Facile synthesis of SAM-peptide conjugates through alkyl linkers targeting protein N-terminal methyltransferase 1.
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ABSTRACT:
SUBMITTER: Zhang G
PROVIDER: S-EPMC5004777 | biostudies-literature | 2016
REPOSITORIES: biostudies-literature
Publications
Facile synthesis of SAM-peptide conjugates through alkyl linkers targeting protein <i>N</i>-terminal methyltransferase 1.
RSC advances 20160111 8
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 <i>N</i>-terminal methyltransferase 1 and the most potent one exhibits a <i>K</i><sub>i</sub> value of 310 ± 55 nM. ...[more]
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