STABILIZED α HELICAL PEPTIDES AND USES THEREOF

摘要

PROBLEM TO BE SOLVED: To provide a stabilized α helical peptide and a production method thereof.SOLUTION: Stably cross-linking a polypeptide having at least two modified amino acids (a process termed "hydrocarbon stapling") can help to conformationally bestow a native secondary structure of that polypeptide, and can have improved biological activity relative to an uncrosslinked polypeptide. The cross-linked polypeptide can include an α-helical domain of a BCL-2 family member polypeptide (e.g., BID-BH3 domain), which can bind to BAK/BAX and/or BCL-2/BCL-XL to promote or inhibit apoptosis, and can treat diseases characterized by excessive or inadequate cellular death.