caa a22 4500 378911260 CHVBK 20180305123542.0 cr unu---uuuuu 161128e20040101xx s 000 0 eng 10.1351/pac200476050921 doi (NATIONALLICENCE)gruyter-10.1351/pac200476050921 Structural basis for 2-amino-3-(3-hydroxy-5-methyl-4-isoxazolyl)propionic acid (AMPA) receptor activation [Elektronische Daten] [T. N. Johansen, J. R. Greenwood, S. B. Vogensen, Povl Krogsgaard-Larsen] (S)-Glutamic acid (Glu), the major excitatory neurotransmitter in the central nervous system, operates through ionotropic as well as metabotropic receptors and is considered to be involved in a number of degenerative brain diseases that are currently without any satisfactory therapeutic treatment. Until recently, development of selective Glu receptor agonists had mainly been based on structural optimization of naturally occurring lead compounds structurally related to Glu. Crystallization of the agonist binding domain of the GluR2 subunit of the 2-amino-3-(3-hydroxy-5-methyl-4-isoxazolyl)propionic acid (AMPA) receptor subtype of ionotropic Glu receptors (iGluRs) in the presence or absence of an agonist has provided important information about ligand-receptor interaction mechanisms. The availability of such binding domain crystal structures has formed the basis for rational design of ligands, especially for the AMPA subtypes of iGluRs. © 2013 Walter de Gruyter GmbH, Berlin/Boston Johansen T. N. Department of Medicinal Chemistry, The Danish University of Pharmaceutical Sciences, Universitetsparken 2, DK-2100, Copenhagen, Denmark aut Greenwood J. R. Department of Medicinal Chemistry, The Danish University of Pharmaceutical Sciences, Universitetsparken 2, DK-2100, Copenhagen, Denmark aut Vogensen S. B. Department of Medicinal Chemistry, The Danish University of Pharmaceutical Sciences, Universitetsparken 2, DK-2100, Copenhagen, Denmark aut Krogsgaard-Larsen Povl Department of Medicinal Chemistry, The Danish University of Pharmaceutical Sciences, Universitetsparken 2, DK-2100, Copenhagen, Denmark aut Pure and Applied Chemistry De Gruyter 76/5(2004-01-01), 921-930 0033-4545 76:5<921 2004 76 pac https://doi.org/10.1351/pac200476050921 text/html Onlinezugriff via DOI 1 research article jats NATIONALLICENCE 856 40 https://doi.org/10.1351/pac200476050921 text/html Onlinezugriff via DOI NATIONALLICENCE 700 1- Johansen T. N. Department of Medicinal Chemistry, The Danish University of Pharmaceutical Sciences, Universitetsparken 2, DK-2100, Copenhagen, Denmark aut NATIONALLICENCE 700 1- Greenwood J. R. Department of Medicinal Chemistry, The Danish University of Pharmaceutical Sciences, Universitetsparken 2, DK-2100, Copenhagen, Denmark aut NATIONALLICENCE 700 1- Vogensen S. B. Department of Medicinal Chemistry, The Danish University of Pharmaceutical Sciences, Universitetsparken 2, DK-2100, Copenhagen, Denmark aut NATIONALLICENCE 700 1- Krogsgaard-Larsen Povl Department of Medicinal Chemistry, The Danish University of Pharmaceutical Sciences, Universitetsparken 2, DK-2100, Copenhagen, Denmark aut NATIONALLICENCE 773 0- Pure and Applied Chemistry De Gruyter 76/5(2004-01-01), 921-930 0033-4545 76:5<921 2004 76 pac CC0 http://creativecommons.org/publicdomain/zero/1.0 nationallicence BK010053 XK010053 XK010000 NATIONALLICENCE NATIONALLICENCE NL-gruyter