PHAR 562 Lecture Notes - Lecture 2: Glioblastoma Multiforme, Nmda Receptor, Neuropathic Pain
12 Feb 2020
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Ionotropic glutamate receptors and their synapses: ampa and nmda diversity. Reminder: all drugs have targeted & off target effects: when studying, always focus on where drugs bind. There are 3 types of iglurs: nmdar. Involved in learning and memory, important for plasticity. Numbers are upregulated and downregulated during synaptic plasticity. Not life-threatening is blocked, though to act as a fine-tuner. All receptors have 3 domains: amino-terminal domain, ligand binding domain. Alpha-helix structure since it"s the most efficient energy wise. Orphan class of glu receptor: their functions are not known. Important: there is asymmetry in each subunit (red vs blue), it allows for interaction between the subunits. Structure: tetramers composed of a combination of 4 subunits. Glua4: subunits are synthesized in the endoplasmic reticulum, then assembled in two stages: dimerization followed by tetramerization. Dimerization: formation of heteromeric dimers is favoured, but homomeric dimers are also allowed. Tetramerization: this results from assembly of a pair of dimers.
