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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Three-dimensional structure of the ligand-binding core of GluR2 in complex with the agonist (S)-ATPA : implications for receptor subunit selectivity. / Lunn, Marie-Louise; Hogner, Anders; Stensbøl, Tine B; Gouaux, Eric; Egebjerg, Jan; Kastrup, Jette Sandholm Jensen.
In: Journal of Medicinal Chemistry, Vol. 46, No. 5, 27.02.2003, p. 872-5.Research output: Contribution to journal › Journal article › Research › peer-review
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TY - JOUR
T1 - Three-dimensional structure of the ligand-binding core of GluR2 in complex with the agonist (S)-ATPA
T2 - implications for receptor subunit selectivity
AU - Lunn, Marie-Louise
AU - Hogner, Anders
AU - Stensbøl, Tine B
AU - Gouaux, Eric
AU - Egebjerg, Jan
AU - Kastrup, Jette Sandholm Jensen
PY - 2003/2/27
Y1 - 2003/2/27
N2 - 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.
AB - 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.
KW - Binding Sites
KW - Crystallography, X-Ray
KW - Dimerization
KW - Excitatory Amino Acid Agonists
KW - Isoxazoles
KW - Ligands
KW - Models, Molecular
KW - Propionates
KW - Protein Conformation
KW - Protein Subunits
KW - Receptors, AMPA
KW - Stereoisomerism
KW - Zinc
U2 - 10.1021/jm021020+
DO - 10.1021/jm021020+
M3 - Journal article
C2 - 12593667
VL - 46
SP - 872
EP - 875
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
SN - 0022-2623
IS - 5
ER -
ID: 44729638