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Application: Study complex formation and screen compounds and biologics that block the binding of NRG1β to HER4 for drug discovery and high throughput screening (HTS) applications.
Background: HER4 (human epidermal growth factor receptor 4), also known as ErbB4 or receptor-tyrosine kinase 4, is a receptor tyrosine kinase protein of the EGFR family. It is required for the development of the heart, nervous system, and mammary gland, and can also be found in the postsynaptic side of neuromuscular junctions and epidermis. HER4 is activated by betacellulin and heparin binding EGF-like growth factor (HB-EGF) and is involved in mitogenesis and cell differentiation. HER4 undergoes a conformational change upon ligand binding and forms homodimers or heterodimers with other HER proteins to activate the MAPK (mitogen-activated protein kinases) and PI3K (phosphoinositide 3-kinase)/AKT pathways. Mutations in this protein can result in cancer but have also been linked to ALS (amyotrophic lateral sclerosis) type 19 and schizophrenia. The role of this protein as oncogene or suppressor is still not fully determined, potentially being dependent on the cancer type. Several HER4 inhibitors targeting the kinase domain of the protein have been developed and are undergoing clinical trials. Afatinib, a pan-HER inhibitor, has been approved for the treatment of NSCLC (non-small cell lung cancer), but may cause acute liver injury and death. 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. Binding of NRG1 to HER4 play an important role in cortical development, and cardiomyocyte proliferation and regeneration, by inducing dimerization to HER2 and activation of multiple signaling pathways. The high similarity between HER3 and HER4 make the development of specific antibodies challenging. Studies focusing on molecules targeting NRG1/HER4 will open new therapies for patients with neurodevelopment and cardiovascular disorders.
Contraindications: The NRG1β: HER4 (ERBB4) Chemiluminescent Assay Kit is compatible with up to 1% final DMSO concentration.
Description: The NRG1β: HER4 (ERBB4) Chemiluminescent Assay Kit is an ELISA-based assay designed to measure the binding between NRG1β (neuregulin-1β) and HER4 (human epidermal growth factor receptor 4, also known as ERBB4) for screening and profiling applications. The NRG1β: HER4 (ERBB4) Chemiluminescent Assay Kit comes with enough purified NRG1β (amino acids 2-246) and HER4 (amino acids 26-651) 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, HER4 is added in an optimized assay buffer. Unbound HER4 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 HER4 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: Q15303
Warnings: Avoid freeze/thaw cycles
Biosafety Level: Not applicable (BSL-1)
References: El-Gamal M., et al., 2021 Molecules 26(23):7376.
Shi L. and Bergson C., 2020 Translational Psychiatry 10: 190.
Shan L., et al., 2020 Scientific Reporters 10: 17257.
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