作为抗癌剂的VEGFR小分子抑制剂的最新发展:专利审查 (2021-2023)
Jing Zeng1, Qichuan Deng2, Zheng Chen3
1School of Food and Bioengineering, Xihua University, Chengdu, Sichuan 610039, China.
Bioorganic chemistry
|March 14, 2024
概括
血管内皮生长因子受体 (VEGFR) 抑制剂向癌症,但面临着挑战. 最近的小分子抑制剂有望降低毒性和提高癌症治疗效率.
科学领域:
- 在瘤学瘤学.
- 分子生物学分子生物学
- 药物发现 药物发现 药物发现
背景情况:
- 血管内皮生长因子受体 (VEGFR) 信号传递对血管生成,瘤生长,侵袭和转移至关重要.
- VEGFR-2是VEGF信号传递的关键媒介,也是各种癌症的重要标,包括NSCLC,HCC和乳腺癌.
- 目前的VEGFR抑制剂显示临床成功,但受到细胞毒性,耐药性和狭窄的指示的限制.
研究的目的:
- 提供VEGFR结构,功能及其在癌症中的作用的概述.
- 审查临床使用的VEGFR抑制剂和最近在专利 (2021-2023) 中报告的小分子抑制剂.
- 分析新型VEGFR抑制剂的体内/体外活性,选择性,结构-活性关系和治疗潜力.
主要方法:
- 对VEGFR结构,功能和抑制剂的文献综述.
- 对小分子VEGFR抑制剂的专利文献 (2021-2023) 的分析.
- 评估抑制剂数据,包括活性,选择性和结构-活性关系.
主要成果:
- 在多种癌症类型中,VEGFR-2是关键标.
- 许多VEGFR抑制剂正在临床使用中,并且正在开发新的小分子.
- 最近的专利强调了具有改善抗药性,较低细胞毒性和增强亲和力的抑制剂.
结论:
- 在癌症治疗中,VEGFR-2 仍然是一个重要的治疗点.
- 小分子VEGFR抑制剂为克服现有治疗方法的局限性提供了潜力.
- 未来的开发工作应该集中在优化针对性癌症治疗的选择性,疗效和安全性.
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