Three-dimensional structure of the ligand-binding core of GluR2 in complex with the agonist (S)-ATPA: implications for receptor subunit selectivity

Research output: Contribution to journalJournal articleResearchpeer-review

Standard

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 journalJournal articleResearchpeer-review

Harvard

Lunn, M-L, Hogner, A, Stensbøl, TB, Gouaux, E, Egebjerg, J & Kastrup, JSJ 2003, 'Three-dimensional structure of the ligand-binding core of GluR2 in complex with the agonist (S)-ATPA: implications for receptor subunit selectivity', Journal of Medicinal Chemistry, vol. 46, no. 5, pp. 872-5. https://doi.org/10.1021/jm021020+

APA

Lunn, M-L., Hogner, A., Stensbøl, T. B., Gouaux, E., Egebjerg, J., & Kastrup, J. S. J. (2003). Three-dimensional structure of the ligand-binding core of GluR2 in complex with the agonist (S)-ATPA: implications for receptor subunit selectivity. Journal of Medicinal Chemistry, 46(5), 872-5. https://doi.org/10.1021/jm021020+

Vancouver

Lunn M-L, Hogner A, Stensbøl TB, Gouaux E, Egebjerg J, Kastrup JSJ. Three-dimensional structure of the ligand-binding core of GluR2 in complex with the agonist (S)-ATPA: implications for receptor subunit selectivity. Journal of Medicinal Chemistry. 2003 Feb 27;46(5):872-5. https://doi.org/10.1021/jm021020+

Author

Lunn, Marie-Louise ; Hogner, Anders ; Stensbøl, Tine B ; Gouaux, Eric ; Egebjerg, Jan ; Kastrup, Jette Sandholm Jensen. / Three-dimensional structure of the ligand-binding core of GluR2 in complex with the agonist (S)-ATPA : implications for receptor subunit selectivity. In: Journal of Medicinal Chemistry. 2003 ; Vol. 46, No. 5. pp. 872-5.

Bibtex

@article{5a425b6004c8429fa5396f8774130c56,
title = "Three-dimensional structure of the ligand-binding core of GluR2 in complex with the agonist (S)-ATPA: implications for receptor subunit selectivity",
abstract = "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.",
keywords = "Binding Sites, Crystallography, X-Ray, Dimerization, Excitatory Amino Acid Agonists, Isoxazoles, Ligands, Models, Molecular, Propionates, Protein Conformation, Protein Subunits, Receptors, AMPA, Stereoisomerism, Zinc",
author = "Marie-Louise Lunn and Anders Hogner and Stensb{\o}l, {Tine B} and Eric Gouaux and Jan Egebjerg and Kastrup, {Jette Sandholm Jensen}",
year = "2003",
month = "2",
day = "27",
doi = "10.1021/jm021020+",
language = "English",
volume = "46",
pages = "872--5",
journal = "Journal of Medicinal Chemistry",
issn = "0022-2623",
publisher = "American Chemical Society",
number = "5",

}

RIS

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