N ϵ -Thioacetyl-Lysine-Containing Tri-, Tetra-, and Pentapeptides as SIRT1 and SIRT2 Inhibitors
2009; American Chemical Society; Volume: 52; Issue: 7 Linguagem: Inglês
10.1021/jm801401k
ISSN1520-4804
AutoresPäivi H. Kiviranta, Tiina Suuronen, Erik A. A. Wallén, Jukka Leppänen, Jussi Tervonen, Sergiy Kyrylenko, Antero Salminen, Antti Poso, Elina M. Jarho,
Tópico(s)Redox biology and oxidative stress
ResumoNϵ-Thioacetyl-lysine-containing tri-, tetra-, and pentapeptides, based on the α-tubulin and p53 protein sequences, were studied as SIRT1 and SIRT2 inhibitors. The potency of the pentapeptides depended on the selection of the side chains. The removal of N- and C-terminal residues of the pentapeptides yielded tripeptides with retained SIRT1 inhibitory activity but decreased SIRT2 inhibitory activity. The most potent SIRT1 inhibitors were equipotent with the reference compound (6-chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide) with the IC50 values of 180−330 nM.
Referência(s)