Anti-ETaR Antibody Introduction

Endothelin (ET) is an amino acid peptide. It has vasoconstrictive properties. Endothelin has been implicated in the development and progression of several diseases. It has been found that in renal disease secondary to hypertension, hyperglycemia, acidosis, insulin, or elevated pro-inflammatory factors, endothelin secretion is increased and can bind to endothelin receptor A (ETα) to produce a series of adverse physiologic effects. These adverse physiologic effects may include persistent constriction of small arteries, the development of hyperfiltration, podocyte injury, and proteinuria. These may ultimately lead to a decrease in glomerular filtration rate. Therefore, it is a valuable research direction to fully understand and utilize the physiological activities of ET and ETα to develop agonist antibody therapies and other therapies for controlling or even treating the disease. Based on our rich field experience and advanced technology platform, Creative Biolabs provides comprehensive services for custom agonistic antibody and anti-ETaR antibody discovery to support agonistic antibody therapy development.

Fig 1. Human endothelin receptor type-B (green) in complex with endothelin-1 (brown).

Anti-ETaR Antibody

The endothelium of vascular tissues produces endothelin-1, as well as the subtypes endothelin A and B. Endothelin A binds to the endothelin A receptor site located at the end of smooth muscle, which causes vasoconstriction while promoting cell reproduction. This substance also binds to proteins called Gq, an initiating chemical process that triggers the release of calcium from the sarcoplasmic reticulum within the cell. Elevated calcium levels also cause vasoconstriction, vasospasm, and increased contractility and heart rate. Scientists have also implied that this peptide causes congestive heart failure and pulmonary hypertension.

Endothelin B binds the endothelin B receptor site, leading to activation of the site that induces nitric oxide formation and causes subsequent vasodilation and inhibition of cell reproduction. The study suggests that under normal conditions, these two isoforms maintain adequate circulation by performing alternate tasks when needed. Researchers believe that endothelin A is the key to high blood pressure. Scientists now believe that there are points at which the balance between endothelin A and B is lost, causing the dominant hypertensive effects of endothelin A.

Studies have found that endothelin receptor blockers block endothelin receptor sites on smooth muscle and organs. Endothelin-1 is one of three endothelin amino acid peptides and has two isoforms that work together to regulate blood pressure. Researchers have developed these drugs that deactivate both isoforms, ensuring that blood vessels relax. Antibody drugs that act on the endothelin receptor Eta are currently used in the treatment of pulmonary arterial hypertension. GMA301 is the first antibody candidate acting on Eta to be developed for pulmonary arterial hypertension. It is able to alleviate the symptoms of high pressure in the pulmonary arteries by binding to the endothelin receptor Eta and reducing the increase in vascular pressure caused by endothelin. The drug has good target specificity, a long duration of action, and no hepatotoxicity associated with small molecule drugs. It can effectively inhibit or slow down the hypertrophy of the right heart and pulmonary artery and further improve the exercise tolerance, quality of life, and survival time of patients with pulmonary arterial hypertension, which is expected to become a new generation of long-lasting drugs for the treatment of pulmonary arterial hypertension and bring new treatment options for patients. With further research, anti-ETaR antibodies will show more potential in the field of disease treatment.

Creative Biolabs has a wealth of knowledge and experience in custom agonistic autoantibody. We would be happy to share with you our knowledge and experience in anti-ETaR antibodies by phage display.

All listed services and products are For Research Use Only. Do Not use in any diagnostic or therapeutic applications.

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