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Title
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Three-dimensional structure of the ligand-binding core of GluR2 in complex with the agonist (S)-ATPA: implications for receptor subunit selectivity.
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Authors
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M.L.Lunn,
A.Hogner,
T.B.Stensbøl,
E.Gouaux,
J.Egebjerg,
J.S.Kastrup.
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Ref.
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J Med Chem, 2003,
46,
872-875.
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PubMed id
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Abstract
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Two X-ray structures of the GluR2 ligand-binding core in complex with
(S)-2-amino-3-(5-tert-butyl-3-hydroxy-4-isoxazolyl)propionic acid ((S)-ATPA)
have been determined with and without Zn(2+) ions. (S)-ATPA induces a domain
closure of ca. 21 degrees compared to the apo form. The tert-butyl moiety of
(S)-ATPA is buried in a partially hydrophobic pocket and forces the ligand into
the glutamate-like binding mode. The structures provide new insight into the
molecular basis of agonist selectivity between AMPA and kainate receptors.
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