Structure-Function Relationships of the NMDA Receptor Antagonist Conantokin Peptides

Title: Structure-Function Relationships of the NMDA Receptor Antagonist Conantokin Peptides

Volume: 2 Issue: 3

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

Affiliation:

Keywords: NMDA Receptor Antagonist, Conantokin Peptides, progressive C-terminal truncations, N-terminal residues, con-T-based peptide

Abstract: The three members of the conantokin peptide family identified to date are conantokin(con)-G, -T and -R. Their defining attributes include a high relative content of gama-carboxyglutamic acid (Gla), N-terminal sequence identity, as well as considerable overall sequence homology, and antagonism of the N-methyl-D-aspartate receptor (NMDAR). As promising templates for the design of neuroprotective agents, a thorough evaluation of structure-function relationships in these peptides will be invaluable in aiding rational drug modeling. To this end, a comprehensive assessment of the contributions of individual residues to conantokin structure and function is required. The current review summarizes recent efforts in this area, and also includes the effects of peptide length, as well as structural-stabilization and -destabilization on the structural and inhibitory profiles of an extensive panel of conantokin derivatives.

Cite this article as:

Prorok Mary and Castellino J. Francis, Structure-Function Relationships of the NMDA Receptor Antagonist Conantokin Peptides, Current Drug Targets 2001; 2 (3) . https://dx.doi.org/10.2174/1389450013348542