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Cover Picture: Structure–Activity Relationship Study of Spider Polyamine Toxins as Inhibitors of Ionotropic Glutamate Receptors (ChemMedChem 12/2014)
Author(s) -
Xiong XiaoFeng,
Poulsen Mette H.,
Hussein Rama A.,
Nørager Niels G.,
Strømgaard Kristian
Publication year - 2014
Publication title -
chemmedchem
Language(s) - English
Resource type - Reports
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201490044
Subject(s) - ionotropic effect , ampa receptor , spider toxin , polyamine , spider , chemistry , receptor , structure–activity relationship , kainate receptor , stereochemistry , nmda receptor , glutamate receptor , biochemistry , biology , ecology , in vitro
The front cover picture shows the structure–activity relationship study of Joro spider polyamine toxins JSTX‐3 (top structure), NPTX‐1 (middle structure) and NPTX‐8 (bottom structure) as inhibitors of inotropic glutamate receptors (iGluRs). Based on the three natural toxins and through newly developed solid‐phase synthetic strategies, a library of 24 analogues was successfully prepared with systematic structural variation. Biological evaluation revealed the importance of each structural region in the toxins, and more importantly, three compounds were found to be both highly potent AMPA receptor antagonists and very selective for this receptor subtype over other iGluRs such as the NMDA receptor. For more details, see the Full Paper by Kristian Strømgaard et al. on p. 2661 ff.