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Updated: Nov 15, 2025
A Simple Bioassay for the Evaluation of Vascular Endothelial Growth Factors
Published on: March 15, 2016
Molecular Targeting of Epidermal Growth Factor Receptor (EGFR) and Vascular Endothelial Growth Factor Receptor
Nichole E M Kaufman1, Simran Dhingra1, Seetharama D Jois2
1Department of Chemistry, Louisiana State University, Baton Rouge, LA 70803, USA.
Abstract:
Epidermal growth factor receptor (EGFR) and vascular endothelial growth factor receptor (VEGFR) are two extensively studied membrane-bound receptor tyrosine kinase proteins that are frequently overexpressed in many cancers. As a result, these receptor families constitute attractive targets for imaging and therapeutic applications in the detection and treatment of cancer. This review explores the dynamic structure and structure-function relationships of these two growth factor receptors and their significance as it relates to theranostics of cancer, followed by some of the common inhibition modalities frequently employed to target EGFR and VEGFR, such as tyrosine kinase inhibitors (TKIs), antibodies, nanobodies, and peptides. A summary of the recent advances in molecular imaging techniques, including positron emission tomography (PET), single-photon emission computerized tomography (SPECT), computed tomography (CT), magnetic resonance imaging (MRI), and optical imaging (OI), and in particular, near-IR fluorescence imaging using tetrapyrrolic-based fluorophores, concludes this review.
Insights
This review covers epidermal growth factor receptor (EGFR) and vascular endothelial growth factor receptor (VEGFR) in cancer theranostics. It details their structure, function, targeting inhibitors, and advanced molecular imaging techniques.
Area of Science:
- Oncology
- Molecular Biology
- Biochemistry
Background:
- Epidermal growth factor receptor (EGFR) and vascular endothelial growth factor receptor (VEGFR) are key receptor tyrosine kinases.
- Overexpression of EGFR and VEGFR is common in various cancers, making them critical targets.
Purpose of the Study:
- To review the dynamic structure and function of EGFR and VEGFR.
- To explore their significance in cancer theranostics.
- To summarize inhibition modalities and molecular imaging advancements.
Main Methods:
- Literature review of structural biology, cancer biology, and imaging techniques.
- Analysis of structure-function relationships of EGFR and VEGFR.
- Compilation of data on targeted therapies and molecular imaging modalities.
Main Results:
- EGFR and VEGFR are crucial targets for cancer imaging and therapy.
- Various inhibition strategies, including TKIs, antibodies, nanobodies, and peptides, are effective.
- Advances in molecular imaging like PET, SPECT, CT, MRI, and OI offer new diagnostic and therapeutic approaches.
Conclusions:
- Understanding EGFR and VEGFR structure-function is vital for cancer theranostics.
- Targeted inhibition and advanced molecular imaging are transforming cancer detection and treatment.
- Near-infrared fluorescence imaging shows promise for precise cancer visualization.
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