HTScan® EGF Receptor Kinase Assay Kit

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Product Information

Product Description

The kit provides a means of performing kinase activity assays with recombinant human EGFR kinase. It includes active EGFR kinase (supplied as a GST fusion protein), a biotinylated peptide substrate and a phospho-tyrosine monoclonal antibody for detection of the phosphorylated form of the substrate peptide.

Molecular Formula

Peptide substrate, Biotin-PTP1B (Tyr66): 2141 Daltons. GST-EGFR Kinase: 87 kDa.

Background

The epidermal growth factor (EGF) receptor is a transmembrane tyrosine kinase that belongs to the HER/ErbB protein family. Ligand binding results in receptor dimerization, autophosphorylation, activation of downstream signaling, internalization, and lysosomal degradation (1,2). Phosphorylation of EGF receptor (EGFR) at Tyr845 in the kinase domain is implicated in stabilizing the activation loop, maintaining the active state enzyme, and providing a binding surface for substrate proteins (3,4). c-Src is involved in phosphorylation of EGFR at Tyr845 (5). The SH2 domain of PLCγ binds at phospho-Tyr992, resulting in activation of PLCγ-mediated downstream signaling (6). Phosphorylation of EGFR at Tyr1045 creates a major docking site for the adaptor protein c-Cbl, leading to receptor ubiquitination and degradation following EGFR activation (7,8). The GRB2 adaptor protein binds activated EGFR at phospho-Tyr1068 (9). A pair of phosphorylated EGFR residues (Tyr1148 and Tyr1173) provide a docking site for the Shc scaffold protein, with both sites involved in MAP kinase signaling activation (2). Phosphorylation of EGFR at specific serine and threonine residues attenuates EGFR kinase activity. EGFR carboxy-terminal residues Ser1046 and Ser1047 are phosphorylated by CaM kinase II; mutation of either of these serines results in upregulated EGFR tyrosine autophosphorylation (10).

Alternate Names

EGF; ERBB1; HER1; high through put; HTS; Kinase; kinase assay; tyrosine kinase

Database Links

UniProt ID: P00533

Entrez-Gene Id: 1956

Limited Uses

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For Research Use Only. Not for Use in Diagnostic Procedures.

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HTScan® EGF Receptor Kinase Assay Kit #7909