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通过药代动力学、毒性、分子对接和分子动力学模拟对一种新型癌症EGFR和VEGFR-2激酶抑制剂(药物)进行计算机再利用研究。

In Silico Repurposing of a Novel Inhibitor (drug) of EGFR and VEGFR-2 Kinases of Cancer by Pharmacokinetics, Toxicity, Molecular Docking, and Molecular Dynamics Simulation.

作者信息

Ibraheim Mona H, Maher Ibrahim, Khater Ibrahim

机构信息

Physics Department, Faculty of Science, Zagazig University, P.O.44519, Zagazig, Egypt.

Biophysics Department, Faculty of Science, Cairo University, Giza, Egypt.

出版信息

Appl Biochem Biotechnol. 2024 Nov;196(11):8332-8365. doi: 10.1007/s12010-024-04958-8. Epub 2024 May 24.

Abstract

Vascular endothelial growth factor is an angiogenic that promotes the development and metastasis of tumors (VEGF). The epidermal growth factor receptor, or EGFR, controls the division, growth, and death of cells via several signaling pathways. It has been found that most of the tyrosine kinase EGFR/VEGFR-2 inhibited by drugs that the FDA has approved are so far. The main objective of the present study was to identify an efficacious and selective dual inhibitor of VEGFR-2/EGFR for the treatment of cancer. Out of the 400 ligands tested against the kinases, 12 compounds demonstrated the best docking scores through molecular docking for the two kinases. Of these, only compound SCHEMBL2435814 inhibited the kinases with the highest score values when compared to a reference, vandetanib, as a dual inhibitor of EGFR/VEGFR-2 kinases through interaction with the identified active sites pocket. Following drug-likeness score toxicity and pharmacokinetic testing, the two compounds, SCHEMBL2435814 and vandetanib, were analyzed to determine how the two kinases interacted with each other. The results of calculations of π-cation interactions, hydrogen bonds, and hydrophobic interactions demonstrated a strong interaction between the two kinases and SCHEMBL2435814. Eventually, molecular dynamic modeling was used to assess the stability of complexes. This demonstrated many characteristics, including RMSF, RMSD, SASA, RG, and H-bond analysis, which demonstrated that SCHEMBL2435814 with the two kinases was more stable than vandetanib over a 100ns simulation period. By suppressing EGFR/VEGFR-2, chemical SCHEMBL2435814 may be able to postpone the signaling pathway of proteins that are essential to the advancement of cancer.

摘要

血管内皮生长因子是一种促进肿瘤发展和转移的血管生成因子(VEGF)。表皮生长因子受体(EGFR)通过多种信号通路控制细胞的分裂、生长和死亡。据发现,美国食品药品监督管理局(FDA)迄今批准的药物所抑制的大多数酪氨酸激酶EGFR/VEGFR-2。本研究的主要目的是鉴定一种用于治疗癌症的有效且选择性的VEGFR-2/EGFR双重抑制剂。在针对这些激酶测试的400种配体中,有12种化合物通过分子对接对这两种激酶表现出最佳对接分数。其中,与作为EGFR/VEGFR-2激酶双重抑制剂的参考药物凡德他尼相比,只有化合物SCHEMBL2435814通过与确定的活性位点口袋相互作用以最高分数值抑制了这些激酶。在进行类药性质评分、毒性和药代动力学测试后,对两种化合物SCHEMBL2435814和凡德他尼进行了分析,以确定这两种激酶如何相互作用。π-阳离子相互作用、氢键和疏水相互作用的计算结果表明,这两种激酶与SCHEMBL2435814之间存在强烈相互作用。最终,使用分子动力学建模来评估复合物的稳定性。这显示出许多特征,包括均方根波动(RMSF)、均方根偏差(RMSD)、溶剂可及表面积(SASA)、回转半径(RG)和氢键分析,这些结果表明在100纳秒的模拟期内,SCHEMBL2435814与这两种激酶形成的复合物比凡德他尼更稳定。通过抑制EGFR/VEGFR-2,化学物质SCHEMBL2435814可能能够延缓对癌症进展至关重要的蛋白质的信号通路。

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