“Although 5-(N,N-hexamethylene)-amiloride(HMA) and amantadine, tworeported inhibitors of proton pumpsand SARS-CoV-E channels, exhibited inhibitoryactivity on 2-E channels at 50mM or greater, further investigation into these compounds was hindered by theirstrong cytotoxicity.”(BingqingXia).
https://pubmed.ncbi.nlm.nih.gov/29169687/
“Another new inhibitor identified as BIT225, a derivative of amiloride, also inhibits the viroporin function of HIV-1 Vpu and HCV p7. In the present study, molecular dynamics simulations were applied to get insights into molecular details of a BIT225 binding site. In addition, the g_mmpbsa approach was employed to calculate the binding free energy and free energy decomposition per residue. MD simulation results in the p7-BIT225 complex revealed that drug binding to hydrophobic pocket can allosterically inhibit ion conduction via the funnel tip by restricting significant intrinsic channel breath at the tip of the funnel.”
So many possible connections here.
BIT225 having completed toxicity studies…!
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