BIO200H5 Lecture Notes - Lecture 6: Dill, Intermolecular Force, Diazepam

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2 Oct 2016
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Effectors communicate to the cell that the drug is doing an effect. Change in target conformations: kinases have a pocket for atp that either accepts it or blocks it off. This small change is enough to change the entire protein function. Ligand is still able to bind naturally to its pocket at the site. The allosteric drug would bind to another side of the drug (a different pocket!) Allosteric can enhance or inhibit target activity: ex; benzodiazepines (this case valium) and gaba receptor (gaba is a neurotransmitter). When gaba binds, ligand-gated channels open, which increases chloride influx. In the absence of gaba, there is high neuronal activity. When gaba binds, it opens receptors and decreases neuronal activity by allowing negatively charged ions into the cell. The valium then binds to another pocket to cause an even greater conformational change, allowing even more ions to flow in. It speeds up the ion transmission, decreasing neuronal activity.

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