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| Content Provider | Springer Nature Link |
|---|---|
| Author | Poulsen, Mette H. Lucas, Simon Strømgaard, Kristian Kristensen, Anders S. |
| Copyright Year | 2014 |
| Abstract | The α-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid receptors (AMPARs) are glutamate-gated cation channels mediating the majority of fast excitatory synaptic transmission in the central nervous system (CNS). Polyamine toxins derived from spiders and wasps are use- and voltage-dependent channel blockers of Ca$^{2+}$-permeable AMPARs. Recent studies have suggested that AMPAR block by polyamine toxins is modulated by auxiliary subunits from the class of transmembrane AMPAR regulatory proteins (TARPs), which may have implications for their use as tool compounds in native systems. We have explored the effect of the TARP γ-2 (also known as stargazin) on the inhibitory potency of three structurally different polyamine toxins at Ca$^{2+}$-permeable homomeric GluA1 AMPARs expressed in oocytes. We find that polyamine toxin IC$_{50}$ is differentially affected by presence of stargazin depending on the efficacy of the agonists used to activate GluA1. Co-assembly of GluA1 receptors with stargazin increases the potency of the polyamine toxins when activated by the weak partial agonist kainate, but has no effect in presence of full-agonist l-glutamate (Glu) and partial agonist (RS)-willardiine. |
| Starting Page | 1906 |
| Ending Page | 1913 |
| Page Count | 8 |
| File Format | |
| ISSN | 03643190 |
| Journal | Neurochemical Research |
| Volume Number | 39 |
| Issue Number | 10 |
| e-ISSN | 15736903 |
| Language | English |
| Publisher | Springer US |
| Publisher Date | 2014-02-22 |
| Publisher Place | Boston |
| Access Restriction | One Nation One Subscription (ONOS) |
| Subject Keyword | Ca$^{2+}$-permeable AMPARs Polyamine toxins Auxiliary subunits Xenopus oocytes Neurosciences Neurochemistry Biochemistry Cell Biology Neurology |
| Content Type | Text |
| Resource Type | Article |
| Subject | Medicine Biochemistry Cellular and Molecular Neuroscience |
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