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Updated: Sep 5, 2025

Dual Bioluminescence Imaging of Tumor Progression and Angiogenesis
Published on: August 1, 2019
Recent progress on vascular endothelial growth factor receptor inhibitors with dual targeting capabilities for tumor
Yun Liu1,2, Yang Li1,2, Yuxi Wang2,3
1Department of Neurology, Joint Research Institution of Altitude Health, West China Hospital, Sichuan University, Chengdu, 610041, Sichuan, China.
Abstract:
Vascular endothelial growth factor receptors (VEGFRs) are a family of receptor protein tyrosine kinases that play an important role in the regulation of tumor-induced angiogenesis. Currently, VEGFR inhibitors have been widely used in the treatment of various tumors. However, current VEGFR inhibitors are limited to a certain extent due to limited clinical efficacy and potential toxicity, which hinder their clinical application. Thus, the development of new strategies to improve the clinical outcomes and minimize the toxic effects of VEGFR inhibitors is required. Given the synergistic effect of VEGFR and other therapies in tumor development and progression, VEGFR dual-target inhibitors are becoming an attractive approach due to their favorable pharmacodynamics, low toxicity, and anti-resistant effects. This perspective provides an overview of the development of VEGFR dual-target inhibitors from multiple aspects, including rational target combinations, drug discovery strategies, structure-activity relationships and future directions.
Insights
New dual-target inhibitors for vascular endothelial growth factor receptors (VEGFRs) show promise for improving cancer treatment. These inhibitors offer better efficacy and reduced toxicity compared to current options.
Area of Science:
- Oncology
- Pharmacology
- Molecular Biology
Background:
- Vascular endothelial growth factor receptors (VEGFRs) are crucial for tumor angiogenesis.
- Current VEGFR inhibitors have limitations in clinical efficacy and toxicity.
- There is a need for improved therapeutic strategies targeting VEGFRs.
Purpose of the Study:
- To provide an overview of VEGFR dual-target inhibitors.
- To discuss rational target combinations for dual-inhibition strategies.
- To explore drug discovery, structure-activity relationships, and future directions for VEGFR dual-target inhibitors.
Main Methods:
- Literature review and analysis of existing research on VEGFR inhibitors.
- Examination of synergistic effects between VEGFR and other therapeutic targets.
- Discussion of drug design principles and structure-activity relationships for dual-target inhibitors.
Main Results:
- VEGFR dual-target inhibitors present a promising approach with potential for improved pharmacodynamics.
- These inhibitors may offer reduced toxicity and overcome resistance mechanisms.
- Synergistic effects with other therapies enhance anti-tumor activity.
Conclusions:
- VEGFR dual-target inhibitors represent an attractive strategy for cancer therapy.
- Further research into rational target combinations and drug discovery is warranted.
- Optimizing dual-target inhibitors can lead to improved clinical outcomes and reduced side effects.
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