The Molecular Basis of Conantokin Antagonism of NMDA Receptor Function

Author(s): Mary Prorok, Francis J. Castellino.

Journal Name: Current Drug Targets

Volume 8 , Issue 5 , 2007

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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

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Article Details

VOLUME: 8
ISSUE: 5
Year: 2007
Page: [633 - 642]
Pages: 10
DOI: 10.2174/138945007780618481
Price: $58

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