ADC Development Services Targeting ETBR

Antibody-drug conjugates (ADCs) represent one of the most promising and effective therapeutic options for cancer treatment. Melanoma as a fetal cancer has been treated by the ADCs strategy. Creative Biolabs is a bioconjugation service provider focusing primarily on ADCs development targeting a variety of targets. We have built a highly characterized, high-quality ADCs construction platform. Now we provide a full range of ADC development services against the ETBR biomarker.

Introduction of ETBR

ETRB (endothelin B receptor), also known as ETB, HSCR or ABCDS, is a protein encoded by the EDNRB gene in humans. It is a G protein-coupled receptor associated with the activation of phosphatidylinositol-calcium second messenger system. The ligands of the receptor are three potent vasoactive peptides, i.e. ET1, ET2, and ET3. ETBR is mainly expressed on the endothelium and smooth muscle cells. Activation of ETBR on lung smooth muscle cells can cause vasoconstriction and bronchoconstriction. Besides, ETBR is also found to be involved in inflammatory processes. Its overexpression in bronchial smooth muscle cells will lead to airway inflammation.In addition, ETRB is also highly expressed on some tumor cells such as the melanoma, and it is considered as a potential target for the cancer treatment.

Endothelin signaling-endothelial cells. Fig.1 Endothelin signaling-endothelial cells.

Anti-ETBR ADC in Melanoma

ETBR as a G-protein coupled receptor is overexpressed in metastatic melanoma. It has been regarded as a promising target in the ADC development. RG7636 (also known as DEDN6526A) is an ADC against the ETBR, consisting of an anti-ETBR humanized IgG1 monoclonal linked to the antimitotic agent monomethyl auristatin (MMAE) via a protease-cleavable valine-alanine linker. Once the ADC binds to the ETBR target, it can be internalized and release the payload and cause the tumor cell death. Clinical trials demonstrated that RG7636 is safe and tolerable, and has significant antitumor activity in patients with metastatic or unresectable cutaneous, mucosal, or ocular melanoma. Therefore, this ADC represents a novel targeted treatment against melanoma.

Chemical structure of RG7636 (DEDN6526A). Fig.2 Chemical structure of RG7636 (DEDN6526A).

What Can We Do for You?

Creative Biolabs is an experienced service provider focusing on the ADCs development for many years. We provide clients the most affordable, high-quality ADCs design and preparation services with advanced linker-payload synthesis, antibody production and bioconjugation platforms. Our scientists are dedicated to creating the drug-antibody complex with the greatest chance to succeed. In addition, based on the commitment of prompt communication and on-time reporting, our staff will ensure a high-efficiency service to meet the strict project timelines.

Our ADCs development services include:

If you are interested in our services, please contact us for more information.

For lab research use only, not for any in vivo human use.

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