Sandbox Reserved 430: Difference between revisions
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The P2Y12 receptor is mainly found on the surface of blood platelets, and functions as a regulator in platelet activation and therefore blood clotting. The P2Y12 receptor is a G-protein coupled receptor, <scene name='48/483887/Sun/1'>a seven-transmembrane domain protein</scene> linked to the cAMP-signaling pathway. It mediates platelet activation by decreasing intracellular cAMP levels through inhibition of an AC-mediated signaling pathway. Acting as a chemoreceptor, P2Y12 utilizes ADP as an agonist, which initiates ADP-induced platelet aggregation. Clopidogrel in covalent binding complex with P2Y12 acts as an antiplatelet agent, specifically as an ADP receptor inhibitor to decrease platelet aggregation and inhibit thrombus formation. | The P2Y12 receptor is mainly found on the surface of blood platelets, and functions as a regulator in platelet activation and therefore blood clotting. The P2Y12 receptor is a G-protein coupled receptor, <scene name='48/483887/Sun/1'>a seven-transmembrane domain protein</scene> linked to the cAMP-signaling pathway. It mediates platelet activation by decreasing intracellular cAMP levels through inhibition of an AC-mediated signaling pathway. Acting as a chemoreceptor, P2Y12 utilizes ADP as an agonist, which initiates ADP-induced platelet aggregation. Clopidogrel in covalent binding complex with P2Y12 acts as an antiplatelet agent, specifically as an ADP receptor inhibitor to decrease platelet aggregation and inhibit thrombus formation. | ||
Clopidogrel is a pro-drug and thienopyridine-type inhibitor of the P2Y12 receptor, which requires Cytochrome P450 to hepatically transform it to exert its anti platelet effect. <scene name='48/483887/P450/3'>Cytochrome P450</scene> is a membrane protein, characteristic of alternating font color='gray'>hydrophobic</font> and font color='pink'>polar</font> groups. The central heme group is stabilized by several side chains. The <font color='orange'>Fe2+</font> atom that makes up the heart of the heme group is surrounded by a font color='blue'>highly hydrophobic porphyrin ring</font> . The role of the heme group in biological systems is to facilitate oxygen transport as well as aid in electron transfer as part of the electron transport chain. The heme group of the hemeprotein Cytochrome P450 acts as a catalyst for the metabolism of clopidogrel. Shown below is the activation of Clopidogrel in vivo. CYP2C19 is an enzymatic member of the cytochrome P450 mixed-function oxidase system. | Clopidogrel is a pro-drug and thienopyridine-type inhibitor of the P2Y12 receptor, which requires Cytochrome P450 to hepatically transform it to exert its anti platelet effect. <scene name='48/483887/P450/3'>Cytochrome P450</scene> is a membrane protein, characteristic of alternating <font color='gray'>hydrophobic</font> and <font color='pink'>polar</font> groups. The central heme group is stabilized by several side chains. The <font color='orange'>Fe2+</font> atom that makes up the heart of the heme group is surrounded by a <font color='blue'>highly hydrophobic porphyrin ring</font> . The role of the heme group in biological systems is to facilitate oxygen transport as well as aid in electron transfer as part of the electron transport chain. The heme group of the hemeprotein Cytochrome P450 acts as a catalyst for the metabolism of clopidogrel. Shown below is the activation of Clopidogrel in vivo. CYP2C19 is an enzymatic member of the cytochrome P450 mixed-function oxidase system. | ||
[[Image:Clop converted.jpg]] | [[Image:Clop converted.jpg]] | ||