印度尼西亚多种药用植物中抑制人乳头瘤病毒16型E6蛋白在宫颈癌发展中的活性物质的虚拟筛选、分子对接和分子动力学模拟

IF 1.1 Q3 BIOLOGY
Tropical life sciences research Pub Date : 2025-03-01 Epub Date: 2025-03-30 DOI:10.21315/tlsr2025.36.1.1
Arief Hidayatullah, Diana Widiastuti, Wira Eka Putra, Muhaimin Rifa'i, Muhammad Fikri Heikal, Sustiprijatno
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引用次数: 0

摘要

角化细胞感染高危人乳头瘤病毒(HPV)毒株,特别是HPV16,是宫颈癌发病的原因。E6蛋白是与癌症进展有关的关键癌蛋白。我们利用虚拟筛选方法鉴定了印度尼西亚多种常用药用植物中的生物活性化合物。所有前5个化合物都与E6主疏水槽上的单个结合位点结合,该结合位点与E6AP和IRF3的LxxLL基序的结合位点相对应。它们有望作为竞争性抑制剂发挥作用,抑制E6-E6AP和E6-IRF3复合物的发展,从而限制p53的降解和细胞增殖,从而保持对HPV16感染的先天免疫反应。Asarinin和噻唑[3,2-a]苯并咪唑-3(2H)- 1,2 -(2- fluoroboblideno)-7,8-二甲基被预测为本研究中最有效的化合物,因为它们对E6主要疏水沟槽具有很强的亲和力并与之持续相互作用,特别是与药理学对照相比。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Virtual Screening, Molecular Docking and Molecular Dynamics Simulation of Bioactive Compounds from Various Indonesian Medicinal Plants as Potential Inhibitors of Human Papillomavirus Type 16 E6 Protein in Cervical Cancer Development.

Infection of keratinocytes by high-risk human papillomavirus (HPV) strains, notably HPV16, is responsible for the onset of cervical cancer. The E6 protein serves as a pivotal oncoprotein implicated in the progression of cancer. We utilised a virtual screening method to identify bioactive compounds in a variety of commonly used medicinal plants in Indonesia. All the top five compounds bind to a single binding site on the E6 major hydrophobic groove, which corresponds to the binding site for the E6AP and IRF3's LxxLL motifs. They are expected to function as competitive inhibitors, inhibiting the development of the E6-E6AP and E6-IRF3 complexes, which limit p53 degradation and therefore cell proliferation, thus preserving the innate immune response to HPV16 infection. Asarinin and thiazolo[3,2-a]benzimidazole-3(2H)-one,2-(2-fluorobenzylideno)-7,8-dimethyl were predicted to be the most effective compounds in this research owing to their strong affinity for and persistent interactions with the E6 major hydrophobic groove, particularly in comparison to pharmacological controls.

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来源期刊
CiteScore
2.60
自引率
0.00%
发文量
40
审稿时长
20 weeks
期刊介绍: Tropical Life Sciences Research (TLSR) formerly known as Journal of Bioscience seeks to publish relevant ideas and knowledge addressing vital life sciences issues in the tropical region. The Journal’s scope is interdisciplinary in nature and covers any aspects related to issues on life sciences especially from the field of biochemistry, microbiology, biotechnology and animal, plant, environmental, biomedical and pharmaceutical sciences. TLSR practices double blind peer review system to ensure and maintain the good quality of articles published in this journal. Two issues are published annually in printed and electronic form. TLSR also accepts review articles, experimental papers and short communications. The Chief Editor would like to invite researchers to use this journal as a mean to rapidly promote their research findings.
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