Abstract
Angiotensin II (AII), Asp1-Arg2-Val3-Tyr4-Ile5-His6-Pro7-Phe8, the primary active hormone of the Renin- Angiotensin-System (RAS), is a major vasoconstrictor implicated in the cause of hypertension. To unravel the question of the biologically active conformation(s) of this flexible peptide hormone and to better understand the stereoelectronic requirements that lead to the molecular basis of hypertension, we will analyze research efforts in the identification of pharmacophoric groups of AII and three general approaches for structural characterisation: the free peptide - ligand approach, the receptor based approach, and approaches that target the peptide - receptor complex. The free peptide - ligand based approach can be further categorized to: (a) conformational analysis of AII and linear peptide analogues in aqueous solution; (b) the use of solvents of medium dielectric constants; (c) conformationally restricted analogues, with emphasis to cyclic analogues; (d) the use of receptor - simulating environments, and (e) non-peptide mimetics. The receptor and peptide - receptor based approaches can be categorised to: (a) The use of monoclonal antibodies and (b) the generic description of AII receptor sites through homology modelling and mutagenesis studies. These investigations, with particular emphasis to recent developments, have greatly assisted in the identification of pharmacophoric groups for receptor activation and the development of several models of AII - receptor complexes.
Keywords: Angiotensin II, monoclonal antibodies, pharmacophoric
Current Topics in Medicinal Chemistry
Title: On the Structural Basis of the Hypertensive Properties of Angiotensin II: A Solved Mystery or a Controversial Issue?
Volume: 4 Issue: 4
Author(s): Andreas G. Tzakos, Ioannis P. Gerothanassis and Anastassios N. Troganis
Affiliation:
Keywords: Angiotensin II, monoclonal antibodies, pharmacophoric
Abstract: Angiotensin II (AII), Asp1-Arg2-Val3-Tyr4-Ile5-His6-Pro7-Phe8, the primary active hormone of the Renin- Angiotensin-System (RAS), is a major vasoconstrictor implicated in the cause of hypertension. To unravel the question of the biologically active conformation(s) of this flexible peptide hormone and to better understand the stereoelectronic requirements that lead to the molecular basis of hypertension, we will analyze research efforts in the identification of pharmacophoric groups of AII and three general approaches for structural characterisation: the free peptide - ligand approach, the receptor based approach, and approaches that target the peptide - receptor complex. The free peptide - ligand based approach can be further categorized to: (a) conformational analysis of AII and linear peptide analogues in aqueous solution; (b) the use of solvents of medium dielectric constants; (c) conformationally restricted analogues, with emphasis to cyclic analogues; (d) the use of receptor - simulating environments, and (e) non-peptide mimetics. The receptor and peptide - receptor based approaches can be categorised to: (a) The use of monoclonal antibodies and (b) the generic description of AII receptor sites through homology modelling and mutagenesis studies. These investigations, with particular emphasis to recent developments, have greatly assisted in the identification of pharmacophoric groups for receptor activation and the development of several models of AII - receptor complexes.
Export Options
About this article
Cite this article as:
Tzakos G. Andreas, Gerothanassis P. Ioannis and Troganis N. Anastassios, On the Structural Basis of the Hypertensive Properties of Angiotensin II: A Solved Mystery or a Controversial Issue?, Current Topics in Medicinal Chemistry 2004; 4 (4) . https://dx.doi.org/10.2174/1568026043451375
DOI https://dx.doi.org/10.2174/1568026043451375 |
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
-
Granulocyte Colony-stimulating Factor and Bone Marrow Mononuclear Cells for Stroke Treatment in the Aged Brain
Current Neurovascular Research Treating Older HIV-1-infected Subjects With Cobicistat-boosted Darunavir in a 48-week Phase 3 Trial
Reviews on Recent Clinical Trials Antioxidant Activity of Two Wild Edible Mushrooms (Morchella vulgaris and Morchella esculanta) from North Turkey
Combinatorial Chemistry & High Throughput Screening Characterization and Antihypertensive Effect of the Complex of (-)-β- pinene in β-cyclodextrin
Current Pharmaceutical Biotechnology Ambulatory Blood Pressure Monitoring in Type 2 Diabetes Mellitus: A Cross-sectional Study
Current Hypertension Reviews History and Therapeutic Use of MAO-A Inhibitors: A Historical Perspective of MAO-A Inhibitors As Antidepressant Drug
Current Topics in Medicinal Chemistry Red Wine, Arterial Stiffness and Central Hemodynamics
Current Pharmaceutical Design Medical Complications of Binge Eating Disorder
Current Women`s Health Reviews PAI-1 Antagonists: Predictable Indications and Unconventional Applications
Current Drug Targets Non Smoking for Successful Aging: Therapeutic Perspectives
Current Pharmaceutical Design Modulators of Vascular Sex Hormone Receptors and their Effects in Estrogen-Deficiency States Associated with Menopause
Recent Patents on Cardiovascular Drug Discovery Production and Purification of Functional Lipids Through Enzymatic and Microorganism-Mediated Processes
Current Organic Chemistry Endothelial Function Assessment in Complicated Hypertension
Current Pharmaceutical Design Omentin: Linking Metabolic Syndrome and Cardiovascular Disease
Current Vascular Pharmacology Atrial Fibrillation: The Emerging Role of Inflammation and Oxidative Stress
Cardiovascular & Hematological Disorders-Drug Targets Antioxidant Treatment and Endothelial Dysfunction: Is it Time for Flavonoids?
Recent Patents on Cardiovascular Drug Discovery The use of Sildenafil in the Treatment of Persistent Pulmonary Hypertension of the Newborn: A Review of the Literature
Current Pharmaceutical Design Patent Annotations
Recent Patents on Cardiovascular Drug Discovery Targeting Angiogenesis in Gastro-Intestinal Non Colorectal Cancers; A Review
Current Angiogenesis (Discontinued) Formulation Development and Characterization of Controlled Release Core-in-cup Matrix Tablets of Venlafaxine HCl
Current Drug Therapy