TY - JOUR
T1 - Synthesis and biological characterisation of sirtuin inhibitors based on the tenovins
AU - McCarthy, Anna R.
AU - Pirrie, Lisa
AU - Hollick, Jonathan J.
AU - Ronseaux, Sebastien
AU - Campbell, Johanna
AU - Higgins, Maureen
AU - Staples, Oliver D.
AU - Tran, Fanny
AU - Slawin, Alexandra M. Z.
AU - Lain, Sonia
AU - Westwood, Nicholas J.
PY - 2012/3/1
Y1 - 2012/3/1
N2 - The tenovins are small molecule inhibitors of the NAD(+)-dependent family of protein deacetylases known as the sirtuins. There remains considerable interest in inhibitors of this enzyme family due to possible applications in both cancer and neurodegenerative disease therapy. Through the synthesis of novel tenovin analogues, further insights into the structural requirements for activity against the sirtuins in vitro are provided. In addition, the activity of one of the analogues in cells led to an improved understanding of the function of SirT1 in cells. (C) 2012 Elsevier Ltd. All rights reserved.
AB - The tenovins are small molecule inhibitors of the NAD(+)-dependent family of protein deacetylases known as the sirtuins. There remains considerable interest in inhibitors of this enzyme family due to possible applications in both cancer and neurodegenerative disease therapy. Through the synthesis of novel tenovin analogues, further insights into the structural requirements for activity against the sirtuins in vitro are provided. In addition, the activity of one of the analogues in cells led to an improved understanding of the function of SirT1 in cells. (C) 2012 Elsevier Ltd. All rights reserved.
U2 - 10.1016/j.bmc.2012.01.001
DO - 10.1016/j.bmc.2012.01.001
M3 - Article
SN - 0968-0896
VL - 20
SP - 1779
EP - 1793
JO - Bioorganic & Medicinal Chemistry
JF - Bioorganic & Medicinal Chemistry
IS - 5
ER -
