<br>VEGFR小分子抑制剂在眼部新生血管疾病中的研究进展,European Journal of Medicinal Chemistry

当前位置： X-MOL 学术 › Eur. J. Med. Chem. › 论文详情

Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)

VEGFR小分子抑制剂在眼部新生血管疾病中的研究进展
European Journal of Medicinal Chemistry ( IF 6.0 ) Pub Date : 2023-05-29 , DOI: 10.1016/j.ejmech.2023.115535
Die Jiang ₁ , Ting Xu ₂ , Lei Zhong ₃ , Qi Liang ₄ , Yonghe Hu ₅ , Wenjing Xiao ₆ , Jianyou Shi ₇

Affiliation

School of Life Science and Engineering, Southwest Jiaotong University, Chengdu 610031, China.
Department of Anesthesiology, Sichuan Academy of Medical Sciences & Sichuan Provincial People's Hospital, School of Medicine, University of Electronic Science and Technology of China, Chengdu, Sichuan, 610072, China.
Department of Pharmacy, Personalized Drug Therapy Key Laboratory of Sichuan Province, Sichuan Academy of Medical Science & Sichuan Provincial People's Hospital, Sichuan Provincial People's Hospital, School of Medicine, University of Electronic Science and Technology of China, Chengdu, 610072, China.
College of Medicine, Southwest Jiaotong University, Chengdu, Sichuan, 611756, China.
School of Life Science and Engineering, Southwest Jiaotong University, Chengdu 610031, China; Department of Pharmacy, The General Hospital of Western Theater Command of PLA, Chengdu, 610083, China.
Department of Pharmacy, The General Hospital of Western Theater Command of PLA, Chengdu, 610083, China.
Department of Pharmacy, Personalized Drug Therapy Key Laboratory of Sichuan Province, Sichuan Academy of Medical Science & Sichuan Provincial People's Hospital, Sichuan Provincial People's Hospital, School of Medicine, University of Electronic Science and Technology of China, Chengdu, 610072, China; State Key Laboratory of Southwestern Chinese Medicine Resources, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China.

血管生成是现有血管产生新血管的生物过程，对于身体生长和发育、伤口愈合和肉芽组织形成至关重要。血管内皮生长因子受体 (VEGFR) 是一种重要的细胞膜受体，可与 VEGF 结合来调节血管生成和维持。 VEGFR 信号传导失调可导致多种疾病，例如癌症和眼部新生血管疾病，使其成为疾病治疗的重要研究领域。目前眼科常用的抗VEGF药物主要有贝伐珠单抗、雷珠单抗、康柏西普和阿柏西普四种大分子药物。虽然这些药物在治疗眼部新生血管疾病方面相对有效，但其大分子特性、强亲水性和血眼屏障穿透性差限制了其疗效。然而，VEGFR小分子抑制剂具有较高的细胞渗透性和选择性，使其能够特异性地穿过并与VEGF-A结合。因此，它们对目标的作用持续时间较短，并在短期内为患者提供显着的治疗益处。因此，需要开发VEGFR的小分子抑制剂来靶向眼部新生血管形成疾病。本文综述了潜在的VEGFR小分子抑制剂用于眼部新生血管疾病靶向治疗的最新进展，旨在为VEGFR小分子抑制剂的未来研究提供参考。

"点击查看英文标题和摘要"

Research progress of VEGFR small molecule inhibitors in ocular neovascular diseases

Angiogenesis is the biological process in which existing blood vessels generate new ones and it is essential for body growth and development, wound healing, and granulation tissue formation. Vascular endothelial growth factor receptor (VEGFR) is a crucial cell membrane receptor that binds to VEGF to regulate angiogenesis and maintenance. Dysregulation of VEGFR signaling can lead to several diseases, such as cancer and ocular neovascular disease, making it a crucial research area for disease treatment. Currently, anti-VEGF drugs commonly used in ophthalmology are mainly four macromolecular drugs, Bevacizumab, Ranibizumab, Conbercept and Aflibercept. Although these drugs are relatively effective in treating ocular neovascular diseases, their macromolecular properties, strong hydrophilicity, and poor blood-eye barrier penetration limit their efficacy. However, VEGFR small molecule inhibitors possess high cell permeability and selectivity, allowing them to traverse and bind to VEGF-A specifically. Consequently, they have a shorter duration of action on the target, and they offer significant therapeutic benefits to patients in the short term. Consequently, there is a need to develop small molecule inhibitors of VEGFR to target ocular neovascularization diseases. This review summarizes the recent developments in potential VEGFR small molecule inhibitors for the targeted treatment of ocular neovascularization diseases, with the aim of providing insights for future studies on VEGFR small molecule inhibitors.

更新日期：2023-05-29

点击分享查看原文

点击收藏

阅读更多本刊新发论文本刊介绍/投稿指南