Document Type
Article
Publication Date
6-4-2025
Abstract
Vascular endothelial growth factor receptors (VEGFRs) are key regulators of angiogenesis, lymphangiogenesis, and vascular permeability, playing essential roles in both physiological and pathological processes. The VEGFR family, including VEGFR-1, VEGFR-2, and VEGFR-3, interacts with structurally related VEGF ligands (VEGFA, VEGFB, VEGFC, VEGFD, and placental growth factor [PlGF]), activating downstream signaling pathways that mediate critical cellular processes, including proliferation, migration, and survival. Dysregulation of VEGFR signaling has been implicated in numerous diseases, such as cancer, cardiovascular conditions, and inflammatory disorders. Targeting VEGFRs with radiopharmaceuticals, such as radiolabeled peptides, antibodies, and specific tracers like 64Cu-bevacizumab and 89Zr-ramucirumab, has emerged as a powerful strategy for non-invasive imaging of VEGFR expression and distribution in vivo. Through positron emission tomography (PET) and single-photon emission computed tomography (SPECT), these targeted tracers enable real-time visualization of angiogenic and lymphangiogenic activity, providing insights into disease progression and therapeutic responses. This review explores the current advances in VEGFR-targeted imaging, focusing on the development of novel tracers, radiolabeling techniques, and their in vivo imaging characteristics. We discuss the preclinical and clinical applications of VEGFR imaging, highlight existing challenges, and provide perspectives on future innovations that could further enhance precision diagnostics and therapeutic monitoring in angiogenesis and lymphangiogenesis- driven diseases.
Recommended Citation
Karimi, Hanieh; Lee, Sarah; Xu, Wenqi; Langhans, Sigrid A.; Johnson, David K.; Stauff, Erik; Kecskemethy, Heidi H.; Averill, Lauren W.; and Yue, Xuyi, "Advances in Molecular Imaging of VEGFRs: Innovations in Imaging and Therapeutics" (2025). Department of Radiology Faculty Papers. Paper 175.
https://jdc.jefferson.edu/radiologyfp/175
Creative Commons License
This work is licensed under a Creative Commons Attribution 4.0 License.
PubMed ID
40508182
Language
English
Included in
Amino Acids, Peptides, and Proteins Commons, Diagnosis Commons, Enzymes and Coenzymes Commons, Radiology Commons, Therapeutics Commons
Comments
This article is the author's final published version in International Journal of Molecular Sciences, Volume 26, issue 11, June 2025, 5373.
The published version is available at https://doi.org/10.3390/ijms26115373.
Copyright © 2025 by the authors