Stapling of conantokin G 1 Stapling Mimics Noncovalent Interactions of γ-Carboxyglutamates in Conantokins, Peptidic Antagonists of N-Methyl-D-Aspartic Acid (NMDA) Receptors
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چکیده
Background: Can dicarba bridges (stapling) replace non-covalent interactions that stabilize helical conformation of neuroactive peptides? Result: A rational design, synthesis, structural and functional characterization of stapled conG analogs that target NMDA receptors is reported. Conclusion: Stapled conG analogs are potent antagonists of NMDA receptors and anticonvulsant compounds. Significance: Stapling can be successfully applied to convert neuroactive peptides into drug leads.
منابع مشابه
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تاریخ انتشار 2012