Abstract
A series of 30 tripeptides were synthesized and tested as novel 5-HT4 receptor ligands. Receptor binding assays showed that a subset of compounds had reasonable potency relative to the agonists serotonin and 5-methoxytryptamine. Structure-activity analyses and molecular docking have highlighted avenues for further synthetic work.
Keywords: Serotonin, 5-HT, 5-HT4, tripeptide, molecular docking, radioligand binding
Protein & Peptide Letters
Title: The Use of Tripeptides for Lead Discovery of 5-HT4 Receptor Ligands
Volume: 16 Issue: 7
Author(s): A. Hanna-Elias, P. E. Thompson, D. T. Manallack, H. R. Irving, I. M. Coupar, I. Berque-Bestel and M. N. Iskander
Affiliation:
Keywords: Serotonin, 5-HT, 5-HT4, tripeptide, molecular docking, radioligand binding
Abstract: A series of 30 tripeptides were synthesized and tested as novel 5-HT4 receptor ligands. Receptor binding assays showed that a subset of compounds had reasonable potency relative to the agonists serotonin and 5-methoxytryptamine. Structure-activity analyses and molecular docking have highlighted avenues for further synthetic work.
Export Options
About this article
Cite this article as:
Hanna-Elias A., Thompson E. P., Manallack T. D., Irving R. H., Coupar M. I., Berque-Bestel I. and Iskander N. M., The Use of Tripeptides for Lead Discovery of 5-HT4 Receptor Ligands, Protein & Peptide Letters 2009; 16 (7) . https://dx.doi.org/10.2174/092986609788681805
DOI https://dx.doi.org/10.2174/092986609788681805 |
Print ISSN 0929-8665 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5305 |
- 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
Related Articles
-
Synthesis and Cytotoxic Properties of Halogen and Aryl-/Heteroarylpiperazinyl Derivatives of Benzofurans
Anti-Cancer Agents in Medicinal Chemistry Type 1 Diabetes Mellitus - Risk Factor for Cardiovascular Disease Morbidity and Mortality
Current Diabetes Reviews Myocardial Structure and Matrix Metalloproteinases
Current Topics in Medicinal Chemistry Effects of Drug Transporters on Pharmacological Responses and Safety
Current Drug Metabolism Cardiovascular Effects of Phosphodiesterase 5 Inhibitors
Current Pharmaceutical Design Tetracyclic Triterpenoids in Herbal Medicines and their Activities in Diabetes and its Complications
Current Topics in Medicinal Chemistry Vascular Toxicity of Chemotherapeutic Agents
Current Vascular Pharmacology Cardiovascular Drugs and Bone
Current Drug Safety B-Type Natriuretic Peptide: Endogenous Regulator of Myocardial Structure, Biomarker and Therapeutic Target
Current Molecular Medicine QT Dispersion and Age; Independent Predictors of Restenosis after Percutaneous Coronary Intervention
Reviews on Recent Clinical Trials Left Ventricular Hypertrophy in Isolated Aortic Stenosis: Primetime for the Ventricle
Current Pharmaceutical Biotechnology Gene-Wide Approach: New Frontiers in Cardiovascular Genetic Epidemiology
Current Hypertension Reviews The Right Ventricle: Biologic Insights and Response to Disease
Current Cardiology Reviews Anticancer Drug Discovery Targeting DNA Hypermethylation
Current Medicinal Chemistry Pharmacology of Ivabradine and the Effect on Chronic Heart Failure
Current Topics in Medicinal Chemistry The Treatment of Painful Diabetic Neuropathy
Current Diabetes Reviews Mitochondrial Aldehyde Dehydrogenase, A Potential Drug Target for Protection of Heart and Brain from Ischemia/Reperfusion Injury
Current Drug Targets Anti-inflammatory Property of AMP-activated Protein Kinase
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Cardiac Metabolism in Diabetes Mellitus
Current Pharmaceutical Design Nitric Oxide-Derived Oxidants with a Focus on Peroxynitrite: Molecular Targets,Cellular Responses and Therapeutic Implications
Current Pharmaceutical Design