EphB4 Human RTK Kinase Cell Based Agonist Functional LeadHunter Assay - US

Background Information:

Eph family tyrosine kinase receptors consist of two groups: EphA group members respond to ephrin-A, which is anchored to the cell membrane by glycosylphosphatidylinositol, whereas EphB group members respond to ephrin-B, containing a transmembrane domain. Among them, only EphA4 can cross-respond to both ephrin-A and -B. Expression of the EPB4 (EphB4, Ephrin type-B receptor 4, Tyrosine-protein kinase receptor HTK, EC 2.7.1.112) receptors and their ephrinB ligands play a key role in normal vascular formation as well as in diabetic retinopathy, malignant tumor progression and angiogenesis. Inhibition of EPB4 may be used in the treatment of diabetic renopathy and angioproliferative tumors.

PathHunter Receptor Tyrosine Kinase (RTK) Functional cell lines are engineered to co-express a ProLink™ (PK) tagged RTK, an Enzyme Acceptor (EA) tagged SH2 domain, and, in some cases, an untagged co-receptor. Activation of the RTK-PK induces receptor dimerization, leading to SH2-EA recruitment, and 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:

EphB4

Uniprot Number:

P54760

Protein Aliases:

Hepatoma transmembrane kinase|Tyrosine-protein kinase TYRO11

Gene Name:

EPHB4

Gene ID:

2050

Gene Aliases:

Tyro11

Accession Number:

NM_004444

Organism:

Human

Cell Type:

U2OS