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Endothelin receptors as novel targets in tumor therapy
The endotelin (ET) axis, that includes ET-1, ET-2, ET-3, and the ET receptors, ET(A )and ET(B), plays an important physiological role, as modulator of vasomotor tone, tissue differentiation and development, cell proliferation, and hormone production. Recently, investigations into the role of the ET...
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Formato: | Texto |
Lenguaje: | English |
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BioMed Central
2004
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Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC436068/ https://www.ncbi.nlm.nih.gov/pubmed/15165288 http://dx.doi.org/10.1186/1479-5876-2-16 |
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author | Bagnato, Anna Natali, Pier Giorgio |
author_facet | Bagnato, Anna Natali, Pier Giorgio |
author_sort | Bagnato, Anna |
collection | PubMed |
description | The endotelin (ET) axis, that includes ET-1, ET-2, ET-3, and the ET receptors, ET(A )and ET(B), plays an important physiological role, as modulator of vasomotor tone, tissue differentiation and development, cell proliferation, and hormone production. Recently, investigations into the role of the ET axis in mitogenesis, apoptosis inhibition, invasiveness, angiogenesis and bone remodeling have provided evidence of the importance of the ET-1 axis in cancer. Data suggest that ET-1 participates in the growth and progression of a variety of tumors such as prostatic, ovarian, renal, pulmonary, colorectal, cervical, breast carcinoma, Kaposi's sarcoma, brain tumors, melanoma, and bone metastases. ET-1 receptor antagonists beside providing ideal tools for dissecting the ET axis at molecular level have demonstrated their potential in developing novel therapeutic opportunity. The major relevance of ET(A )receptor in tumor development has led to an extensive search of highly selective antagonists. Atrasentan, one of such antagonists, is orally bioavailable, has suitable pharmacokinetic and toxicity profiles for clinical use. Preliminary data from clinical trials investigating atrasentan in patients with prostate cancer are encouraging. This large body of evidence demonstrates the antitumor activity of endothelin receptor antagonists and provides a rationale for the clinical evaluation of these molecules alone and in combination with cytotoxic drugs or molecular inhibitors leading to a new generation of anticancer therapies targeting endothelin receptors. |
format | Text |
id | pubmed-436068 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2004 |
publisher | BioMed Central |
record_format | MEDLINE/PubMed |
spelling | pubmed-4360682004-06-26 Endothelin receptors as novel targets in tumor therapy Bagnato, Anna Natali, Pier Giorgio J Transl Med Review The endotelin (ET) axis, that includes ET-1, ET-2, ET-3, and the ET receptors, ET(A )and ET(B), plays an important physiological role, as modulator of vasomotor tone, tissue differentiation and development, cell proliferation, and hormone production. Recently, investigations into the role of the ET axis in mitogenesis, apoptosis inhibition, invasiveness, angiogenesis and bone remodeling have provided evidence of the importance of the ET-1 axis in cancer. Data suggest that ET-1 participates in the growth and progression of a variety of tumors such as prostatic, ovarian, renal, pulmonary, colorectal, cervical, breast carcinoma, Kaposi's sarcoma, brain tumors, melanoma, and bone metastases. ET-1 receptor antagonists beside providing ideal tools for dissecting the ET axis at molecular level have demonstrated their potential in developing novel therapeutic opportunity. The major relevance of ET(A )receptor in tumor development has led to an extensive search of highly selective antagonists. Atrasentan, one of such antagonists, is orally bioavailable, has suitable pharmacokinetic and toxicity profiles for clinical use. Preliminary data from clinical trials investigating atrasentan in patients with prostate cancer are encouraging. This large body of evidence demonstrates the antitumor activity of endothelin receptor antagonists and provides a rationale for the clinical evaluation of these molecules alone and in combination with cytotoxic drugs or molecular inhibitors leading to a new generation of anticancer therapies targeting endothelin receptors. BioMed Central 2004-05-27 /pmc/articles/PMC436068/ /pubmed/15165288 http://dx.doi.org/10.1186/1479-5876-2-16 Text en Copyright © 2004 Bagnato and Natali; licensee BioMed Central Ltd. This is an Open Access article: verbatim copying and redistribution of this article are permitted in all media for any purpose, provided this notice is preserved along with the article's original URL. |
spellingShingle | Review Bagnato, Anna Natali, Pier Giorgio Endothelin receptors as novel targets in tumor therapy |
title | Endothelin receptors as novel targets in tumor therapy |
title_full | Endothelin receptors as novel targets in tumor therapy |
title_fullStr | Endothelin receptors as novel targets in tumor therapy |
title_full_unstemmed | Endothelin receptors as novel targets in tumor therapy |
title_short | Endothelin receptors as novel targets in tumor therapy |
title_sort | endothelin receptors as novel targets in tumor therapy |
topic | Review |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC436068/ https://www.ncbi.nlm.nih.gov/pubmed/15165288 http://dx.doi.org/10.1186/1479-5876-2-16 |
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