Linear aliphatic dialkynes as alternative linkers for double-click stapling of p53-derived peptides.

Abstract

We investigated linear aliphatic dialkynes as a new structural class of i,i+7 linkers for the double-click stapling of p53-based peptides. The optimal combination of azido amino acids and dialkynyl linker length for MDM2 binding was determined. In a direct comparison between aliphatic and aromatic staple scaffolds, the aliphatic staples resulted in superior… (More)
DOI: 10.1002/cbic.201402374

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