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Neurochem Res
2014 Oct 01;3910:1906-13. doi: 10.1007/s11064-014-1258-6.
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Inhibition of AMPA receptors by polyamine toxins is regulated by agonist efficacy and stargazin.
Poulsen MH
,
Lucas S
,
Strømgaard K
,
Kristensen AS
.
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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 IC50 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.
Andersen,
Uncompetitive antagonism of AMPA receptors: Mechanistic insights from studies of polyamine toxin derivatives.
2006, Pubmed,
Xenbase
Andersen,
Uncompetitive antagonism of AMPA receptors: Mechanistic insights from studies of polyamine toxin derivatives.
2006,
Pubmed
,
Xenbase
Banke,
Control of GluR1 AMPA receptor function by cAMP-dependent protein kinase.
2000,
Pubmed
Barygin,
Argiotoxin in the closed AMPA receptor channel: experimental and modeling study.
2011,
Pubmed
Bats,
Channel properties reveal differential expression of TARPed and TARPless AMPARs in stargazer neurons.
2012,
Pubmed
Burnashev,
Divalent ion permeability of AMPA receptor channels is dominated by the edited form of a single subunit.
1992,
Pubmed
Bähring,
An analysis of philanthotoxin block for recombinant rat GluR6(Q) glutamate receptor channels.
1998,
Pubmed
Coleman,
Isoform-specific early trafficking of AMPA receptor flip and flop variants.
2006,
Pubmed
Coombs,
Cornichons modify channel properties of recombinant and glial AMPA receptors.
2012,
Pubmed
Derkach,
Ca2+/calmodulin-kinase II enhances channel conductance of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionate type glutamate receptors.
1999,
Pubmed
Geiger,
Relative abundance of subunit mRNAs determines gating and Ca2+ permeability of AMPA receptors in principal neurons and interneurons in rat CNS.
1995,
Pubmed
Herlitze,
Argiotoxin detects molecular differences in AMPA receptor channels.
1993,
Pubmed
,
Xenbase
Hogner,
Structural basis for AMPA receptor activation and ligand selectivity: crystal structures of five agonist complexes with the GluR2 ligand-binding core.
2002,
Pubmed
Huganir,
AMPARs and synaptic plasticity: the last 25 years.
2013,
Pubmed
Jackson,
Stargazing from a new vantage--TARP modulation of AMPA receptor pharmacology.
2011,
Pubmed
Jackson,
The expanding social network of ionotropic glutamate receptors: TARPs and other transmembrane auxiliary subunits.
2011,
Pubmed
Jackson,
Probing TARP modulation of AMPA receptor conductance with polyamine toxins.
2011,
Pubmed
,
Xenbase
Jin,
Structural basis for partial agonist action at ionotropic glutamate receptors.
2003,
Pubmed
,
Xenbase
Koike,
Blocking effect of 1-naphthyl acetyl spermine on Ca(2+)-permeable AMPA receptors in cultured rat hippocampal neurons.
1997,
Pubmed
Kott,
Comparative analysis of the pharmacology of GluR1 in complex with transmembrane AMPA receptor regulatory proteins gamma2, gamma3, gamma4, and gamma8.
2009,
Pubmed
,
Xenbase
Kott,
Electrophysiological properties of AMPA receptors are differentially modulated depending on the associated member of the TARP family.
2007,
Pubmed
,
Xenbase
Kristensen,
Mechanism of Ca2+/calmodulin-dependent kinase II regulation of AMPA receptor gating.
2011,
Pubmed
Kromann,
Solid-phase synthesis of polyamine toxin analogues: potent and selective antagonists of Ca2+-permeable AMPA receptors.
2002,
Pubmed
,
Xenbase
Körber,
Stargazin interaction with alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionate (AMPA) receptors is critically dependent on the amino acid at the narrow constriction of the ion channel.
2007,
Pubmed
,
Xenbase
Lomeli,
Control of kinetic properties of AMPA receptor channels by nuclear RNA editing.
1994,
Pubmed
,
Xenbase
Lucas,
General synthesis of β-alanine-containing spider polyamine toxins and discovery of nephila polyamine toxins 1 and 8 as highly potent inhibitors of ionotropic glutamate receptors.
2012,
Pubmed
Mosbacher,
A molecular determinant for submillisecond desensitization in glutamate receptors.
1994,
Pubmed
,
Xenbase
Nelson,
Synthesis and biological activity of argiotoxin 636 and analogues: selective antagonists for ionotropic glutamate receptors.
2009,
Pubmed
Olsen,
Small molecules from spiders used as chemical probes.
2011,
Pubmed
Poulsen,
Evaluation of PhTX-74 as subtype-selective inhibitor of GluA2-containing AMPA receptors.
2014,
Pubmed
,
Xenbase
Poulsen,
Structure-activity relationship studies of argiotoxins: selective and potent inhibitors of ionotropic glutamate receptors.
2013,
Pubmed
Rosenmund,
The tetrameric structure of a glutamate receptor channel.
1998,
Pubmed
Shelley,
TARP-associated AMPA receptors display an increased maximum channel conductance and multiple kinetically distinct open states.
2012,
Pubmed
Shi,
The stoichiometry of AMPA receptors and TARPs varies by neuronal cell type.
2009,
Pubmed
Smith,
Concentration-dependent substate behavior of native AMPA receptors.
2000,
Pubmed
Sobolevsky,
X-ray structure, symmetry and mechanism of an AMPA-subtype glutamate receptor.
2009,
Pubmed
Sommer,
RNA editing in brain controls a determinant of ion flow in glutamate-gated channels.
1991,
Pubmed
Sommer,
Flip and flop: a cell-specific functional switch in glutamate-operated channels of the CNS.
1990,
Pubmed
Soto,
Stargazin attenuates intracellular polyamine block of calcium-permeable AMPA receptors.
2007,
Pubmed
Swanson,
Single-channel properties of recombinant AMPA receptors depend on RNA editing, splice variation, and subunit composition.
1997,
Pubmed
Tikhonov,
Ion channels of glutamate receptors: structural modeling.
2007,
Pubmed
Tomita,
Stargazin modulates AMPA receptor gating and trafficking by distinct domains.
2005,
Pubmed
,
Xenbase
Traynelis,
Glutamate receptor ion channels: structure, regulation, and function.
2010,
Pubmed
Turetsky,
Stargazin modulates native AMPA receptor functional properties by two distinct mechanisms.
2005,
Pubmed
Verdoorn,
Structural determinants of ion flow through recombinant glutamate receptor channels.
1991,
Pubmed
Washburn,
Block of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors by polyamines and polyamine toxins.
1996,
Pubmed
,
Xenbase
Wollmuth,
Structure and gating of the glutamate receptor ion channel.
2004,
Pubmed
Yan,
Defined criteria for auxiliary subunits of glutamate receptors.
2012,
Pubmed
von Engelhardt,
CKAMP44: a brain-specific protein attenuating short-term synaptic plasticity in the dentate gyrus.
2010,
Pubmed
,
Xenbase
