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Published on: October 14, 2015
The endothelin axis in cancer: the promise and the challenges of molecularly targeted therapy
Anna Bagnato1, Francesca Spinella, Laura Rosanò
1Molecular Pathology and Ultrastructure Laboratory, Regina Elena Cancer Institute, Via delle Messi d'Oro 156, Rome, Italy. bagnato@ifo.it
Abstract:
The endothelin (ET) axis, which includes ET-1, ET-2, ET-3, and 2 G protein-coupled receptor subtypes, ET AR and ET BR, 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.
Insights
The endothelin (ET) axis promotes tumor growth and spread. Endothelin receptor antagonists show promise for new cancer therapies, potentially combined with existing treatments.
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- The endothelin (ET) axis, comprising ET-1, ET-2, ET-3, and receptors ET A R and ET B R, is implicated in the growth and progression of numerous cancers.
- ET-1 signaling influences key cancer hallmarks including proliferation, survival, angiogenesis, and metastasis.
Purpose of the Study:
- To explore the therapeutic potential of targeting the endothelin axis in cancer.
- To evaluate endothelin receptor antagonists as novel therapeutic strategies.
Main Methods:
- Review of experimental and clinical data on endothelin receptor antagonists.
- Analysis of the role of ET-1 in tumor biology.
Main Results:
- Endothelin receptor antagonists serve as valuable tools for studying the ET axis.
- These antagonists demonstrate potential in developing novel therapeutic strategies for various tumors.
- Interference with endothelin receptors offers opportunities for combinatorial therapies.
Conclusions:
- Targeting the endothelin axis presents a promising avenue for cancer treatment.
- Endothelin receptor antagonists can be integrated into rational combinatorial approaches with chemotherapy or targeted therapies.
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