Stapling mimics noncovalent interactions of γ-carboxyglutamates in conantokins, peptidic antagonists of N-methyl-D-aspartic acid receptors

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Publication Type Journal Article
School or College College of Science
Department Biology
Creator Olivera, Baldomero M.
Other Author Platt, Randall J.; Han, Tiffany S.; Green, Brad R.; Smith, Misty D.; Skalicky, Jack; Gruszczyński, Pawel; White, H. Steve; Bulaj, Grzegorz; Gajewiak, Joanna
Title Stapling mimics noncovalent interactions of γ-carboxyglutamates in conantokins, peptidic antagonists of N-methyl-D-aspartic acid receptors
Date 2012-01-01
Description Background: Can dicarba bridges (stapling) replace noncovalent interactions that stabilize helical conformation of neuroactivepeptides? Results: A rational design, synthesis, structural, and functional characterization of stapled conG analogs that target NMDAreceptors 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.
Type Text
Publisher American Soc. for Biochemistry and Molecular Biology (ASBMB)
Volume 287
Issue 24
First Page 20727
Last Page 20736
Dissertation Institution University of Utah
Language eng
Bibliographic Citation Platt, R. J., Han, T. S., Green, B. R., Smith, M. D., Skalicky, J., Gruszczyński, P., White, H. S., Olivera, B., Bulaj, G., & Gajewiak, J. (2012). Stapling mimics noncovalent interactions of γ-carboxyglutamates in conantokins, peptidic antagonists of N-methyl-D-aspartic acid receptors. Journal of Biological Chemistry, 287(24), 20727-36.
Rights Management (c)American Society for Biochemistry and Molecular Biology (ASBMB) http://www.asbmb.org/
Format Medium application/pdf
Format Extent 463,045 bytes
Identifier uspace,17534
ARK ark:/87278/s6kh162q
Setname ir_uspace
ID 708046
Reference URL https://collections.lib.utah.edu/ark:/87278/s6kh162q
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