The Molecular Basis of Conantokin Antagonism of NMDA Receptor Function

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.

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