Targeting VEGF-neuropilin interactions: a promising antitumor strategy
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Published on: June 28, 2021
Kewen Peng1, Ying Bai1, Qihua Zhu2
1Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China.
Abstract:
Inhibition of vascular endothelial growth factor (VEGF) or its corresponding receptor (VEGFR) has been validated as an efficacious antiangiogenetic approach for cancer treatment. More recently, neuropilins (NRPs), the essential coreceptors for VEGF, have also been shown to have a significant role in VEGF signaling. Given the multifaceted effects of VEGF-NRP interactions on tumor initiation and progression, the exploration of new chemical entities that selectively block these interactions has recently attracted considerable interest as a novel antitumor strategy. Here, we summarize the biological functions of VEGF-NRP interactions in tumor biology, analyze the structural basis for these interactions, and present a detailed discussion of the development of the NRP antagonists reported so far.
Insights
Targeting vascular endothelial growth factor (VEGF) and its coreceptors, neuropilins (NRPs), offers a novel anti-cancer strategy. Blocking VEGF-NRP interactions shows promise for inhibiting tumor growth and progression.
Area of Science:
- Oncology
- Molecular Biology
- Biochemistry
Background:
- Vascular endothelial growth factor (VEGF) and its receptor (VEGFR) inhibition is an established anti-angiogenesis cancer therapy.
- Neuropilins (NRPs) act as essential coreceptors for VEGF, playing a critical role in VEGF signaling pathways.
- VEGF-NRP interactions significantly influence tumor initiation and progression.
Purpose of the Study:
- To explore novel anti-tumor strategies by targeting VEGF-NRP interactions.
- To summarize the biological functions of VEGF-NRP interactions in tumor biology.
- To discuss the structural basis of VEGF-NRP interactions and the development of NRP antagonists.
Main Methods:
- Literature review and analysis of existing research on VEGF-NRP interactions.
- Examination of the structural mechanisms underlying VEGF binding to NRPs.
- Compilation and discussion of reported NRP antagonist development.
Main Results:
- VEGF-NRP interactions are integral to tumor development and progression.
- Understanding the structural basis of these interactions is key to designing targeted therapies.
- Several NRP antagonists have been developed, representing a new frontier in cancer treatment.
Conclusions:
- Targeting VEGF-NRP interactions presents a promising novel anti-cancer therapeutic approach.
- Further research into NRP antagonists could lead to more effective cancer treatments.
- Selective blockade of VEGF-NRP interactions offers a refined strategy beyond traditional VEGF/VEGFR inhibition.
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