scholarly journals The endothelin axis in cancer: the promise and the challenges of molecularly targeted therapyThis article is one of a selection of papers published in the special issue (part 2 of 2) on Forefronts in Endothelin.

2008 ◽  
Vol 86 (8) ◽  
pp. 473-484 ◽  
Author(s):  
Anna Bagnato ◽  
Francesca Spinella ◽  
Laura Rosanò
Keyword(s):  
Epithelial To Mesenchymal Transition ◽  
Molecular Level ◽  
Receptor Subtypes ◽  
Endothelin Receptor Antagonists ◽  
Endothelin Receptor ◽  
Receptor Antagonists ◽  
Mesenchymal Transition ◽  
Novel Therapeutic Strategies ◽  
G Protein Coupled ◽  
Selection Of

The endothelin (ET) axis, which includes ET-1, ET-2, ET-3, and 2 G protein-coupled receptor subtypes, ETAR and ETBR, promotes growth and progression of a variety of tumors, such as prostatic, ovarian, renal, pulmonary, colorectal, cervical, breast, lung, bladder, endometrial carcinoma, Kaposi’s sarcoma, brain tumors, and melanoma. Acting on selective receptors, ET-1 regulates mitogenesis, cell survival, angiogenesis, bone remodeling, stimulation of nociceptors, tumor-infiltrating immune cells, epithelial-to-mesenchymal transition, invasion, and metastatic dissemination. At the molecular level, endothelin receptor antagonists, besides providing ideal tools for dissecting the ET axis, have demonstrated their potential in developing novel therapeutic strategies. Emerging experimental and clinical data demonstrate that interfering with endothelin receptors provides an opportunity for the development of rational combinatorial approaches using endothelin receptor antagonists in combination with chemotherapy or molecularly targeted therapy.

Endothelin receptor antagonists: a brief review

1994 ◽  
Vol 72 (11) ◽  
pp. 1469-1471 ◽  
Author(s):  
Suzanne Moreland
Keyword(s):  
Smooth Muscle ◽  
Receptor Antagonist ◽  
Receptor Subtypes ◽  
Endothelin Receptor Antagonists ◽  
Endothelin Receptor ◽  
Receptor Antagonists ◽  
Vascular Activity ◽  
Vasodilatory Activity ◽  
Healthy Control ◽  
Circulating Levels

The endothelins are a family of potent vasoconstrictors, some of which also have vasodilatory activity. In many diseases associated with tissue hypoxia or ischemia and in diseases in which vasoconstriction plays a role, the circulating levels of endothelin are higher than in healthy, control subjects. These findings stimulated research aimed at discovering endothelin receptor antagonists. This review focuses on the binding potency and vascular activity of these new peptide and nonpeptide endothelin receptor antagonists.Key words: endothelin, endothelin receptor subtypes, vascular smooth muscle, endothelin receptor antagonist.

ChemInform Abstract: 2-Aryloxycarbonylthiophene-3-sulfonamides: Highly Potent and ETA Selective Endothelin Receptor Antagonists.

ChemInform ◽  
2010 ◽  
Vol 28 (50) ◽  
pp. no-no
Author(s):  
B. RAJU ◽  
C. WU ◽  
R. CASTILLO ◽  
I. OKUN ◽  
F. STAVROS ◽  
...  
Keyword(s):  
Endothelin Receptor Antagonists ◽  
Endothelin Receptor ◽  
Receptor Antagonists

Multiple Compound-Related Adverse Properties Contribute to Liver Injury Caused by Endothelin Receptor Antagonists

2014 ◽  
Vol 352 (2) ◽  
pp. 281-290 ◽  
Author(s):  
J. Gerry Kenna ◽  
Simone H. Stahl ◽  
Julie A. Eakins ◽  
Alison J. Foster ◽  
Linda C. Andersson ◽  
...  
Keyword(s):  
Liver Injury ◽  
Endothelin Receptor Antagonists ◽  
Endothelin Receptor ◽  
Receptor Antagonists
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