abstract |
PROBLEM TO BE SOLVED: To provide a peptide comprising a bridging ("hydrocarbon staple") moiety that provides a tether between two amino acid motifs. A composition for treating cancer caused by a BCL-2 family member comprising a cell-permeable cross-linked polypeptide of formula (I) and a pharmaceutically acceptable excipient. The cross-linked polypeptide has (i) an α-helical secondary structure in an aqueous solution and has an α-helical property of at least 35%, as determined by circular dichroism, (ii) Comprising an amino acid sequence exhibiting enhanced cell permeability compared to a non-crosslinking polypeptide, and (iii) at least 60% identical to an amino acid sequence selected from the group consisting of SEQ ID NOs: 92-111, Composition. [Selection figure] None |