CBIO 3400 Lecture Notes - Lecture 36: G Protein–Coupled Receptor, Cyclic Adenosine Monophosphate, Adrenergic Receptor

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Activate g protein which goes on to activate more proteins. More than 800 gpcrs in human genomes 150 are of unknown function. *almost half of known drugs work through gpcrs. When gpcr bind signal (or ligand) and undergo a conformational change which allows them to activate trimeric g-protein. Beta and gamma are bound by a lipid anchor into the plasma membrane. Gpcr is a gef for the alpha subunit of g-protein. Replaces gdp wiith gtp on alpha subunit and activate alpha subunit and b and gamma subunit. And they activate enzymes like: adenylyl cyclase (makes camp), guanylyl cyclase (makes cgmp) Hormone binds to gpcr which activates alpha subunit, releasing gdp and replacing with gtp. Hydrolysis of gtp to gdp causes alpha to dissociate from effector and associate with beta and gamma. Adrenalin stimulates beta adrenergic receptor which is a gpcr. Pka phosphorylates creb (cyclic amp response element binding protein) Which binds the cyclic amp response element (cre) upstream of gene.

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