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

Takahiro OnoKohsuke AikawaTakashi OkazoeJumpei MorimotoShinsuke Sando
Published in: Organic & biomolecular chemistry (2021)
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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