Evidence is lacking on the differential effects of the two therapeutic concepts of endothelin receptor antagonists (ERAs): the blockade of only the endothelin receptor A (ETAR; selective antagonism) versus both ETAR and endothelin receptor B (ETBR; dual blockade). Ambrisentan, a selective ERA, and bosentan, a dual blocker, are both available for therapy. We hypothesized that there are differenc...

Activation of renal mechanosensory nerves is enhanced by high and suppressed by low sodium dietary intake. Afferent renal denervation results in salt-sensitive hypertension, suggesting that activation of the afferent renal nerves contributes to water and sodium balance. Another model of salt-sensitive hypertension is the endothelin B receptor (ETBR)-deficient rat. ET and its receptors are prese...

IgA nephropathy is the most common primary glomerulonephritis worldwide and carries a substantial risk of kidney failure. New agency-approved therapies, either specifically for or chronic disease in general, hold out hope mitigating renal deterioration patients with nephropathy. The latest addition to this therapeutic armamentarium targets endothelin-A receptor (ETAR). Activation ETAR on multip...

Endothelin-1 receptors (ETAR and ETBR) act as a pivotal regulator in the biological effects of ET-1 and represent a potential drug target for the treatment of multiple cardiovascular diseases. The purpose of the study is to discover dual ETA/ETB receptor antagonists from traditional Chinese herbs. Ligand- and structure-based virtual screening was performed to screen an in-house database of trad...

Introduction. Breast cancer recurrence can develop years after primary treatment. Crosstalk between breast cancer cells and their stromal microenvironment may influence tumor progression. Our primary study aim was to determine whether endothelin-1 (ET-1) expression in tumor and stroma predicts breast cancer relapse. The secondary aim was to determine ET-1/endothelin receptor A (ETAR) role on si...

In their study, Haque and colleagues evaluate the specific endothelin A receptor (ETAR) antagonist zibotentan in colorectal cancer cellular models with relevance to proliferation andmigration potential of tumor cells and stromal fibroblasts. Interestingly, they demonstrate that ETAR is the principal receptor used by ET-1 and provide evidence for involvement of stromal fibroblasts in cancer prog...

Proteinuria is a major pathologic feature of a wide variety of progressive CKD. Even if it is accompanied by a normal GFR, proteinuria indicates significant kidney dysfunction and its presence has been incorporated into definitions for CKD.1 Because proteinuria is an independent risk factor for CKD, it is imperative to determine the mechanisms leading to its development. Current antiproteinuric...

Endothelin-1 (ET-1) predominates in the endothelin family effectively in vascular tone control, mitogenesis, and neuromodulation. Its receptors are widespread in the central nervous system (CNS) associated with endogenous pain control, suggesting an important role of ET-1 in central pain processing. This study aimed to evaluate the effect of central ET-1 on the development of neuropathic pain b...