Q3 - 3269557 QUESTION 3 There are two primary ways to turn...

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3269557 QUESTION 3 There are two primary ways to turn off G-protein coupled receptor (GPCR) – dependent responses. One way is the deactivation of G-protein via the hydrolysis of GTP to GDP. The other was involves the desensitization of GPCRs in either a non-selective or an agonist specific manner. The non-selective way involves blocking the interaction with G-proteins. On the other hand there is an agonist specific approach that blocks the ability to activate G-proteins. Deactivation of G-proteins The inactive form of G-protein complex is comprised of α, β, and γ subunits bound to a receptor. The α subunit is bound to GDP, and the β/γ subunits stay associated throughout the activation-inactivation cycle. First, there is an agonist-mediated GPCR activation causing a conformational change to expose the binding site for the transducer. Diffusion of the complex leads to the association with its respective G protein (ex. Gs) which promotes GDP-GTP exchange via guanine exchange factors (GEFs).
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This note was uploaded on 04/07/2008 for the course NSCI 5461 taught by Professor Newman during the Spring '08 term at Minnesota.

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Q3 - 3269557 QUESTION 3 There are two primary ways to turn...

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