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ChemMedChem

Selective modification of the N-terminal structure of polytheonamide B significantly changes its cytotoxicity and activity as an ion channel.


PMID 22489077

Abstract

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.

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