Facile synthesis of SAM-peptide conjugates through alkyl linkers targeting protein N-terminal methyltransferase 1.

ABSTRACT: We report the first chemical synthesis of SAM-peptide conjugates through alkyl linkers to prepare bisubstrate analogs for protein methyltransferases. We demonstrate its application by developing a series of bisubstrate inhibitors for protein N-terminal methyltransferase 1 and the most potent one exhibits a K_i value of 310 ± 55 nM.

SUBMITTER: Zhang G 

PROVIDER: S-EPMC5004777 | biostudies-literature | 2016

REPOSITORIES: biostudies-literature