IndraLab

Statements

KCNH2 binds astemizole. 7 / 7
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"A recently determined cryo-EM structure for the HERG-astemizole complex has confirmed the general understanding that blockers bind to a hydrophobic pocket at the entrance of the SF, thus blocking the passage of K ions, and provides further tools for structure-based screening of HERG-related cardiotoxicity [21–24]."
40197385
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"Astemizole binds with high affinity to membrane embedded hERG with a single binding site per tetramer."
25656388
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"Purified recombinant hERG binds Astemizole."
25656388
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"[ 3 H]Astemizole binds to recombinant HERG ( K D 5.9 nM) and terfenadine competes efficiently for this binding ( K i 101 nM), but not diphendydramine ( K i 21.7 μM; Chiu et al., 2004 )."
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"We determined the structure of hERG bound to astemizole, showing a clear map in the pore pathway."
39321803
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"They were tested for stability in human liver microsomes, inhibition of cloned cytochrome P450 enzymes, and inhibition of astemizole binding to hERG channel."
17532631
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"In this regard, the cryo-EM structure of hERG in complex with astemizole has been recently solved, showing the binding of astemizole to hERG [ 62 ]."
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