Systematic Exploration of Passive Permeability in Tetrapeptides with Hydrogen‐Bond‐Accepting Amino Acid Side Chains
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DOI: 10.1002/cmdc.202200204
Abstract: We synthesized and experimentally tested the passive permeability of more than thirty tetrapeptides mimicking the N‐terminus of the pro‐apoptotic protein Smac (Second mitochondria‐derived activator of caspases). Each peptide bore one or two unnatural Hydrogen Bond… read more here.
Keywords: permeability; amino acid; hydrogen bond; passive permeability ... See more keywords
Impact of In Vitro Passive Permeability in a P-gp-transfected LLC-PK1 Model on the Prediction of the Rat and Human Unbound Brain-to-Plasma Concentration Ratio.
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DOI: 10.1007/s11095-020-02867-z
Abstract: PURPOSE More accurate prediction of the extent of drug brain exposure in early drug discovery and understanding potential species differences could help to guide medicinal chemistry and avoid unnecessary animal studies. Hence, the aim of… read more here.
Keywords: transfected llc; brain; llc pk1; passive permeability ... See more keywords
Each side chain of cyclosporin A is not essential for high passive permeability across lipid bilayers
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DOI: 10.1039/d3ra01358h
Abstract: We compared the passive permeability of cyclosporin A (CsA) derivatives with side chain deletions across lipid bilayers. CsA maintained passive permeability after losing any one of the side chains, which suggests that the propensity of… read more here.
Keywords: side chain; passive permeability; across lipid; high passive ... See more keywords