The importance of two specific domains in ligand binding to the AMPA/kainate glutamate receptors GluR2 and GluR6

FEBS Letters
C K TygesenP H Andersen

Abstract

Chimeric receptor subunits of the AMPA receptor subunit GluR2 and the kainate receptor subunit GluR6 were constructed and stably expressed in baby hamster kidney cells. By using Ca2+ imaging and radioligand binding, we demonstrated that substitution of a specific domain showing homology to a bacterial leucine-isoleucine-valine binding protein (LIVBP) had no effect on the affinities of the tested agonists, but decreased the affinities of the antagonists CNQX, DNQX, and NBQX. On the other hand, when the first of two domains showing homology to a bacterial glutamine binding protein (QBP) in GluR2 was substituted with the corresponding region from GluR6, the affinity of AMPA decreased sevenfold and the affinity of kainate increased fourfold, indicating the importance of this domain in binding of these agonists. In contrast to this, the affinities of quisqualate and domoate, two other agonists, were unchanged, indicating that a region located C-terminal to the QBP domain is also involved in agonist binding.

References

Dec 1, 1977·Proceedings of the National Academy of Sciences of the United States of America·F SangerA R Coulson
Jul 28, 1992·FEBS Letters·H LomeliP H Seeburg
Jun 1, 1992·Annals of Neurology·C D BlackstoneR L Huganir
Oct 31, 1991·Biochemical and Biophysical Research Communications·M MishinaK Nagahari
Nov 7, 1991·Nature·K MoriyoshiS Nakanishi
Aug 3, 1990·Science·K KeinänenP H Seeburg
Jan 1, 1990·Annual Review of Pharmacology and Toxicology·J W Olney
Feb 1, 1989·Proceedings of the National Academy of Sciences of the United States of America·M L Mayer, L Vyklicky
Dec 20, 1994·Proceedings of the National Academy of Sciences of the United States of America·C K TygesenP H Andersen
Jul 19, 1994·Proceedings of the National Academy of Sciences of the United States of America·Z G Wo, R E Oswald
Jan 7, 1993·Nature·T V Bliss, G L Collingridge

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Citations

Nov 27, 2004·Archives of Toxicology·Annamarie RogersD Clive Williams
Sep 5, 1996·European Journal of Pharmacology·P H AndersenC E Stidsen
Feb 13, 2003·Il Farmaco·Laura De LucaRoberto Pellicciari
Dec 16, 1998·Neuropharmacology·D Bleakman, D Lodge
Aug 19, 2010·Pharmacological Reviews·Stephen F TraynelisRay Dingledine
Feb 14, 2006·British Journal of Pharmacology·Philip E Chen, David J A Wyllie
May 11, 2006·The Neuroscientist : a Review Journal Bringing Neurobiology, Neurology and Psychiatry·Mark W Fleck
Feb 14, 2018·ACS Chemical Biology·Shigeki KiyonakaItaru Hamachi

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