Sandbox Reserved 430: Difference between revisions
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==Binding Interactions== | ==Binding Interactions== | ||
The <scene name='48/483887/Binding_site/4'>Binding Site</scene> of P2Y12 is colored in purple, which | The <scene name='48/483887/Binding_site/4'>Binding Site</scene> of P2Y12 is colored in purple, and the ligand (AZD1283) is colored in yellow. The binding site for AZD1283, pocket 1, is composed of helices III–VII, while pocket II contains helices I-III and VII is not represented here. The two pockets are separated by two residues, Y1053 and K2807, which makes the pocket II not a binding site for AZD1283. With the observation of the AZD1283-bound P2Y12R with residue C97 belong to pocket 2, the active metabolites drugs might occupy this pocket. | ||
==Additional Features== | ==Additional Features== | ||
Acute coronary syndrome, a condition in which there is sudden blockage of blood flow to the heart, is majorly caused by a disease known as atherothrombosis. P2Y12 receptors are a source of anti platelet therapy for the prevention of these conditions. Clopidogrel in complex with P2Y12 in combination with aspirin has guaranteed benefits, however many of the patients treated with clopidogrel-linked P2Y12 with insufficient P2Y12-inhibition experienced inimical side effects. Drug-drug interactions, obesity, diabetes mellitus (DM), reduced left ventricular function and inflammation are all associated with inadequate response to clopidogrel therapy. Clopidogrel is a pro-drug and thienopyridine-type inhibitor of the P2Y12 receptor, which requires Cytochrome P450 to hepatic ally transform it to exert its anti platelet effect. <scene name='48/483887/P450/1'>Click Here</scene> to see this interaction between the P450 complex and Clopidogrel | Acute coronary syndrome, a condition in which there is sudden blockage of blood flow to the heart, is majorly caused by a disease known as atherothrombosis. P2Y12 receptors are a source of anti platelet therapy for the prevention of these conditions. Clopidogrel in complex with P2Y12 in combination with aspirin has guaranteed benefits, however many of the patients treated with clopidogrel-linked P2Y12 with insufficient P2Y12-inhibition experienced inimical side effects. Drug-drug interactions, obesity, diabetes mellitus (DM), reduced left ventricular function and inflammation are all associated with inadequate response to clopidogrel therapy. Clopidogrel is a pro-drug and thienopyridine-type inhibitor of the P2Y12 receptor, which requires Cytochrome P450 to hepatic ally transform it to exert its anti platelet effect. <scene name='48/483887/P450/1'>Click Here</scene> to see this interaction between the P450 complex and Clopidogrel. | ||
==Quiz Question 1== | ==Quiz Question 1== | ||