Title : Inactivation of the human P2Y12 receptor by thiol reagents requires interaction with both extracellular cysteine residues, Cys17 and Cys270.

Pub. Date : 2003 May 15

PMID : 12560222






25 Functional Relationships(s)
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1 Inactivation of the human P2Y12 receptor by thiol reagents requires interaction with both extracellular cysteine residues, Cys17 and Cys270. Sulfhydryl Compounds purinergic receptor P2Y12 Homo sapiens
2 Inactivation of the human P2Y12 receptor by thiol reagents requires interaction with both extracellular cysteine residues, Cys17 and Cys270. Cysteine purinergic receptor P2Y12 Homo sapiens
3 The thiol agent p-chloromercuribenzene sulfonic acid (pCMBS) and the active metabolites from antiplatelet drugs, clopidogrel and CS-747, inactivate the P2Y(12) receptor and are predicted to interact with the extracellular cysteine residues on the P2Y(12) receptor. Sulfhydryl Compounds purinergic receptor P2Y12 Homo sapiens
4 The thiol agent p-chloromercuribenzene sulfonic acid (pCMBS) and the active metabolites from antiplatelet drugs, clopidogrel and CS-747, inactivate the P2Y(12) receptor and are predicted to interact with the extracellular cysteine residues on the P2Y(12) receptor. Sulfhydryl Compounds purinergic receptor P2Y12 Homo sapiens
5 The thiol agent p-chloromercuribenzene sulfonic acid (pCMBS) and the active metabolites from antiplatelet drugs, clopidogrel and CS-747, inactivate the P2Y(12) receptor and are predicted to interact with the extracellular cysteine residues on the P2Y(12) receptor. Phosphorus purinergic receptor P2Y12 Homo sapiens
6 The thiol agent p-chloromercuribenzene sulfonic acid (pCMBS) and the active metabolites from antiplatelet drugs, clopidogrel and CS-747, inactivate the P2Y(12) receptor and are predicted to interact with the extracellular cysteine residues on the P2Y(12) receptor. Phosphorus purinergic receptor P2Y12 Homo sapiens
7 The thiol agent p-chloromercuribenzene sulfonic acid (pCMBS) and the active metabolites from antiplatelet drugs, clopidogrel and CS-747, inactivate the P2Y(12) receptor and are predicted to interact with the extracellular cysteine residues on the P2Y(12) receptor. chloromercuribenzene sulfonic acid purinergic receptor P2Y12 Homo sapiens
8 The thiol agent p-chloromercuribenzene sulfonic acid (pCMBS) and the active metabolites from antiplatelet drugs, clopidogrel and CS-747, inactivate the P2Y(12) receptor and are predicted to interact with the extracellular cysteine residues on the P2Y(12) receptor. chloromercuribenzene sulfonic acid purinergic receptor P2Y12 Homo sapiens
9 The thiol agent p-chloromercuribenzene sulfonic acid (pCMBS) and the active metabolites from antiplatelet drugs, clopidogrel and CS-747, inactivate the P2Y(12) receptor and are predicted to interact with the extracellular cysteine residues on the P2Y(12) receptor. 4-Chloromercuribenzenesulfonate purinergic receptor P2Y12 Homo sapiens
10 The thiol agent p-chloromercuribenzene sulfonic acid (pCMBS) and the active metabolites from antiplatelet drugs, clopidogrel and CS-747, inactivate the P2Y(12) receptor and are predicted to interact with the extracellular cysteine residues on the P2Y(12) receptor. 4-Chloromercuribenzenesulfonate purinergic receptor P2Y12 Homo sapiens
11 The thiol agent p-chloromercuribenzene sulfonic acid (pCMBS) and the active metabolites from antiplatelet drugs, clopidogrel and CS-747, inactivate the P2Y(12) receptor and are predicted to interact with the extracellular cysteine residues on the P2Y(12) receptor. Clopidogrel purinergic receptor P2Y12 Homo sapiens
