|本期目录/Table of Contents|

[1]孟小力,刘立丽,王磊.VEGF-B线性模拟肽的设计、合成和抗血管新生活性研究[J].浙江理工大学学报,2025,53-54(自科六):864-871.
　MENG Xiaoli,LIU Lili,WANG Lei.Design, synthesis, and anti-angiogenic activity evaluation of a linear peptide mimicking VEGF-BMENG Xiaoli, LIU Lili, WANG Lei[J].Journal of Zhejiang Sci-Tech University,2025,53-54(自科六):864-871.
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VEGF-B线性模拟肽的设计、合成和抗血管新生活性研究
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浙江理工大学学报[ISSN:1673-3851/CN:33-1338/TS]

卷:
第53-54卷
期数:
2025年自科第六期
页码:
864-871
栏目:
出版日期:
2025-11-10

文章信息/Info

Title:
Design, synthesis, and anti-angiogenic activity evaluation of a linear peptide mimicking VEGF-B
MENG Xiaoli, LIU Lili, WANG Lei
文章编号:
1673-3851(2025)11-0864-08
作者:
孟小力; 刘立丽; 王磊
浙江理工大学生命科学与医药学院,杭州310018
Author(s):
MENG Xiaoli;  LIU Lili;  WANG Lei
College of Life Sciences and Medicine, Zhejiang Sci-Tech University, Hangzhou 310018, China
关键词:
抗血管新生; 血管内皮生长因子受体; 多肽抑制剂; 计算机辅助药物设计; 人脐静脉内皮细胞
分类号:
TQ464.7;R914
文献标志码:
A
摘要:
靶向抗血管内皮生长因子(Vascularendothelialgrowthfactor,VEGF)与血管内皮生长因子受体
(Vascularendothelialgrowthfactorreceptors,VEGFRs)结合的抗血管新生抑制剂,在治疗肿瘤和视网膜黄斑病变上
有重要的临床价值。为进一步探索更多新型高效的靶向VEGFR抑制剂,采用计算机辅助药物设计(Computer-aided
drugdesign,CADD)方法分析VEGF-B与VEGFR1的相互作用,通过模拟VEGF-B关键位点设计多肽抑制剂,合成
得到 VEGF-B线性模拟肽Peptide1,并通过细胞实验评估线性模拟肽Peptide1的靶向性和抗血管新生活性。结果
表明:Peptide1的氨基酸序列为Leu-Thr-Val-Glu-Leu-Met-Gly-Thr-Val-Ala-Lys-Gln-Leu-Val-Pro-Ser-NH2,纯度为
97.3%,合成收率为10.3%;Peptide1能特异性抑制 VEGF与 VEGFR1的结合,半数抑制浓度(Halfmaximal
inhibitoryconcentration,IC50)为 21.9μmol;Peptide1 显 著 抑 制 了 人 脐 静 脉 内 皮 细 胞 (Humanumbilicalvein
endothelialcells,HUVECs)的增殖、迁移及微管形成。该文探索了基于 VEGF-B结构设计 VEGFR多肽抑制剂的可
行性与潜在应用价值,为开发新型靶向抗血管新生多肽抑制剂提供了科学依据。

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备注/Memo

备注/Memo:
收稿日期:2025-04-22 网络出版日期:2025-09-17
基金项目:浙江理工大学青年创新专项项目(24202106-Y)
作者简介:孟小力(1994— ),男,湖北公安人,硕士研究生,主要从事抗肿瘤药物方面的研究。
通信作者:王 磊,E-mail:wanglei@zstu.edu.cn
更新日期/Last Update: 2025-11-25