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Application: Screen or titrate small molecule inhibitors or antibodies that block VEGF165 binding to VEGFR2 for drug discovery and high-throughput screening (HTS) applications.
Background: VEGF165 (Vascular Endothelial Growth Factor 165), a potent isoform of VEGF-A, belongs to the VEGF family of homodimer glycoproteins and is produced and secreted by various cells when angiogenesis is required. Angiogenesis involves endothelial cell proliferation, migration, and formation of blood vessels, which under normal conditions serve to provide nutrients and oxygen to tissues during development or wound healing. However, tumor cells can promote new blood vessel formation by secreting pro-angiogenesis factors. VEGF-A can bind to both VEGFR1 (Vascular Endothelial Growth Factor Receptor 1) and VEGFR2, also known as KDR (kinase insert domain receptor), on the surface of endothelial cells or cancer cells. VEGFR2 is considered the main signaling receptor, while VEGFR1 leads to a weak signaling and can be seen as a decoy receptor. Ligand binding induces VEGFR2 receptor dimerization and activates its tyrosine kinase activity. As a result, multiple downstream signaling cascades, including the MAPK (mitogen activated protein kinase) pathway, get activated. The VEGF-VEGFR signal pathway has been a significant target in therapeutic strategies aimed at controlling angiogenesis in diseases like cancer and AMD (age macular degeneration), and several small molecules, neutralizing antibodies and blockers have been FDA-approved. However, the development of drug resistance is still a challenge. The use of combinatory therapy or development of new generation drugs will continue to benefit cancer therapy.
Contraindications: The DMSO concentration in the final reaction should be ≤1%.
Description: The VEGF165:VEGFR2 [Biotinylated] Inhibitor Screening Chemiluminescence Assay Kit is an ELISA designed for screening and profiling molecules that block the binding between VEGF165 (vascular endothelial growth factor 165) and VEGFR2 (vascular endothelial growth factor receptor 2). This kit comes in a convenient 96-well format, with enough recombinant biotin-labeled VEGFR2 (amino acids20-764(end), extracellular domain), purified VEGF165 (amino acids 27-191), streptavidin-labeled HRP, and assay buffer for 100 binding reactions.
Storage Stability: This assay kit will perform optimally for up to 6 months from date of receipt when the materials are stored as directed.
Uniprot: VEGF165: P15692; VEGFR2: P35968
Warnings: Avoid freeze/thaw cycles
Biosafety Level: Not applicable (BSL-1)
References: Wang L., et al., 2024 Front Pharmacol. 14:1307860.
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