KDR (VEGFR2) Human RTK Kinase Cell Based Antagonist Activity LeadHunter Assay - US

Background Information:

Two high affinity VEGF receptors, Flt-1 (VEGFR-1, activated by placental growth factor PlGF) and KDR (Kinase insert domain receptor, Flk-1/VEGFR2, activated by VEGF), have been identified. These receptors can be divided into three structural regions: seven extracellular Ig-like domains that contain the growth factor binding sites, a single polypeptide chain hydrophobic trans-membrane sequence, and intracellular cytoplasmic domains that confer the tyrosine kinase activity required for signal transduction. VEGF-B and VEGF-D homologues bind with high affinity to FLT1 (fms-related tyrosine kinase 1, vascular endothelial growth factor/vascular permeability factor receptor).

PathHunter Receptor Tyrosine Kinase (RTK) Activity cell lines are engineered to express a fusion of the intracellular catalytic domain from the target RTK and the extracellular ligand binding domain of EGFR. This fusion protein is tagged with ProLink™ (PK). The cells co-express an Enzyme Acceptor (EA) tagged SH2 domain. Ligand induced cross-phosphorylation of the PK-tagged fusion protein leads to SH2-EA recruitment, forcing complementation of the two β-galactosidase enzyme fragments (EA and PK). The resulting functional enzyme hydrolyzes substrate to generate a chemiluminescent signal.

Family:

Kinase

Sub Family:

RTK

Class:

Protein Tyrosine

Protein Name:

KDR (VEGFR2)

Uniprot Number:

P35968

Protein Aliases:

vascular endothelial growth factor receptor 2|fetal liver kinase 1

Gene Name:

KDR

Gene ID:

3791

Gene Aliases:

FLK1|VEGFR|VEGFR2|CD309

Accession Number:

NM_002253

Organism:

Human

Cell Type:

U2OS