified compounds suggest a possible interplay between AhR signaling and sirtuin modulation, highlighting a previously unexplored avenue in psoriasis therapy. Our findings underscore the potential of computational approaches in accelerating the discovery of novel AhR-targeting agents and provide a foundation for further experimental validation.

摘要

芳基烃受体(AhR)是一种依赖配体的转录因子,参与多种病理生理过程的调节。其中,免疫系统调节以及皮肤稳态和炎症的调节,使其成为银屑病治疗的一个有前景的靶点。替帕罗夫是一种最近被批准用于治疗银屑病的AhR激动剂,它通过抗氧化、抗炎和恢复屏障功能发挥作用。在本研究中,我们采用了一种计算机辅助药物发现方法来识别具有银屑病治疗潜力的新型AhR调节剂。我们在PubChem中进行了多步基于相似性的筛选。分子对接导致鉴定出具有高对接分数和潜在AhR活性的多种化学支架,其中一些属于具有已知药理学相关性的化学类别。然后通过分子动力学模拟验证了每个家族中最有前景的化合物的结合几何结构的稳定性,并使用ADMETlab 2.0和SwissADME预测了药代动力学特征。值得注意的是,几种鉴定出的化合物表明AhR信号传导与沉默调节蛋白调节之间可能存在相互作用,突出了银屑病治疗中一条以前未被探索的途径。我们的研究结果强调了计算机方法在加速新型AhR靶向药物发现方面的潜力,并为进一步的实验验证提供了基础。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1eda/12144160/5ee2e62a4db1/41598_2025_3626_Fig6_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1eda/12144160/ecaf1a17826b/41598_2025_3626_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1eda/12144160/580f459cb6e6/41598_2025_3626_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1eda/12144160/822bda39e865/41598_2025_3626_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1eda/12144160/d9e4a4c065a5/41598_2025_3626_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1eda/12144160/6eaca99935cb/41598_2025_3626_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1eda/12144160/5ee2e62a4db1/41598_2025_3626_Fig6_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1eda/12144160/ecaf1a17826b/41598_2025_3626_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1eda/12144160/580f459cb6e6/41598_2025_3626_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1eda/12144160/822bda39e865/41598_2025_3626_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1eda/12144160/d9e4a4c065a5/41598_2025_3626_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1eda/12144160/6eaca99935cb/41598_2025_3626_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1eda/12144160/5ee2e62a4db1/41598_2025_3626_Fig6_HTML.jpg

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本文引用的文献

1
Structural basis for the ligand-dependent activation of heterodimeric AHR-ARNT complex.异二聚体芳烃受体-芳香烃受体核转运蛋白复合物配体依赖性激活的结构基础。
Nat Commun. 2025 Feb 3;16(1):1282. doi: 10.1038/s41467-025-56574-7.
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PubChem 2025 update.PubChem 2025更新版。
Nucleic Acids Res. 2025 Jan 6;53(D1):D1516-D1525. doi: 10.1093/nar/gkae1059.
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Structural Insights into the Activation of Human Aryl Hydrocarbon Receptor by the Environmental Contaminant Benzo[a]pyrene and Structurally Related Compounds.环境污染物苯并[a]芘及结构相关化合物对人芳烃受体激活作用的结构见解
J Mol Biol. 2024 Feb 1;436(3):168411. doi: 10.1016/j.jmb.2023.168411. Epub 2023 Dec 20.
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The AhR Signaling Mechanism: A Structural Point of View.芳烃受体信号传导机制:结构视角
J Mol Biol. 2024 Feb 1;436(3):168296. doi: 10.1016/j.jmb.2023.168296. Epub 2023 Oct 4.
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TCDD-Induced Allosteric Perturbation of the AhR:ARNT Binding to DNA.TCDD 诱导的 AhR:ARNT 与 DNA 的变构结合扰动。
Int J Mol Sci. 2023 May 26;24(11):9339. doi: 10.3390/ijms24119339.
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Natural Coumarin Derivatives Activating Nrf2 Signaling Pathway as Lead Compounds for the Design and Synthesis of Intestinal Anti-Inflammatory Drugs.天然香豆素衍生物激活Nrf2信号通路作为肠道抗炎药物设计与合成的先导化合物
Pharmaceuticals (Basel). 2023 Mar 30;16(4):511. doi: 10.3390/ph16040511.
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Cryo-EM structure of the cytosolic AhR complex.胞质芳烃受体复合物的冷冻电镜结构
Structure. 2023 Mar 2;31(3):295-308.e4. doi: 10.1016/j.str.2022.12.013. Epub 2023 Jan 16.
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Aryl hydrocarbon receptor: The master regulator of immune responses in allergic diseases.芳烃受体:变应性疾病中免疫反应的主要调节因子。
Front Immunol. 2022 Dec 19;13:1057555. doi: 10.3389/fimmu.2022.1057555. eCollection 2022.
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Functions of the aryl hydrocarbon receptor (AHR) beyond the canonical AHR/ARNT signaling pathway.芳香烃受体 (AHR) 除了经典的 AHR/ARNT 信号通路之外的功能。
Biochem Pharmacol. 2023 Feb;208:115371. doi: 10.1016/j.bcp.2022.115371. Epub 2022 Dec 15.
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Cryo-EM structure of the agonist-bound Hsp90-XAP2-AHR cytosolic complex.激动剂结合的 HSP90-XAP2-AHR 胞质复合物的冷冻电镜结构。
Nat Commun. 2022 Nov 16;13(1):7010. doi: 10.1038/s41467-022-34773-w.