Suppr超能文献

用于治疗转移性宫颈癌的潜在VEGFR2抑制剂:来自分子动力学和自由能景观研究的见解

Potential VEGFR2 inhibitors for managing metastatic cervical cancer: insights from molecular dynamics and free energy landscape studies.

作者信息

Alobaida Ahmed, Abouzied Amr S, Taslim Ahmed A, Huwaimel Bader

机构信息

Department of Pharmaceutics, College of Pharmacy, University of Ha'il, 81442, Ha'il, Saudi Arabia.

Department of Pharmaceutical Chemistry, College of Pharmacy, University of Hail, 81442, Hail, Saudi Arabia.

出版信息

Mol Divers. 2024 Dec 18. doi: 10.1007/s11030-024-11080-8.

Abstract

Metastatic cervical cancer, the advanced stage where the cancer spreads beyond the cervix to other parts of the body, poses significant treatment challenges and is associated with poor survival rates. Vascular Endothelial Growth Factor Receptor 2 (VEGFR2), a critical angiogenic mediator, is upregulated in metastatic cervical cancer, driving the formation of new blood vessels that fuel tumor growth and spread, making it an attractive target for anti-angiogenic therapies aimed at halting metastasis. This study aims to determine the anti-angiogenic effects of natural compounds to identify new VEGFR2 inhibitors for managing metastatic cervical cancer. The potential effect of these compounds as VEGFR2 inhibitors at the structural level was assessed using various methods such as virtual screening, docking, MD simulations (1000 ns), binding free energy calculations, and free energy landscape analysis. Four compounds, including IMPHY007574, IMPHY004129, IMPHY008783, and IMPHY004928, were found to be potential VEGFR2 inhibitors. Among the structures analyzed in the present work, IMPHY007574 revealed the highest binding stability with VEGFR2 and the most favorable interaction pattern, thus proving the possibility of its use as an effective anti-angiogenic compound. The other three compounds also demonstrated a reasonably good promise in VEGFR2 inhibition. These findings provide a foundation for developing novel therapeutic strategies for metastatic cervical cancer, potentially overcoming drug resistance and improving patient survival rates.

摘要

转移性宫颈癌是癌症发展到晚期,癌细胞从子宫颈扩散到身体其他部位的阶段,它带来了重大的治疗挑战,且与低生存率相关。血管内皮生长因子受体2(VEGFR2)是一种关键的血管生成介质,在转移性宫颈癌中上调,促使形成新的血管,为肿瘤生长和扩散提供养分,这使其成为旨在阻止转移的抗血管生成疗法的一个有吸引力的靶点。本研究旨在确定天然化合物的抗血管生成作用,以识别用于治疗转移性宫颈癌的新型VEGFR2抑制剂。使用虚拟筛选、对接、分子动力学模拟(1000纳秒)、结合自由能计算和自由能景观分析等各种方法,在结构水平上评估了这些化合物作为VEGFR2抑制剂的潜在效果。发现四种化合物,即IMPHY007574、IMPHY004129、IMPHY008783和IMPHY004928,是潜在的VEGFR2抑制剂。在本研究分析的结构中,IMPHY007574与VEGFR2显示出最高的结合稳定性和最有利的相互作用模式,从而证明了其作为有效抗血管生成化合物使用的可能性。其他三种化合物在抑制VEGFR2方面也显示出相当不错的前景。这些发现为开发转移性宫颈癌的新型治疗策略奠定了基础,有望克服耐药性并提高患者生存率。

文献AI研究员

20分钟写一篇综述,助力文献阅读效率提升50倍。

立即体验

用中文搜PubMed

大模型驱动的PubMed中文搜索引擎

马上搜索

文档翻译

学术文献翻译模型,支持多种主流文档格式。

立即体验