A Mechanism-based Potent Sirtuin Inhibitor Containing Nε-thiocarbamoyl-lysine (TuAcK)

Overview

Journal Bioorg Med Chem Lett

Specialty Biochemistry

Date 2011 Jul 15

PMID 21752644

Citations 9

Authors

Brett M Hirsch

Yujun Hao

Xiaopeng Li

Chrys Wesdemiotis

Zhenghe Wang

Weiping Zheng

Affiliations

Soon will be listed here.

Abstract

In the current study, we have identified N(ε)-thiocarbamoyl-lysine (TuAcK) as a general sirtuin inhibitory warhead which was shown to be able to confer potent sirtuin inhibition. This inhibition was also shown to be mechanism-based in that the TuAck residue was able to be processed by a sirtuin enzyme with the formation of a stalled S-alkylamidate intermediate.

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