![conference banner](/images/conference-banner.jpeg)
Abstract
Calcium flow through the ion channel of the N-methyl-D-aspartate receptor (NMDAR) has been implicated as contributing to a variety of neuropathologies. This receptor is a complex heteromeric oligomer consisting of different types of subunits, the nature of which governs its properties, as well as its response to a variety of agonists, antagonists, and other types of inhibitors. A new natural series of NMDAR inhibitors, the conantokins, have been shown to be present in the venoms of snails within the genus, Conus. These agents appear to function by inhibition of the spermine/spermidine stimulation of ion flow through the NMDAR channel. These small peptides (17-27 amino acid residues) are highly processed post-translationally. One such processing event is the vitamin K-dependent gamma-carboxylation of glutamate, resulting in placement of gamma-carboxyglutamic acid residues in these peptides. As a result, these peptides then possess the ability to interact with divalent metal ions and concomitantly u ndergo a conformational alteration. Rational drug design based on the characteristics of these promising peptides requires knowledge of their properties and the manner in which they target the NMDAR. This review summarizes current knowledge in this area.
Keywords: Conantokins, Inhibitors, Ion Flow, NMDAR, Vitamin K dependent gamma carboxylation, Central Nervous System, Clutamate receptor, Polyamine Sites
Current Drug Targets
Title: Conantokins Inhibitors of Ion Flow through the N-Methyl-D-Aspartate Receptor Channels
Volume: 1 Issue: 3
Author(s): Francis J. Castellin and Mary Porok
Affiliation:
Keywords: Conantokins, Inhibitors, Ion Flow, NMDAR, Vitamin K dependent gamma carboxylation, Central Nervous System, Clutamate receptor, Polyamine Sites
Abstract: Calcium flow through the ion channel of the N-methyl-D-aspartate receptor (NMDAR) has been implicated as contributing to a variety of neuropathologies. This receptor is a complex heteromeric oligomer consisting of different types of subunits, the nature of which governs its properties, as well as its response to a variety of agonists, antagonists, and other types of inhibitors. A new natural series of NMDAR inhibitors, the conantokins, have been shown to be present in the venoms of snails within the genus, Conus. These agents appear to function by inhibition of the spermine/spermidine stimulation of ion flow through the NMDAR channel. These small peptides (17-27 amino acid residues) are highly processed post-translationally. One such processing event is the vitamin K-dependent gamma-carboxylation of glutamate, resulting in placement of gamma-carboxyglutamic acid residues in these peptides. As a result, these peptides then possess the ability to interact with divalent metal ions and concomitantly u ndergo a conformational alteration. Rational drug design based on the characteristics of these promising peptides requires knowledge of their properties and the manner in which they target the NMDAR. This review summarizes current knowledge in this area.
Export Options
About this article
Cite this article as:
Castellin J. Francis and Porok Mary, Conantokins Inhibitors of Ion Flow through the N-Methyl-D-Aspartate Receptor Channels, Current Drug Targets 2000; 1 (3) . https://dx.doi.org/10.2174/1389450003349218
DOI https://dx.doi.org/10.2174/1389450003349218 |
Print ISSN 1389-4501 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5592 |
Call for Papers in Thematic Issues
Drug-Targeted Approach with Polymer Nanocomposites for Improved Therapeutics
Polymer nanocomposites have been recognized as an advanced and cutting-edge technique in drug targeting administration. These materials combine the unique features of nanoparticles with the adaptability of polymers to produce highly personalized drug administration devices. Integrating nanoparticles containing pharmaceuticals into a polymer matrix enables researchers to regulate the rates at ...read more
RNA Molecules in the Treatment of Human Diseases
Messenger and non-coding RNAs, including long and small transcripts, are mediators of gene expression. Gene expression at the RNA level shows significant aberrations in human diseases, including cancer, leukemia, lymphoma, cardiovascular diseases, and neurological disorders. Human transcripts serve either as biomarkers of diagnosis, prognosis, prediction of treatment response, and/or therapy ...read more
![Wayfinder Image](/images/wayfinder.jpg)
- 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
-
Book Review: “Dendrites- Third Edition”
CNS & Neurological Disorders - Drug Targets Metabolic Targeting of Cancers: From Molecular Mechanisms to Therapeutic Strategies
Current Medicinal Chemistry The Number of Antiseizure Medications Taken and not the Lipid Profile was Associated with Seizure Control in Adult Patients with Epilepsy
CNS & Neurological Disorders - Drug Targets From Genomic Imprinting to Developmental Physiology: Identifying Stepping Stones
Current Pharmacogenomics Mitochondrial Complex I Deficiency in Humans
Current Genomics Small Interfering RNAs and Antisense Oligonucleotides for Treatment of Neurological Diseases
Current Drug Targets Current Status of Epigenetics and Anticancer Drug Discovery
Anti-Cancer Agents in Medicinal Chemistry Considering New and Emerging Treatment Strategies for Depression: Beyond STAR*D and the Monoamines
Current Psychiatry Research and Reviews Antitumor Potential and Possible Targets of Phenothiazine-Related Compounds
Current Drug Targets Antiepileptic Drugs for the Treatment of Impulsivity
Current Psychiatry Reviews Asymmetric Dimethylarginine: Clinical Significance and Novel Therapeutic Approaches
Current Medicinal Chemistry Cannabinoids
Current Drug Targets - CNS & Neurological Disorders Lipid Nanocarriers for Neurotherapeutics: Introduction, Challenges, Blood-brain Barrier, and Promises of Delivery Approaches
CNS & Neurological Disorders - Drug Targets Mechanism of <i>Polygala-Acorus</i> in Treating Autism Spectrum Disorder Based on Network Pharmacology and Molecular Docking
Current Computer-Aided Drug Design Targeting TRPs in Neurodegenerative Disorders
Current Topics in Medicinal Chemistry Review of Treatment for Cocaine Dependence
Current Drug Abuse Reviews Targeted Blockade of TARP-γ8-Associated AMPA Receptors: Anticonvulsant Activity with the Selective Antagonist LY3130481 (CERC-611)
CNS & Neurological Disorders - Drug Targets Inborn Errors of Metabolism Screening in Neonates: Current Perspective with Diagnosis and Therapy
Current Pediatric Reviews Synthesis and Anticonvulsant Activity of N-(trans)- 3-phenylprop-2-en-1-yl (Cinnamyl) Derivatives of Aminoalkanols
Letters in Drug Design & Discovery Telmisartan Promotes Potential Glucose Homeostasis in Stroke-Resistant Spontaneously Hypertensive Rats via Peroxisome Proliferator-Activated Receptor γ Activation
Current Neurovascular Research