Literature DB >> 19700324

Identification of a cell-active non-peptide sirtuin inhibitor containing N-thioacetyl lysine.

Takayoshi Suzuki1, Tomomi Asaba, Erika Imai, Hiroki Tsumoto, Hidehiko Nakagawa, Naoki Miyata.   

Abstract

To identify cell-active sirtuin inhibitors containing N-thioacetyl lysine, we synthesized compound 1, which was designed based on the structure of the reported N-ethoxycarbonylacetyl lysine-based sirtuin inhibitor NCS-12k. Compound 1 selectively inhibited SIRT1 in enzyme assays. Compound 1 also caused a dose-dependent increase in p53 acetylation in human colon cancer HCT116 cells, indicating the inhibition of SIRT1 in these cells.

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Year:  2009        PMID： 19700324     DOI： 10.1016/j.bmcl.2009.08.028

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  12 in total

Review 1.  Sirtuin catalysis and regulation.

Authors:  Jessica L Feldman; Kristin E Dittenhafer-Reed; John M Denu
Journal:  J Biol Chem       Date:  2012-10-18       Impact factor: 5.157

Review 2.  Using mitochondrial sirtuins as drug targets: disease implications and available compounds.

Authors:  Melanie Gertz; Clemens Steegborn
Journal:  Cell Mol Life Sci       Date:  2016-03-23       Impact factor: 9.261

3.  Mechanism-Based Inhibitors of the Human Sirtuin 5 Deacylase: Structure-Activity Relationship, Biostructural, and Kinetic Insight.

Authors:  Nima Rajabi; Marina Auth; Kathrin R Troelsen; Martin Pannek; Dhaval P Bhatt; Martin Fontenas; Matthew D Hirschey; Clemens Steegborn; Andreas S Madsen; Christian A Olsen
Journal:  Angew Chem Int Ed Engl       Date:  2017-11-02       Impact factor: 15.336

4.  A SIRT2-Selective Inhibitor Promotes c-Myc Oncoprotein Degradation and Exhibits Broad Anticancer Activity.

Authors:  Hui Jing; Jing Hu; Bin He; Yashira L Negrón Abril; Jack Stupinski; Keren Weiser; Marisa Carbonaro; Ying-Ling Chiang; Teresa Southard; Paraskevi Giannakakou; Robert S Weiss; Hening Lin
Journal:  Cancer Cell       Date:  2016-03-14       Impact factor: 31.743

Review 5.  Sirtuin inhibitors as anticancer agents.

Authors:  Jing Hu; Hui Jing; Hening Lin
Journal:  Future Med Chem       Date:  2014-05       Impact factor: 3.808

6.  Insights into Lysine Deacetylation of Natively Folded Substrate Proteins by Sirtuins.

Authors:  Philipp Knyphausen; Susanne de Boor; Nora Kuhlmann; Lukas Scislowski; Antje Extra; Linda Baldus; Magdalena Schacherl; Ulrich Baumann; Ines Neundorf; Michael Lammers
Journal:  J Biol Chem       Date:  2016-05-18       Impact factor: 5.157

Review 7.  Rejuvenating sirtuins: the rise of a new family of cancer drug targets.

Authors:  Santina Bruzzone; Marco Daniele Parenti; Alessia Grozio; Alberto Ballestrero; Inga Bauer; Alberto Del Rio; Alessio Nencioni
Journal:  Curr Pharm Des       Date:  2013       Impact factor: 3.116

8.  Genetically encoding thioacetyl-lysine as a non-deacetylatable analog of lysine acetylation in Escherichia coli.

Authors:  Sumana Venkat; Dharma Theja Nannapaneni; Caroline Gregory; Qinglei Gan; Matt McIntosh; Chenguang Fan
Journal:  FEBS Open Bio       Date:  2017-10-16       Impact factor: 2.693

Review 9.  Sirtuin functions and modulation: from chemistry to the clinic.

Authors:  Vincenzo Carafa; Dante Rotili; Mariantonietta Forgione; Francesca Cuomo; Enrica Serretiello; Gebremedhin Solomon Hailu; Elina Jarho; Maija Lahtela-Kakkonen; Antonello Mai; Lucia Altucci
Journal:  Clin Epigenetics       Date:  2016-05-25       Impact factor: 6.551

10.  Ligand-based virtual screening and inductive learning for identification of SIRT1 inhibitors in natural products.

Authors:  Yunan Sun; Hui Zhou; Hongmei Zhu; Siu-wai Leung
Journal:  Sci Rep       Date:  2016-01-25       Impact factor: 4.379
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