D103 - Lecture 17 - Signaling III.docx

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University of California - Irvine
Biological Sciences
Grant Mac Gregor

A. Clicker a. No GAP = signaling would occur for a longer period of time B. G-Protein Coupled Receptors C. Allosteric Binding Sites a. Secondary binding sites b. Causes conformational change in the primary binding site i. Increase or decrease affinity B. Monomeric GTPases a. GTPase are only active when they are GTP bound b. Has an allosteric-type effect on target molecules B. Binding site of GTPase a. Conformational change when GTP and GDP binds b. Small changes can cause a big change B. GTPase cycle a. GDI and GEF are opposites b. Very slow GTP hydrolysis i. Key in allowing these molecules to act as signaling molecules B. G protein a. Heterotrimeric GTPase b. Subunits i. Alpha 1. Has lipid modifications ii. Beta iii. Gamma 1. Has lipid modifications b. Interacts with GPCR i. 7 - alpha helix transmembrane receptor ii. Affects conformational change in the alpha subunit 1. Takes up GTP ii. Alpha separates from beta/gamma subunits B. GPCR Facts a. Important in vision b. Drugs are popular in targeting GPCR c. Beta/gamma i. Helps to shut down the alpha subunit ii. Can also signal things B. GPCR process a. Ligand binds to GPCR b. GPCR conformational change
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