Biomaterial Database

Peptide antagonists of NMDA receptors: Structure-activity relationships for potential therapeutics. 2022

Elsie C Jimenez

Department of Physical Sciences, College of Science, University of the Philippines Baguio, Baguio City 2600, Philippines. Electronic address: ecjimenez@up.edu.ph.

The N-methyl-D-aspartate (NMDA) receptors are heteromeric cation channels involved in memory, learning, and synaptic plasticity. The dysfunction associated with NMDA receptors results in neurodegenerative conditions. The conantokins comprise a family of Conus venom peptides that induce sleep upon intracranial injection into young mice and are known to be NMDA receptor antagonists. This work comprehensibly documents the conantokins that have been characterized to date, focusing on the biochemistry, solution structures in the presence or absence of divalent cations, functions as selective NMDA receptor antagonists, and structure-activity relationships. Furthermore, the applications of conantokins as potential therapeutics for certain neurological conditions, including neuropathic pain, epilepsy, and ischaemia that are linked to NMDA receptor dysfunction are reviewed.

UI	MeSH Term	Description	Entries
D008978	Mollusk Venoms	Venoms from mollusks, including CONUS and OCTOPUS species. The venoms contain proteins, enzymes, choline derivatives, slow-reacting substances, and several characterized polypeptide toxins that affect the nervous system. Mollusk venoms include cephalotoxin, venerupin, maculotoxin, surugatoxin, conotoxins, and murexine.	Conus Venoms,Octopus Venoms,Snail Venoms,Conus Venom,Mollusc Venoms,Mollusk Venom,Octopus Venom,Snail Venom,Venom, Conus,Venom, Mollusk,Venom, Octopus,Venom, Snail,Venoms, Conus,Venoms, Mollusc,Venoms, Mollusk,Venoms, Octopus,Venoms, Snail
D010455	Peptides	Members of the class of compounds composed of AMINO ACIDS joined together by peptide bonds between adjacent amino acids into linear, branched or cyclical structures. OLIGOPEPTIDES are composed of approximately 2-12 amino acids. Polypeptides are composed of approximately 13 or more amino acids. PROTEINS are considered to be larger versions of peptides that can form into complex structures such as ENZYMES and RECEPTORS.	Peptide,Polypeptide,Polypeptides
D000818	Animals	Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA.	Animal,Metazoa,Animalia
D013329	Structure-Activity Relationship	The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups.	Relationship, Structure-Activity,Relationships, Structure-Activity,Structure Activity Relationship,Structure-Activity Relationships
D016194	Receptors, N-Methyl-D-Aspartate	A class of ionotropic glutamate receptors characterized by affinity for N-methyl-D-aspartate. NMDA receptors have an allosteric binding site for glycine which must be occupied for the channel to open efficiently and a site within the channel itself to which magnesium ions bind in a voltage-dependent manner. The positive voltage dependence of channel conductance and the high permeability of the conducting channel to calcium ions (as well as to monovalent cations) are important in excitotoxicity and neuronal plasticity.	N-Methyl-D-Aspartate Receptor,N-Methyl-D-Aspartate Receptors,NMDA Receptor,NMDA Receptor-Ionophore Complex,NMDA Receptors,Receptors, NMDA,N-Methylaspartate Receptors,Receptors, N-Methylaspartate,N Methyl D Aspartate Receptor,N Methyl D Aspartate Receptors,N Methylaspartate Receptors,NMDA Receptor Ionophore Complex,Receptor, N-Methyl-D-Aspartate,Receptor, NMDA,Receptors, N Methyl D Aspartate,Receptors, N Methylaspartate
D051379	Mice	The common name for the genus Mus.	Mice, House,Mus,Mus musculus,Mice, Laboratory,Mouse,Mouse, House,Mouse, Laboratory,Mouse, Swiss,Mus domesticus,Mus musculus domesticus,Swiss Mice,House Mice,House Mouse,Laboratory Mice,Laboratory Mouse,Mice, Swiss,Swiss Mouse,domesticus, Mus musculus
D020916	Conotoxins	Peptide neurotoxins from the marine fish-hunting snails of the genus CONUS. They contain 13 to 29 amino acids which are strongly basic and are highly cross-linked by disulfide bonds. There are three types of conotoxins, omega-, alpha-, and mu-. OMEGA-CONOTOXINS inhibit voltage-activated entry of calcium into the presynaptic membrane and therefore the release of ACETYLCHOLINE. Alpha-conotoxins inhibit the postsynaptic acetylcholine receptor. Mu-conotoxins prevent the generation of muscle action potentials. (From Concise Encyclopedia Biochemistry and Molecular Biology, 3rd ed)	alpha-Conotoxins,mu-Conotoxins,Conotoxin,alpha-Conotoxin,mu-Conotoxin,alpha Conotoxin,alpha Conotoxins,mu Conotoxin,mu Conotoxins