Late-stage lipidation of fully elaborated tryptophan-containing peptides for improved pharmacokinetics

Tetrahedron Letters(2017)

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摘要
•Selective tryptophan functionalization was applied in non-protected peptides with native sequence.•The model peptide modified through tryptophan late-stage lipidation conserved bioactivity.•Peptide glucagon with lipidation on tryptophan shown a greatly improved pharmacokinetic profile.
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关键词
Late-stage functionalization,Lipidation,Peptides,Incretin,Glucagon
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