2. Academic Validation
  3. Research progress of VEGFR small molecule inhibitors in ocular neovascular diseases

Research progress of VEGFR small molecule inhibitors in ocular neovascular diseases

  • Eur J Med Chem. 2023 Sep 5:257:115535. 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
Affiliations

Affiliations

  • 1 School of Life Science and Engineering, Southwest Jiaotong University, Chengdu 610031, China.
  • 2 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.
  • 3 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.
  • 4 College of Medicine, Southwest Jiaotong University, Chengdu, Sichuan, 611756, China.
  • 5 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. Electronic address: [email protected].
  • 6 Department of Pharmacy, The General Hospital of Western Theater Command of PLA, Chengdu, 610083, China. Electronic address: [email protected].
  • 7 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. Electronic address: [email protected].
PMID: 37285684 DOI: 10.1016/j.ejmech.2023.115535
Abstract

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.

Keywords

Angiogenesis; Inhibitors; Ocular neovascularization; VEGF; VEGFR.

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