ETB Ednra ETBR Endothelin B Receptor GPCR Cell Free Protein

We supply ETBR, Endothelin B receptor, ETB, Ednra, Endothelin receptor type B.

Our Cell-free protein has been Function verificated.

Introduction

Endothelin receptor type B (ETRB) is a G protein-coupled receptor that activates a phosphatidylinoitol-calcium second messenger system. Its ligand, endothelin, consists of a family of three potent vasoactive peptides: ET1, ET2, and ET3. A splice variant (SVR), differing in the intracellular C terminal domain, has been described for this receptor. Both WT and the variant bind ET1. However, they exhibit different responses upon binding - suggesting that these two variants are functionally distinct.

Function

The endothelins and their G protein-coupled receptors A and B have been implicated in numerous diseases and have recently emerged as pivotal players in a variety of malignancies. Tumors overexpress the endothelin 1 (ET-1) ligand and the endothelin-A-receptor (ET_AR). Their interaction induces tumor growth and metastasis by promoting tumor cell survival and proliferation, angiogenesis, and tissue remodeling. On the basis of results from xenograft models, drug development efforts have focused on antagonizing the autocrine-paracrine effects mediated by ET-1/ET_AR.

Endothelin B receptor on the other hand not only inhibits cell growth and vasoconstriction in the vascular system but also functions as a "clearance receptor". This receptor-mediated clearance mechanism is particularly important in the lung, which clears about 80% of circulating endothelin-1.

Subcellular Location

Cell membrane; Multi-pass membrane protein.

DISEASE

Endothelins are able to activate a number of signal transduction processes including phospholipase A2, phospholipase C and phospholipase D, as well as cytosolic protein kinase activation. The play an important role in the regulation of the cardiovascular system and are the most potent vasoconstrictors identified, stimulating cardiac contraction, regulating the release of vasoactive substances, and stimulating mitogenesis in blood vessels . As a result, endothelins are implicated in a number of vascular diseases, including the heart, general circulation and brain. Endothelins stimulate the contraction in almost all other smooth muscles (e.g., uterus, bronchus, vas deferens, stomach) and stimulate secretion in several tissues e.g., kidney, liver and adrenals. Endothelins have also been implicated in a variety of pathophysiological conditions associated with stress including hypertension, myocardial infarction, subarachnoid haemorrhage and renal failure.

Defects in EDNRB are the cause of Hirschsprung disease type 2 (HSCR2); also known as aganglionic megacolon (MGC). HSCR2 is a congenital disorder characterized by absence of enteric ganglia along a variable length of the intestine. It is the most common cause of congenital intestinal obstruction. Early symptoms range from complete acute neonatal obstruction, characterized by vomiting, abdominal distention and failure to pass stool, to chronic constipation in the older child.
Defects in EDNRB are the cause of ABCD syndrome (ABCDS). ABCD syndrome is an autosomal recessive syndrome characterized by albinism, black lock at temporal occipital region, bilateral deafness, aganglionosis of the large intestine and total absence of neurocytes and nerve fibers in the small intestine.

Similarity

Belongs to the G-protein coupled receptor 1 family. Endothelin receptor subfamily. EDNRB sub-subfamily.
 

Advantage of E.Coli system

1. High protein yield
2. Simple cultivation and fast cell growth and lysate preparation
3. Cost-efficient
4. Easy genetic engineering
5. Well-established

Flow chart