12 The thiol agent p-chloromercuribenzene sulfonic acid (pCMBS) and the active metabolites from antiplatelet drugs, clopidogrel and CS-747, inactivate the P2Y(12) receptor and are predicted to interact with the extracellular cysteine residues on the P2Y(12) receptor. Clopidogrel purinergic receptor P2Y12 Homo sapiens
13 The thiol agent p-chloromercuribenzene sulfonic acid (pCMBS) and the active metabolites from antiplatelet drugs, clopidogrel and CS-747, inactivate the P2Y(12) receptor and are predicted to interact with the extracellular cysteine residues on the P2Y(12) receptor. Cesium purinergic receptor P2Y12 Homo sapiens
14 The thiol agent p-chloromercuribenzene sulfonic acid (pCMBS) and the active metabolites from antiplatelet drugs, clopidogrel and CS-747, inactivate the P2Y(12) receptor and are predicted to interact with the extracellular cysteine residues on the P2Y(12) receptor. Cesium purinergic receptor P2Y12 Homo sapiens
15 The thiol agent p-chloromercuribenzene sulfonic acid (pCMBS) and the active metabolites from antiplatelet drugs, clopidogrel and CS-747, inactivate the P2Y(12) receptor and are predicted to interact with the extracellular cysteine residues on the P2Y(12) receptor. Cysteine purinergic receptor P2Y12 Homo sapiens
16 In this study we identified the reactive cysteine residues on the human P2Y(12) receptor by site-directed mutagenesis using pCMBS as the thiol reagent. Cysteine purinergic receptor P2Y12 Homo sapiens
17 In this study we identified the reactive cysteine residues on the human P2Y(12) receptor by site-directed mutagenesis using pCMBS as the thiol reagent. 4-Chloromercuribenzenesulfonate purinergic receptor P2Y12 Homo sapiens
18 In this study we identified the reactive cysteine residues on the human P2Y(12) receptor by site-directed mutagenesis using pCMBS as the thiol reagent. Sulfhydryl Compounds purinergic receptor P2Y12 Homo sapiens
19 Cys97Ser and Cys175Ser mutants of the P2Y(12) receptor did not express when transfected into Chinese hamster ovary (CHO-K1) cells, indicating the essential nature of a disulfide bridge between these residues. Disulfides purinergic receptor P2Y12 Homo sapiens
20 Similarly, the median inhibitory concentration (IC(50)) values for BzATP (2",3"-O-(4- benzoylbenzoyl) adenosine 5"-triphosphate), an antagonist of the P2Y(12) receptor, also did not differ dramatically among these mutants and the wild-type P2Y(12) receptor. 3'-O-(4-benzoyl)benzoyladenosine 5'-triphosphate purinergic receptor P2Y12 Homo sapiens
21 These results indicate that, unlike the P2Y(1) receptor, which has 2 essential disulfide bridges linking its extracellular domains, the P2Y(12) receptor has 2 free cysteines in its extracellular domains (Cys17 and Cys270), both of which are targets of thiol reagents. Cysteine purinergic receptor P2Y12 Homo sapiens
22 These results indicate that, unlike the P2Y(1) receptor, which has 2 essential disulfide bridges linking its extracellular domains, the P2Y(12) receptor has 2 free cysteines in its extracellular domains (Cys17 and Cys270), both of which are targets of thiol reagents. Sulfhydryl Compounds purinergic receptor P2Y12 Homo sapiens
23 We speculate that the active metabolites of clopidogrel and CS-747 form disulfide bridges with both Cys17 and Cys270 in the P2Y(12) receptor, and thereby inactivate the receptor. Clopidogrel purinergic receptor P2Y12 Homo sapiens
24 We speculate that the active metabolites of clopidogrel and CS-747 form disulfide bridges with both Cys17 and Cys270 in the P2Y(12) receptor, and thereby inactivate the receptor. Cesium purinergic receptor P2Y12 Homo sapiens
25 We speculate that the active metabolites of clopidogrel and CS-747 form disulfide bridges with both Cys17 and Cys270 in the P2Y(12) receptor, and thereby inactivate the receptor. Disulfides purinergic receptor P2Y12 Homo sapiens