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Simple N(ε)-thioacetyl-lysine-containing cyclic peptides exhibiting highly potent sirtuin inhibition.
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Mechanism-based inhibition of Sir2 deacetylases by thioacetyl-lysine peptide.
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Identification of a cell-active non-peptide sirtuin inhibitor containing N-thioacetyl lysine.
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Novel sirtuin inhibitory warheads derived from the N(ε)-acetyl-lysine analog L-2-amino-7-carboxamidoheptanoic acid.
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Inhibition of human sirtuins by in situ generation of an acetylated lysine-ADP-ribose conjugate.
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Structural basis of SIRT7 nucleosome engagement and substrate specificity.
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Current Trends in Sirtuin Activator and Inhibitor Development.
Molecules. 2024 Mar 6;29(5):1185. doi: 10.3390/molecules29051185.
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Structural Basis of Sirtuin 6-Catalyzed Nucleosome Deacetylation.
J Am Chem Soc. 2023 Mar 29;145(12):6811-6822. doi: 10.1021/jacs.2c13512. Epub 2023 Mar 17.
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Identification of 2-hydroxybenzoic acid derivatives as selective SIRT5 inhibitors.
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Cyclic Peptide-Based Sirtuin Substrates.
Molecules. 2019 Jan 24;24(3):424. doi: 10.3390/molecules24030424.
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Isoxazole-Derived Amino Acids are Bromodomain-Binding Acetyl-Lysine Mimics: Incorporation into Histone H4 Peptides and Histone H3.
Angew Chem Int Ed Engl. 2016 Jul 11;55(29):8353-7. doi: 10.1002/anie.201602908. Epub 2016 Jun 6.
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Novel thiourea-based sirtuin inhibitory warheads.
Bioorg Med Chem Lett. 2015 Aug 15;25(16):3319-24. doi: 10.1016/j.bmcl.2015.05.058. Epub 2015 May 30.
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Sirtuin inhibitors as anticancer agents.
Future Med Chem. 2014 May;6(8):945-66. doi: 10.4155/fmc.14.44.

本文引用的文献

2
Medicinal chemistry of sirtuin inhibitors.
Curr Med Chem. 2011;18(13):1936-46. doi: 10.2174/092986711795590057.
3
Silencing of SIRT2 induces cell death and a decrease in the intracellular ATP level of PC12 cells.
Int J Physiol Pathophysiol Pharmacol. 2011;3(1):65-70. Epub 2011 Feb 20.
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The sirtuin pathway in ageing and Alzheimer disease: mechanistic and therapeutic considerations.
Lancet Neurol. 2011 Mar;10(3):275-9. doi: 10.1016/S1474-4422(11)70013-8.
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SIRT1 modulation as a novel approach to the treatment of diseases of aging.
J Med Chem. 2011 Jan 27;54(2):417-32. doi: 10.1021/jm100861p. Epub 2010 Nov 16.
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Regulation of intermediary metabolism by protein acetylation.
Trends Biochem Sci. 2011 Feb;36(2):108-16. doi: 10.1016/j.tibs.2010.09.003. Epub 2010 Oct 8.
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Sirtuin regulation of mitochondria: energy production, apoptosis, and signaling.
Trends Biochem Sci. 2010 Dec;35(12):669-75. doi: 10.1016/j.tibs.2010.07.003. Epub 2010 Sep 20.
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Emerging mitochondrial signaling mechanisms in physiology, aging processes, and as drug targets.
Exp Gerontol. 2011 Feb-Mar;46(2-3):174-7. doi: 10.1016/j.exger.2010.08.024. Epub 2010 Sep 16.
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Therapeutic potential of activators and inhibitors of sirtuins.
Biofactors. 2010 Sep-Oct;36(5):383-93. doi: 10.1002/biof.112.
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Sirtuin mechanism and inhibition: explored with N(ε)-acetyl-lysine analogs.
Mol Biosyst. 2011 Jan;7(1):16-28. doi: 10.1039/c0mb00033g. Epub 2010 Sep 15.

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