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血管内皮生长因子受体(VEGFR)抑制剂的进展:新型抗癌药物综述

Advances in VEGFR Inhibitors: A Comprehensive Review of Novel Anticancer Agents.

作者信息

Jha Sumeet, Gupta Sneha, Rani Supriya, Arora Pinky, Choudhary Neeraj, Kumar Shubham

机构信息

Department of Pharmaceutical Chemistry, School of Pharmaceutical Sciences, Lovely Professional University, Jalandhar-Delhi G.T. Road, Phagwara, Punjab, 144411, India.

Department of Biochemistry, School of Bioengineering and Biosciences, Lovely Professional University, Jalandhar-Delhi G.T. Road, Phagwara, Punjab, 144411, India.

出版信息

Anticancer Agents Med Chem. 2025;25(10):663-687. doi: 10.2174/0118715206356712241202112641.

Abstract

Cancer, characterized by aberrant cell growth, presents a formidable health challenge, impacting millions of individuals worldwide each year. Among the myriad mechanisms facilitating tumor progression, Vascular Endothelial Growth Factor receptors (VEGFR) play a pivotal role in driving angiogenesis the process by which tumors develop their own blood supply. This vascularization not only supports tumor nourishment and growth but also facilitates metastasis, enabling cancer to spread to distant sites. VEGFR inhibitors offer a strategic approach to disrupt the VEGF-VEGFR binding pathway, thereby impeding angiogenesis, metastasis, and the proliferation of cancer cells. This review elucidates the latest advancements in medicinal chemistry pertaining to VEGFR inhibitors, showcasing a variety of chemical moieties and assessing their efficacy across different cancer cell lines. The novel compounds highlighted in this review exhibit significant promise for anticancer evaluation through targeted VEGFR kinase inhibition. A robust body of , and studies supports these findings, demonstrating the antitumor effects of these compounds. Computational analyses further enhance our understanding by predicting compound binding affinities, pharmacokinetics, and overall drug-likeness. Despite the significant progress made in developing effective VEGFR inhibitors, challenges remain in refining these agents for optimal cancer treatment. This review not only summarizes the advancements achieved in VEGFR inhibitor development but also emphasizes the ongoing hurdles that must be addressed to enhance the efficacy of cancer therapies.

摘要

癌症以异常细胞生长为特征,是一项严峻的健康挑战,每年影响全球数百万人。在促进肿瘤进展的众多机制中,血管内皮生长因子受体(VEGFR)在驱动血管生成过程中起着关键作用,血管生成是肿瘤形成自身血液供应的过程。这种血管化不仅支持肿瘤的营养供应和生长,还促进转移,使癌症能够扩散到远处。VEGFR抑制剂提供了一种策略性方法来破坏VEGF-VEGFR结合途径,从而阻碍血管生成、转移和癌细胞的增殖。本综述阐述了与VEGFR抑制剂相关的药物化学最新进展,展示了各种化学基团,并评估了它们在不同癌细胞系中的疗效。本综述中强调的新型化合物通过靶向VEGFR激酶抑制在抗癌评估方面显示出巨大前景。大量的 、 和 研究支持这些发现,证明了这些化合物的抗肿瘤作用。计算分析通过预测化合物的结合亲和力、药代动力学和整体药物相似性进一步加深了我们的理解。尽管在开发有效的VEGFR抑制剂方面取得了重大进展,但在优化这些药物以实现最佳癌症治疗方面仍存在挑战。本综述不仅总结了VEGFR抑制剂开发中取得的进展,还强调了为提高癌症治疗效果必须解决的持续障碍。

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