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The authors using biochemical process further deciphered the mechanism of action of …


Biology Articles » Biochemistry » Lipid Biochemistry » The active metabolite of Clopidogrel disrupts P2Y12 receptor oligomers and partitions them out of lipid rafts » Table 1

Table 1
- The active metabolite of Clopidogrel disrupts P2Y12 receptor oligomers and partitions them out of lipid rafts

[33P]2MeS-ADP binding characteristics and Act-Met astagonism on mutant P2Y12 receptors


Binding 2MeS-ADP
Effect of ActMet, IC50, nM
KD, nMBmax, (103 sites per cell)
P2Y12 WT 0.34 ± 0.09 486.7 ± 86.1 154.9 ± 23.8
C17A-P2Y12 0.23 ± 0.04 275.9 ± 25.9 191.5 ± 102.4
C97A-P2Y12 No binding No binding ND
C175A-P2Y12 No binding No binding ND
C194A-P2Y12 0.42 ± 0.07 411.4 ± 44.0 147.9 ± 60.6
C208A-P2Y12 0.39 ± 0.05 1,365.4 ± 97.6 159.2 ± 18.3
C248A-P2Y12 0.33 ± 0.04 718.5 ± 51.8 164.8 ± 74.6
C270A-P2Y12 0.51 ± 0.13 539.7 ± 86.7 70.4 ± 11.3
C292A-P2Y12 0.37 ± 0.06 464.4 ± 44.0 280.3 ± 78.1
C302A-P2Y12 0.63 ± 0.23 495.7 ± 138.5 85.9 ± 18.3
C315A-P2Y12 0.48 ± 0.15 453.5 ± 107.8 154.9 ± 58.8
C17A/C270A-P2Y12 3.15 ± 2.03 445.7 ± 236.7 137.9 ± 7.4
Cos7 cells transfected with plasmids encoding for P2Y12 cystein–alanine mutants were studied for their ability to bind to 2MeS-ADP and the sensitivity of this binding to Act-Met. ND, not determined.

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