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VEGF Signaling Pathway
A comprehensive guide to Vascular Endothelial Growth Factors, VEGFR2 signal transduction, and targeted anti-angiogenic therapies in oncology.
Vascular endothelial growth factors (VEGFs) are master regulators of vascular development and of blood and lymphatic vessel function during health and disease in the adult.
VEGF is produced by several cell types such as fibroblasts, inflammatory cells, and importantly, many tumor cells. Production is often massively upregulated in response to increasing tumor hypoxia via the HIF-1α pathway.
The VEGF Family
Currently, the VEGF family is composed of five structurally related factors: VEGFA (the most well-characterized, denoted as VEGFA165), VEGFB, VEGFC, VEGFD, and placenta growth factor (PlGF).
The VEGF family members are primarily homodimeric polypeptides, although naturally occurring heterodimers of VEGFA and PlGF have been described. The main VEGF receptor on endothelial cells is VEGFR2, which is essential for endothelial cell biology during development and in the adult, both in physiology and pathology. Consequently, significantly more is known about VEGFR2 signaling than for the other VEGF receptors.
1. VEGF Signaling Pathway Map
The binding of VEGF ligands to their corresponding receptor tyrosine kinases initiates a complex network of intracellular signal transduction pathways.
2. VEGFR2 Signal Transduction
In VEGFA165-mediated signal transduction of VEGFR2, the coordinated arrangement of endothelial cells in three dimensions to form and maintain a vascular tube requires precise endothelial cell proliferation, migration, survival, and permeability.
1
Ligand Binding
Signal transduction begins when VEGFA binds directly to the extracellular Ig-like domains 2 and 3 of the VEGFR2 receptor, inducing receptor dimerization.
2
Intracellular Phosphorylation
Dimerization triggers autophosphorylation at specific tyrosine sites within the intracellular domain of VEGFR2. These phosphorylation sites serve as high-affinity docking stations for downstream signaling molecules.
3
Endothelial Response
Recruited mediators (such as PLCγ, PI3K/Akt, and Ras/MAPK components) activate distinct downstream cascades, ultimately resulting in robust biological responses including cell proliferation, migration, survival, and vascular permeability.
3. Pathological Significance & Clinical Inhibitors
Activation of the VEGF pathway has been identified as a critical driver in many disease processes, ranging from solid tumor cancers to autoimmunity and retinopathy.
Clinical Interventions: Because this pathway is absolutely central to disease-driven angiogenesis, the pharmaceutical industry has developed highly specific inhibitors targeting both sides of the interaction:
- Targeting the Ligand: Bevacizumab, VEGF-Trap, Ranibizumab.
- Targeting the Receptor: Cediranib, Pazopanib, Sorafenib, Sunitinib, Vandetanib, Axitinib, Telatinib, Semaxanib, Motesanib, Vatalanib, Zactima.
4. A Selection of VEGF Research Products
Biorbyt offers a comprehensive catalog of highly validated primary antibodies, ELISA kits, and active recombinant proteins to map the VEGF signaling cascade.
| Cat. Code | Description | Product Type |
|---|---|---|
| orb11557 | VEGFR2 | Primary Antibody |
| orb76050 | Human VEGFR2 | ELISA Kit |
| orb437591 | Porcine VEGFR2 | ELISA Kit |
| orb244321 | Human VEGFR2 | Recombinant Protein |
| orb191500 | VEGF | Primary Antibody |
| orb1817182 | Human VEGFA | Active Recombinant Protein |
| orb10845 | HSP27 | Primary Antibody |
| orb561761 | Human HSP27 | ELISA Kit |
| orb14551 | FAK | Primary Antibody |
| orb1676540 | Ras | Primary Antibody |
5. Small Molecule Inhibitors & Assays
Biorbyt has an extensive range of small molecules available as research reagents to target specific nodes in the VEGF pathway. We provide the best service and a simple buying process allowing you to focus on your valuable research.
Pathway Inhibition
Sorafenib
A highly potent multikinase inhibitor that targets VEGFR, PDGFR, and Raf kinases, severely disrupting tumor angiogenesis.
Pathway Inhibition
Sunitinib
A well-characterized receptor tyrosine kinase (RTK) inhibitor utilized globally in oncology and angiogenesis research models.
Quantification
Human VEGFA ELISA Kits
Quantify the release of VEGF ligand into cell culture supernatants to evaluate the hypoxic response of tumor cells.
Pathway Inhibition
Pazopanib
A potent and selective multi-targeted receptor tyrosine kinase inhibitor of VEGFR1, VEGFR2, and VEGFR3.
Take a look at our product pages where you will find competitive pricing, lead times, and easy delivery options. If you have any questions, just ask us.