PHAR 562 Lecture Notes - Lecture 7: Alpha Helix, Gria2, Glioblastoma Multiforme
12 Feb 2020
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Gabaa, kainate and nmda receptors are involved in many cns disorders: need for drugs to up- and down-regulate receptor function. Polypharmacy: use drugs with different sites of actions to lower individual drug side-effect (many drugs with save overall effect) Drug companies make thousands of drugs as a library. When information about diseases pops up: check drug library and see if something fit. Gabaar types are region-specific in the brain (more useful for drug action than targeting glurs: unlike glutamate receptors which are not specific. Proposal: transform the type of ampa receptors into calcium-impermeable (add. Glua2) works in mice: expression by region ties into behaviour, distinct gabaar have different roles in microcircuits. Antagonist (mkr-1 (?)) was thought to help. Nmdars are obligate heteromers with multiple drug-binding sites: glun2 is glutamate-binding, glun1 is glycine-binding, other gluns are glycine-regulated (as far as we know) 4 sites: 2 glutamate, 2 glycine. Nmdars are highly regulated by endogenous and exogenous blockers and modulators.
