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
-
Chemokine Receptors as Targets for Cancer Therapy
Current Pharmaceutical Design An Emerging Antiarrhythmic Target: Late Sodium Current
Current Pharmaceutical Design Potentiating the Naturally Occurring Process for Repair of Damaged Heart
Current Pharmaceutical Design Role of Gap Junction Channel in the Development of Beat-to-Beat Action Potential Repolarization Variability and Arrhythmias
Current Pharmaceutical Design New Drugs and Treatment Regimens
Current Respiratory Medicine Reviews L-Type Voltage-Dependent Calcium Channels As Therapeutic Targets for Neurodegenerative Diseases
Current Medicinal Chemistry Clinical Trials Using Vasodilators in Pulmonary Arterial Hypertension:Where Do We Go from Here?
Reviews on Recent Clinical Trials Vascular Effects of Antiarrhythmic Drugs and the Roles of K+ Channels
Current Medicinal Chemistry - Cardiovascular & Hematological Agents Morphological and Molecular Changes of the Myocardium After Left Ventricular Mechanical Support
Current Cardiology Reviews Pompe Disease: From New Views on Pathophysiology to Innovative Therapeutic Strategies
Current Pharmaceutical Biotechnology Neurohormonal Activation in Ischemic Stroke: Effects of Acute Phase Disturbances on Long-Term Mortality
Current Neurovascular Research Intensive Glucose Control in Diabetics with an Acute Myocardial Infarction Does not Improve Mortality and Increases Risk of Hypoglycemia-A Meta-Regression Analysis
Current Vascular Pharmacology Lipids, Statins and Heart Failure: An Update
Current Pharmaceutical Design Endocrine Therapies and QTc Prolongation
Current Drug Safety Standardization of QRS Duration Measurement and LBBB Criteria in CRT Trials and Clinical Practice
Current Cardiology Reviews New Treatments for COPD in the Elderly
Current Pharmaceutical Design Molecular Signals Elicited by GPCR Agonists in Hypertension, Cardiovascular Remodeling: Are MMPs and ADAMs Elusive Therapeutic Targets?
Current Hypertension Reviews High Sensitivity Troponin in Cardiovascular Disease. Is There More Than a Marker of Myocardial Death?
Current Topics in Medicinal Chemistry The Role of microRNAs in Cardiovascular Disease
Current Medicinal Chemistry Ultrasound Guided Central Vascular Access in Neonates, Infants and Children
Current Drug Targets