- Selective modification of the N-terminal structure of polytheonamide B significantly changes its cytotoxicity and activity as an ion channel.
Selective modification of the N-terminal structure of polytheonamide B significantly changes its cytotoxicity and activity as an ion channel.
ChemMedChem (2012-04-11)
Naoki Shinohara, Hiroaki Itoh, Shigeru Matsuoka, Masayuki Inoue
PMID22489077
ZUSAMMENFASSUNG
Chemical point mutation: Polytheonamide B is a naturally occurring polypeptide containing 48 amino acids. It both displays potent cytotoxicity and acts as a monovalent cation channel in vitro. Chemoselective methods to modify the 44th, N-, and C-terminal residues of the natural product have been developed, and evaluation of the resultant derivatives suggests that the intrinsic activities of the peptide can only be altered by switching its N-terminal substitution.