Issue 42, 2015

Novel sirtuin inhibitory warheads derived from the Nε-acetyl-lysine analog l-2-amino-7-carboxamidoheptanoic acid

Abstract

Built upon the catalytic mechanism-based pan-SIRT1/2/3 inhibitory warhead L-2-amino-7-carboxamidoheptanoic acid (L-ACAH, a close structural analog of Nε-acetyl-lysine) that our laboratory discovered recently, in the current study, its carboxamide NH2-ethylated analog was found to be a ∼2.4–6.6-fold stronger SIRT1/2/3 inhibitory warhead than L-ACAH. Carboxamide NH2-dodecylated and carboxymethylated analogs of L-ACAH were also identified as potent SIRT6 and SIRT5 inhibitory warheads, respectively.

Graphical abstract: Novel sirtuin inhibitory warheads derived from the Nε-acetyl-lysine analog l-2-amino-7-carboxamidoheptanoic acid

Supplementary files

Article information

Article type
Communication
Submitted
16 Aug 2015
Accepted
22 Sep 2015
First published
22 Sep 2015

Org. Biomol. Chem., 2015,13, 10442-10450

Novel sirtuin inhibitory warheads derived from the Nε-acetyl-lysine analog L-2-amino-7-carboxamidoheptanoic acid

Y. He, L. Yan, W. Zang and W. Zheng, Org. Biomol. Chem., 2015, 13, 10442 DOI: 10.1039/C5OB01721A

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