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Issue 8, 2016
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Facile synthesis of SAM–peptide conjugates through alkyl linkers targeting protein N-terminal methyltransferase 1

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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 Ki value of 310 ± 55 nM.

Graphical abstract: Facile synthesis of SAM–peptide conjugates through alkyl linkers targeting protein N-terminal methyltransferase 1

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Supplementary files

Article information


Submitted
05 Oct 2015
Accepted
06 Jan 2016
First published
11 Jan 2016

RSC Adv., 2016,6, 6768-6771
Article type
Communication
Author version available

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

G. Zhang and R. Huang, RSC Adv., 2016, 6, 6768
DOI: 10.1039/C5RA20625A

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