Endothelin axis is composed of 2 receptors, ETAR and ETBR as well as 3 endothelin ligands endothelin 1 (ET1), endothelin 2 (ET2), endothelin 3 (ET3).

Aberrant activation of Endothelin 1 (ET1) axis is largely recognized as a common mechanism under lying the progression of various solid tumours, including ovarian, prostate, colon, breast, bladder and lung cancers.
Activation of autocrine and paracrine signalling by ET1 binding to its receptors elicits pleiotropic effects on tumour cells and on the host microenvironment.

This activation modulates cell proliferation, apoptosis, migration, epithelial-to-mesenchymal transition, chemoresistance and neovascularization, thus providing a strong rationale for targeting ET1 receptors in cancer.


From Rosano, et al. (2013)