The endothelin axis in cancer: The promise and the challenges of molecularly targeted therapy

Anna Bagnato, Francesca Spinella, Laura Rosanò

Research output: Contribution to journalArticlepeer-review


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.

Original languageEnglish
Pages (from-to)473-484
Number of pages12
JournalCanadian Journal of Physiology and Pharmacology
Issue number8
Publication statusPublished - Aug 2008


  • Antitumor therapy
  • Endothelin
  • Endothelin receptor antagonist
  • G protein-coupled receptor

ASJC Scopus subject areas

  • Physiology
  • Pharmacology


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