glutamate receptor 1; GluR-1; GluR-A; GluR-K1; glutamate receptor ionotropic, AMPA 1; AMPA-selective glutamate receptor 1 (GRIA1, GLUH1, GLUR1)

Function

• ionotropic glutamate receptor
• role in hippocampal consolidation & reconsolidation of memories
• L-glutamate acts as an excitatory neurotransmitter at many synapses in the central nervous system
• binding of the excitatory neurotransmitter L-glutamate induces a conformation change, leading to the opening of the cation channel, & thereby converts the chemical signal to an electrical impulse
• the receptor then desensitizes rapidly & enters a transient inactive state, characterized by the presence of boundagonist
• palmitoylated, depalmitoylated upon glutamate stimulation
• Cys-603 palmitoylation leads to Golgi retention & decreased cell surface expression
• in contrast, Cys-829 palmitoylation does not affect cell surface expression but regulates stimulation-dependent endocytosis (putative)
• interacts with DLG1 via its C-terminus
• interacts with CACNG2 & RASGRF2 (putative)
• binds AMPA (quisqualate) > glutamate > kainate
• Ser831 & S845 in the C-terminal domain involved in phosphorylation-dependent regulation of activity
• hosphorylation of S831 by CAM kinase 2 or protein kinase C is associated with long-term potentiation
• dephosphorylation* of S845 is associated with long-term depression
• S845 is phosphorylated by protein kinase A

Structure

• homotetramer or heterotetramer of pore-forming glutamate receptor subunits
• tetramers may be formed by the dimerization of dimers
• belongs to the glutamate-gated ion channel (TC 1.A.10) family

Compartment

• cell membrane
• endoplasmic reticulum membrane
• cell junction, synapse, postsynaptic cell membrane
• interaction with CACNG2 promotes cell surface expression (putative)

Alternative splicing

named isoforms=2

Expression

• widely expressed in brain
• together with GluR2 comprise the majority of AMPA receptors in the hippocampus & neocortex.

Notes

• postsynaptic actions of Glu are mediated by a variety of receptors that are named according to their selective agonists

More general terms

• ionotropic receptor subunit

Database

• Kegg: http://www.genome.jp/dbget-bin/www_bget?hsa:2890
• OMIM: https://mirror.omim.org/entry/138248
• UniProt: http://www.uniprot.org/uniprot/P42261.html
• Entrez gene: http://www.ncbi.nlm.nih.gov/sites/entrez?db=gene&cmd=Retrieve&dopt=Graphics&list_uids=2890