Identification of a sirtuin 3 inhibitor that displays selectivity over sirtuin 1 and 2

Ubaldina Galli; Ornella Mesenzani; Camilla Coppo; Giovanni Sorba; Pier Luigi Canonico; Gian Cesare Tron; Armando A Genazzani

doi:10.1016/j.ejmech.2012.07.001

Identification of a sirtuin 3 inhibitor that displays selectivity over sirtuin 1 and 2

Eur J Med Chem. 2012 Sep:55:58-66. doi: 10.1016/j.ejmech.2012.07.001. Epub 2012 Jul 15.

Authors

Ubaldina Galli¹, Ornella Mesenzani, Camilla Coppo, Giovanni Sorba, Pier Luigi Canonico, Gian Cesare Tron, Armando A Genazzani

Affiliation

¹ Dipartimento di Scienze del Farmaco, Università degli Studi del Piemonte Orientale A. Avogadro, Largo Donegani 2, 28100 Novara, Italy.

PMID: 22835719
DOI: 10.1016/j.ejmech.2012.07.001

Abstract

As part of an effort to identify novel selective modulators of sirtuins, we synthesized and tested several isosteres and constrained analogues of nicotinamide. Biological data suggest that compound 2 is selective for Sirt3 over Sirt1 and Sirt2.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Cell Line, Tumor
Cell Proliferation / drug effects
Drug Evaluation, Preclinical
Histone Deacetylase Inhibitors / chemical synthesis
Histone Deacetylase Inhibitors / chemistry
Histone Deacetylase Inhibitors / pharmacology*
Humans
Niacinamide / chemical synthesis
Niacinamide / chemistry
Niacinamide / pharmacology*
Sirtuin 1 / antagonists & inhibitors*
Sirtuin 2 / antagonists & inhibitors*
Sirtuin 3 / antagonists & inhibitors*
Substrate Specificity

Substances

Histone Deacetylase Inhibitors
Niacinamide
Sirtuin 1
Sirtuin 2
Sirtuin 3