Abstract
The N-methyl-D-aspartate receptor (NMDAR), a subtype of ionotropic glutamate receptor, has been implicated in a host of chronic and acute neurological disorders. Accordingly, much emphasis has been placed on the development of safe and effective therapeutic agents that specifically antagonize this target. The conantokins are a class of small, naturally occurring peptides that inhibit ion flow through the NMDAR. Some conantokins demonstrate receptor subunit selectivity, a pharmacological attribute of emerging importance in the search for suitable drug candidates. The current review summarizes the NMDAR inhibitory properties of the conantokins, including structure-function relationships and mechanism of action. This information is fundamental to the rational design of suitable agents that can effectively treat pathophysiologies linked to NMDAR dysfunction.
Keywords: ionotropic glutamate receptors, NR1 exons, long-term potentiation, Conantokin Inhibition, NMDAR antagonists
Current Drug Targets
Title: The Molecular Basis of Conantokin Antagonism of NMDA Receptor Function
Volume: 8 Issue: 5
Author(s): Mary Prorok and Francis J. Castellino
Affiliation:
Keywords: ionotropic glutamate receptors, NR1 exons, long-term potentiation, Conantokin Inhibition, NMDAR antagonists
Abstract: The N-methyl-D-aspartate receptor (NMDAR), a subtype of ionotropic glutamate receptor, has been implicated in a host of chronic and acute neurological disorders. Accordingly, much emphasis has been placed on the development of safe and effective therapeutic agents that specifically antagonize this target. The conantokins are a class of small, naturally occurring peptides that inhibit ion flow through the NMDAR. Some conantokins demonstrate receptor subunit selectivity, a pharmacological attribute of emerging importance in the search for suitable drug candidates. The current review summarizes the NMDAR inhibitory properties of the conantokins, including structure-function relationships and mechanism of action. This information is fundamental to the rational design of suitable agents that can effectively treat pathophysiologies linked to NMDAR dysfunction.
Export Options
About this article
Cite this article as:
Prorok Mary and Castellino J. Francis, The Molecular Basis of Conantokin Antagonism of NMDA Receptor Function, Current Drug Targets 2007; 8 (5) . https://dx.doi.org/10.2174/138945007780618481
DOI https://dx.doi.org/10.2174/138945007780618481 |
Print ISSN 1389-4501 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5592 |
Call for Papers in Thematic Issues
New drug therapy for eye diseases
Eyesight is one of the most critical senses, accounting for over 80% of our perceptions. Our quality of life might be significantly affected by eye disease, including glaucoma, diabetic retinopathy, dry eye, etc. Although the development of microinvasive ocular surgery reduces surgical complications and improves overall outcomes, medication therapy is ...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
Related Articles
-
Transglutaminase Inhibition as a Possible Therapeutical Approach to Protect Cells from Death in Neurodegenerative Diseases
Recent Patents on CNS Drug Discovery (Discontinued) Combating Diseases with Computational Strategies Used for Drug Design and Discovery
Current Topics in Medicinal Chemistry Experimental Treatment Options in Absence Epilepsy
Current Pharmaceutical Design High Throughput Electrophysiology with Xenopus Oocytes
Combinatorial Chemistry & High Throughput Screening Treatment Options in Alzheimer´s Disease: The GABA Story
Current Pharmaceutical Design Neural Stem Cell Niches in Health and Diseases
Current Pharmaceutical Design Development and Validation of a Fluorescence-Based HTS Assay for the Identification of P/Q-Type Calcium Channel Blockers
Combinatorial Chemistry & High Throughput Screening Biological Drugs in Guillain-Barré Syndrome: An Update
Current Neuropharmacology The Place of Somatostatin Analogs in the Diagnosis and Treatment of the Neuoroendocrine Glands Tumors
Recent Patents on Anti-Cancer Drug Discovery Ectonucleotidases and Nucleotide/Nucleoside Transporters as Pharmacological Targets for Neurological Disorders
CNS & Neurological Disorders - Drug Targets The Progress Towards the Development of DHQO Derivatives and Related Analogues with Inotropic Effects
Mini-Reviews in Medicinal Chemistry Importance of ABC Transporters in Drug Development
Current Pharmaceutical Design Complexities of Glucuronidation Affecting In Vitro-In Vivo Extrapolation
Current Drug Metabolism Formulation of Extended-Release Beads of Lamotrigine Based on Alginate and <i>Cassia fistula</i> Seed Gum by QbD Approach
Current Drug Delivery Aligning Animal Models of Clinical Germinal Matrix Hemorrhage, From Basic Correlation to Therapeutic Approach
Current Drug Targets Augmentation of Citalopram with Aspirin for Treating Major Depressive Disorder, a Double Blind Randomized Placebo Controlled Clinical Trial
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Meet the Editorial Board Member
CNS & Neurological Disorders - Drug Targets Lamotrigine Pharmacokinetics During Anticonception and Pregnancy
Letters in Drug Design & Discovery Voltage-Gated Sodium Channels: Mutations, Channelopathies and Targets
Current Medicinal Chemistry Therapeutic Role of Zonisamide in Neuropsychiatric Disorders
Mini-Reviews in Medicinal Chemistry