PCOL3012 Lecture Notes - Lecture 6: Glucose Transporter, Glutamate Transporter, Succinic Acid

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25 Aug 2018
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Intracellular targets: enzymes, nuclear receptors, protein synthesis. Beta adrenergic receptors: a(cid:272)tivated (cid:271)y (cid:272)ate(cid:272)hola(cid:373)i(cid:374)e"s (cid:894)adre(cid:374)ali(cid:374)e or (cid:374)oradre(cid:374)ali(cid:374)e(cid:895, synthetic ligands developed to treat asthma, hypertension or cardiac disease, full agonists, partial agonists or antagonists. Salbutamol- b2 adrenergic receptor agonist: noradrenaline (norepinephrine, activates beta and alpha adrenergic receptors, salbutamol, n-trimethyl group- selectivity for beta2 adrenergic receptors, used for the treatment of asthma- causes bronchodilation. Subtle differences between agonist and antagonist bound states: differences in the ligand-binding pocket between antagonist-bound (grey) and agonist-bound (orange) b1-adrenergic receptor. Transporters: membrane proteins control movement of everything across the cell membrane; nutrient uptake, waste disposal and cell to cell communication (neurotransmitters, transporters move a substrate across the cell membrane. Passive transporters (facilitators, eg. na+ independent glucose transporter) Active transporters (pumps): require energy, move a substrate against a concentration gradient, primary active transporters; light, atp hydrolysis, eg. Na+/k+ atpase: secondary active transporters; pre-existing ion gradients, eg. plasma membrane glutamate transporter (all nt transporters)

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