HER2 (ERBB2)/HER4 (ErbB4) Human RTK Kinase Cell Based Agonist Dimerization LeadHunter Assay - US

Background Information:

Human EGF receptor 2 (HER2, ERBB2) tyrosine kinase is an EGF receptor-related protein tyrosine kinase which is overexpressed in many mammary and ovarian carcinomas. Binding of the ligand to the receptor is believed to activate the receptor’s intrinsic protein kinase activity, initiating a signal transduction pathway which leads to increased cell proliferation. Truncated HER2, lacking the extracellular and transmembrane regions, is constitutively active. The active kinase transfers g-phosphates of ATP to the phenolic hydroxyl of specific tyrosine residues on target proteins.

The PathHunter® Dimerization assay detects ligand induced dimerization of two subunits of a receptor-dimer pair. The cells have been engineered to co-express one receptor subunit fused to Enzyme Donor (ED), and a second dimer partner fused to Enzyme Acceptor (EA). Cytoplasmic tail may have been deleted from one or both receptors. Binding of an agonist to one receptor subunit induces it to interact with its dimer partner, forcing complementation of the two enzyme fragments. This results in the formation of a functional enzyme that hydrolyzes a substrate to generate a chemiluminescent signal.

Family:

Kinase

Sub Family:

RTK

Class:

Protein Tyrosine

Protein Name:

HER2

Uniprot Number:

P04626

Protein Aliases:

neuro/glioblastoma derived oncogene homolog|human epidermal growth factor receptor 2

Gene Name:

ERBB2

Gene ID:

2064

Gene Aliases:

NEU|HER-2|CD340|HER2

Accession Number:

NM_004448.2

Organism:

Human

Cell Type:

U2OS