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Amino Acid Residues in the P2X7 Receptor that Mediate Differential Sensitivity to ATP and BzATP

Amino Acid Residues in the P2X7 Receptor that Mediate Differential Sensitivity to ATP and BzATP,10.1124/mol.106.030163,Molecular Pharmacology,M. T. Yo

Amino Acid Residues in the P2X7 Receptor that Mediate Differential Sensitivity to ATP and BzATP   (Citations: 22)
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Journal: Molecular Pharmacology - MOL PHARMACOL , vol. 71, no. 1, pp. 92-100, 2006
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    • ...Swapping fragments and point mutations in the extracellular loop between rat and mouse P2X7 receptors also demonstrated that amino acid residues in the ectodomain of the P2X7 receptor are involved in the differential sensitivity to agonists between species [79]...

    Chengqun Sunet al. Identification and characterization of a novel variant of the human P2...

    • ...The agonist dependence may relate to the fact that overlapping but distinctive parts of the P2X7 receptor are engaged in the binding of BzATP and ATP (Young et al. 2007)...

    Lin-Hua Jiang. Inhibition of P2X 7 receptors by divalent cations: old action and new ...

    • ...Dose-response curve for BzATP on GSK-3 phosphorylation is shown in Fig. 1b. The EC50 value obtained was 20.77 ± 4.28 lM, which is in the range of that described for the rat P2X7 receptor (Young et al. 2007)...
    • ...First, the EC50 value is in the range (low micromolar) of that described for rat P2X7 receptors (Young et al. 2007)...
    • ...This is in agreement to the 10-fold lower agonistic affinity described for ATP on P2X7 receptors in comparison to BzATP (Young et al. 2007)...

    Felipe Ortegaet al. P2X 7 Nucleotide Receptor is Coupled to GSK-3 Inhibition and Neuroprot...

    • ...more potent than ATP at P2X7 receptors; and more potent at rat P2X7 than mouse P2X7 [17]...
    • ...mouse) [17]. Interestingly, the corresponding residue in zfP2X4.1 (Ser127) is positioned within the ‘head’ region,...
    • ...head domain close to the ATP binding site which corresponds to Lys 127 in rat P2X7 (thought to be involved in BzATP binding; [17]), is shown in purple...

    Mark T. Young. P2X receptors: dawn of the post-structure era

    • ...Moreover, recent reports indicate that mutation of other residues in this region can result in gainof-function P2X7 (A127K in mouse P2X7 and H155Y in human P2X7) [59, 60] or affect the inhibition of P2X7 function by zinc and magnesium (H130A in rat P2X7) [61] (see also Fig. 6, below)...
    • ...Amino acid residues that, when mutated, result in a gain-of-function are shown in bold and are highlighted in green [59, 60]...
    • ...Residues that alter the sensitivity of the receptor to zinc, copper, and/or magnesium are shown in bold red [58, 59, 61, 77]...

    Nicole Schwarzet al. Activation of the P2X7 ion channel by soluble and covalently bound lig...

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