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Application: Study complex formation and screen compounds and biologics that block the binding of NRG1β to HER3 for drug discovery and high throughput screening (HTS) applications.
Background: HER3 (human epidermal growth factor receptor 3) is a transmembrane protein encoded by the ERBB3 gene. HER3 is broadly expressed in human tissues however, increased expression of HER3 has been linked to a variety of solid tumors including ovarian, breast, colon, and gastric cancers and correlates with decreased overall survival in colorectal cancer patients. HER3 has the unique property of being inherently catalytically inactive but still being able to participate in ligand binding, forming heterodimers with nearby receptors of the HER family. The formation of these dimers initiates a cascade of downstream signaling steps critical to cell proliferation. Neuroregulins (NRG) are polypeptide growth factors that bind to HER proteins, with NRG1 being the most studied of the four known proteins in this family. NRG1 specifically binds to HER3 and HER4. NRG1 binding induces dimerization of HER3 with HER2, transphosphorylation, and activation of several pathways such as the PI3K (phosphoinositide 3-kinase)/AKT signaling pathway. Due to HER3 cell surface expression in a variety of cancers and correlation with decreased survival, HER3 is a prospective therapeutic target for antibody-drug conjugate (ADC) development. It has been suggested that elevated levels of NRG1 in the TME (tumor microenvironment) can be considered as a predictive biomarker for the effectiveness of anti-HER3 antibody treatments in cancer. For example anti-HER3 monoclonal antibody, seribantumab, effectively inhibits tumor growth in preclinical models driven by NRG1 fusions. Current efforts are focusing on the development of anti-HER3 therapeutics that block the binding to NRG1, particularly allosteric, non-ligand competing anti-HER3 molecules. One such molecule, 9F7-F11, has resulted in reduced tumor growth in tumor xenografts, versus a ligand-competing anti-HER3 ligand.
Contraindications: The NRG1β: HER3 (ERBB3) Chemiluminescent Assay Kit is compatible with up to 1% final DMSO concentration.
Description: The NRG1β: HER3 (ERBB3) Chemiluminescent Assay Kit is an ELISA-based assay designed to measure the binding between NRG1β (neuregulin-1β) and HER3 (human epidermal growth factor receptor 3, also known as ERBB3) for screening and profiling applications. The NRG1β: HER3 (ERBB3) Chemiluminescent Assay Kit comes with enough purified NRG1β (amino acids 2-246) and HER3 (amino acids 20-643) proteins, detection antibody, assay buffer, and detection reagent for 100 enzyme reactions.A 96-well plate is coated with NRG1β protein. After coating and blocking, HER3 is added in an optimized assay buffer. Unbound HER3 is washed away, and the plate is incubated with a detection antibody. Finally, ELISA ECL substrate is added to produce chemiluminescence that can be measured using a chemiluminescence reader. The chemiluminescence signal is proportional to the efficacy of HER3 binding to NRG1β.
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: P21860
Warnings: Avoid freeze/thaw cycles
Biosafety Level: Not applicable (BSL-1)
References: Le Clorennec C., et al., 2017 Mol Cancer Ther 16(7):1312-1323.
Beji A., et al., 2012 Clin Cancer Res. 18(4):956-68.
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