VEGFR抑制剂研究进展:新型抗癌药物综述

IF 2.6 4区 医学 Q3 CHEMISTRY, MEDICINAL
Sumeet Jha, Sneha Gupta, Supriya Rani, Pinky Arora, Neeraj Choudhary, Shubham Kumar
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引用次数: 0

摘要

癌症以细胞生长异常为特征,是一项巨大的健康挑战,每年影响着全世界数百万人。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(肿瘤发展自身血液供应的过程)中起着关键作用。这种血管化不仅支持肿瘤的营养和生长,而且促进转移,使癌症扩散到远处的部位。VEGFR抑制剂提供了一种战略性的方法来破坏VEGF-VEGFR结合途径,从而阻碍血管生成、转移和癌细胞的增殖。本文综述了与VEGFR抑制剂有关的药物化学的最新进展,展示了多种化学成分,并评估了它们在不同癌细胞系中的疗效。本综述中强调的新化合物通过靶向VEGFR激酶抑制显示出抗癌评价的重大前景。大量的体内、体外和离体研究支持了这些发现,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增强了我们的理解。尽管在开发有效的VEGFR抑制剂方面取得了重大进展,但在改进这些药物以获得最佳癌症治疗方面仍然存在挑战。这篇综述不仅总结了VEGFR抑制剂开发取得的进展,而且强调了必须解决的持续障碍,以提高癌症治疗的疗效。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Advances in VEGFR Inhibitors: A Comprehensive Review of Novel Anticancer Agents.

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 in vivo, in vitro, and ex vivo 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.

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来源期刊
Anti-cancer agents in medicinal chemistry
Anti-cancer agents in medicinal chemistry ONCOLOGY-CHEMISTRY, MEDICINAL
CiteScore
5.10
自引率
3.60%
发文量
323
审稿时长
4-8 weeks
期刊介绍: Formerly: Current Medicinal Chemistry - Anti-Cancer Agents. Anti-Cancer Agents in Medicinal Chemistry aims to cover all the latest and outstanding developments in medicinal chemistry and rational drug design for the discovery of anti-cancer agents. Each issue contains a series of timely in-depth reviews and guest edited issues written by leaders in the field covering a range of current topics in cancer medicinal chemistry. The journal only considers high quality research papers for publication. Anti-Cancer Agents in Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments in cancer drug discovery.
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