4.6 Article

Methyl to trifluoromethyl substitution as a strategy to increase the membrane permeability of short peptides

Journal

ORGANIC & BIOMOLECULAR CHEMISTRY
Volume 19, Issue 43, Pages 9386-9389

Publisher

ROYAL SOC CHEMISTRY
DOI: 10.1039/d1ob01565f

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Funding

  1. AGC Inc.
  2. Program for Leading Graduate School (MERIT)

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The study found that CH3 to CF3 substitution is beneficial for enhancing the membrane permeability of di-/tri-peptides.
Here, we investigated the effect of CH3 to CF3 substitution on the membrane permeability of peptides. We synthesized a series of peptides with CF3 groups and corresponding nonfluorinated peptides and measured the membrane permeability of the peptides. As a result, we demonstrated that CH3 to CF3 substitution is useful for increasing the membrane permeability of di-/tri-peptides.

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