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.
Export Options
About this article
Cite this article as:
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 |
Call for Papers in Thematic Issues
Chemistry Based on Natural Products for Therapeutic Purposes
The development of new pharmaceuticals for a wide range of medical conditions has long relied on the identification of promising natural products (NPs). There are over sixty percent of cancer, infectious illness, and CNS disease medications that include an NP pharmacophore, according to the Food and Drug Administration. Since NP ...read more
Current Trends in Drug Discovery Based on Artificial Intelligence and Computer-Aided Drug Design
Drug development discovery has faced several challenges over the years. In fact, the evolution of classical approaches to modern methods using computational methods, or Computer-Aided Drug Design (CADD), has shown promising and essential results in any drug discovery campaign. Among these methods, molecular docking is one of the most notable ...read more
Drug Discovery in the Age of Artificial Intelligence
In the age of artificial intelligence (AI), we have witnessed a significant boom in AI techniques for drug discovery. AI techniques are increasingly integrated and accelerating the drug discovery process. These developments have not only attracted the attention of academia and industry but also raised important questions regarding the selection ...read more
From Biodiversity to Chemical Diversity: Focus of Flavonoids
Flavonoids are the largest group of polyphenols, plant secondary metabolites arising from the essential aromatic amino acid phenylalanine (or more rarely from tyrosine) via the phenylpropanoid pathway. The flavan nucleus is the basic 15-carbon skeleton of flavonoids (C6-C3-C6), which consists of two phenyl rings (A and B) and a heterocyclic ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Does Brachial Blood Pressure Need to Predict Cardiovascular Outcomes in End Stage Renal Disease? An Update
Current Hypertension Reviews Multifactorial Regulation of GPER Expression in Cancer Cells and Cardiomyocytes
Immunology, Endocrine & Metabolic Agents in Medicinal Chemistry (Discontinued) The Adrenergic System in Gastrointestinal Cancers
Current Cancer Therapy Reviews The Role of Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) in Cardiovascular Homeostasis: A Non-Systematic Literature Review
Current Cardiology Reviews Effects of Aerobic Exercise and Training on Coagulation, Platelet Aggregation, and Plasma Lipids
Vascular Disease Prevention (Discontinued) Therapeutic Role of Methanolic Extract of Ocimum basilicum L. Seeds and its Isolated Compound as Potent Antidiabetic and Antihyperlipidemic Agents
The Natural Products Journal Role of Salt and Potassium in Hypertension and the Associated Organ Damages
Current Hypertension Reviews Folate Status and Depressive Symptoms in Reproductive-Age Women
Current Nutrition & Food Science Omega-3 and Renal Function in Older Adults
Current Pharmaceutical Design Primary Cilia in Tumor Biology: The Primary Cilium as a Therapeutic Target in Cholangiocarcinoma
Current Drug Targets Cell Signaling Mechanisms by which Geniposide Regulates Insulin- Degrading Enzyme Expression in Primary Cortical Neurons
CNS & Neurological Disorders - Drug Targets Impact of Ivabradine on Health-Related Quality of Life of Patients with Ischaemic Chronic Heart Failure
Current Vascular Pharmacology Role of Ox-LDL and LOX-1 in Atherogenesis
Current Medicinal Chemistry Taking Risk Prediction to the Next Level. Advances in Biomarker Research for Atherosclerosis
Current Pharmaceutical Design Pathophysiology and Pharmacologic Treatment of Venous Thromboembolism
Current Drug Targets Association Between the Levels of Circulating Adhesion Molecules and Biopterins in Type-2 Diabetic Normotensive Patients Adhesion Molecules and Biopterins
Endocrine, Metabolic & Immune Disorders - Drug Targets Chemical Constituents of Plants from the Genus Valeriana
Mini-Reviews in Organic Chemistry Hyperglycemia to Nephropathy via Transforming Growth Factor Beta
Current Diabetes Reviews From The Editors Perspective: Unlocking the Secrets to Cell Survival and Longevity
Current Neurovascular Research Adrenomedullin Function in Vascular Endothelial Cells: Insights from Genetic Mouse Models
Current Hypertension Reviews