Recombinant Human ETRB protein

The ETRB (Endothelin Receptor Type B) recombinant protein is a key component in studying the endothelin signaling pathway, which plays critical roles in cardiovascular regulation, cell proliferation, and tissue homeostasis. Endothelin receptors, classified as ETA and ETB, are G protein-coupled receptors (GPCRs) that bind endothelin peptides (ET-1. ET-2. ET-3). Specifically, ETBR is primarily expressed in endothelial cells, smooth muscle, and the nervous system. Unlike ETA, which predominantly mediates vasoconstriction, ETBR often counterbalances these effects by promoting vasodilation through nitric oxide release and clearing endothelin via receptor-mediated internalization.

Recombinant ETBR proteins are engineered using molecular cloning techniques, typically expressed in mammalian systems (e.g., HEK293 or CHO cells) to ensure proper post-translational modifications and membrane localization. These proteins retain functional domains, including seven transmembrane helices and ligand-binding sites, enabling in vitro studies of receptor-ligand interactions, signal transduction mechanisms (e.g., Gαi/o and Gαq coupling), and downstream effects like MAPK activation or calcium mobilization.

ETBR dysregulation is implicated in pathologies such as pulmonary hypertension, cancer metastasis, and neurodegenerative disorders. Recombinant ETBR serves as a vital tool for drug discovery, aiding in the development of antagonists (e.g., bosentan) or agonists targeting endothelin-related diseases. It also facilitates structural studies (e.g., X-ray crystallography) to elucidate receptor activation mechanisms and design selective therapeutics. Current research focuses on ETBR's dual role in pro- and anti-tumorigenic signaling, highlighting its therapeutic potential in precision medicine. Challenges remain in optimizing receptor stability for biophysical assays and addressing species-specific ligand affinity differences during preclinical testing.