abstract |
The present invention provides a stabilized α-helix peptide and a production method thereof. Stable cross-linking of a polypeptide having at least two modified amino acids (a process referred to as “hydrocarbon staple”) sterically alters the original secondary structure of the polypeptide. And has improved biological activity compared to uncrosslinked polypeptides. The cross-linked polypeptide can comprise the α-helix domain (eg, BID-BH3 domain) of a BCL-2 family member polypeptide, which binds to BAK / BAX and / or BCL-2 / BCL-XL, Promotes or inhibits apoptosis and treats diseases characterized by excessive or inappropriate cell death. [Selection figure] None |