Abstract
Since its identification in 1988 and the recognition of its primary role as a potent vasoconstrictor, endothelin has been extensively studied and is now considered as a ubiquitous protein, involved in important aspects of human homeostasis as well as in several pathophysiological pathways, mostly associated with cardiovascular disease. From an evolutionary point of view, endothelin consists a primitive molecule with the rare characteristic of being exactly the same in all mammals, thus permitting scientists to perform experiments in animals and doing predictions for humans. The understanding of its contribution to the genesis, evolution and maintenance of disease through activation of special receptor subtypes has led to the development of both selective and unselective receptor antagonists. Despite the disappointing results of these antagonists in the field of heart failure, almost from the initial animal trials of bosentan, a dual endothelin receptor antagonist, in pulmonary arterial hypertension, it has been demonstrated that the drug leads at least to hemodynamic and clinical improvement of the patients, thus receiving official approval for the management of this rare but eventually lethal disease. Resistant hypertension is another area where endothelin receptor blockers might potentially play a role, while the pathophysiological role of endothelin in atherosclerotic coronary artery disease is well-established and the relative research goes on. The main goal of this review is to describe the endothelin system and mostly to enlighten its role in pathophysiologic pathways, as well to state the relative research in the various fields of cardiovascular disease and also highlight its prognostic significance wherever there exists one.
Keywords: Arterial hypertension, atherosclerosis, bosentan, cardiovascular disease, coronary artery disease, endothelin, heart failure, pulmonary hypertension
Current Topics in Medicinal Chemistry
Title:The Role of Endothelin System in Cardiovascular Disease and the Potential Therapeutic Perspectives of its Inhibition
Volume: 13 Issue: 2
Author(s): Andreas Kaoukis, Spyridon Deftereos, Konstantinos Raisakis, Georgios Giannopoulos, Georgios Bouras, Vasiliki Panagopoulou, Nikolaos Papoutsidakis, Michael W. Cleman and Christodoulos Stefanadis
Affiliation:
Keywords: Arterial hypertension, atherosclerosis, bosentan, cardiovascular disease, coronary artery disease, endothelin, heart failure, pulmonary hypertension
Abstract: Since its identification in 1988 and the recognition of its primary role as a potent vasoconstrictor, endothelin has been extensively studied and is now considered as a ubiquitous protein, involved in important aspects of human homeostasis as well as in several pathophysiological pathways, mostly associated with cardiovascular disease. From an evolutionary point of view, endothelin consists a primitive molecule with the rare characteristic of being exactly the same in all mammals, thus permitting scientists to perform experiments in animals and doing predictions for humans. The understanding of its contribution to the genesis, evolution and maintenance of disease through activation of special receptor subtypes has led to the development of both selective and unselective receptor antagonists. Despite the disappointing results of these antagonists in the field of heart failure, almost from the initial animal trials of bosentan, a dual endothelin receptor antagonist, in pulmonary arterial hypertension, it has been demonstrated that the drug leads at least to hemodynamic and clinical improvement of the patients, thus receiving official approval for the management of this rare but eventually lethal disease. Resistant hypertension is another area where endothelin receptor blockers might potentially play a role, while the pathophysiological role of endothelin in atherosclerotic coronary artery disease is well-established and the relative research goes on. The main goal of this review is to describe the endothelin system and mostly to enlighten its role in pathophysiologic pathways, as well to state the relative research in the various fields of cardiovascular disease and also highlight its prognostic significance wherever there exists one.
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Kaoukis Andreas, Deftereos Spyridon, Raisakis Konstantinos, Giannopoulos Georgios, Bouras Georgios, Panagopoulou Vasiliki, Papoutsidakis Nikolaos, W. Cleman Michael and Stefanadis Christodoulos, The Role of Endothelin System in Cardiovascular Disease and the Potential Therapeutic Perspectives of its Inhibition, Current Topics in Medicinal Chemistry 2013; 13 (2) . https://dx.doi.org/10.2174/1568026611313020003
DOI https://dx.doi.org/10.2174/1568026611313020003 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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