Sirtuin inhibitors as anticancer agents

Regulation of the mPTP by SIRT3-mediated deacetylation of CypD at lysine 166 suppresses age-related cardiac hypertrophy

(2016) Angela V. Hafner et al.   Aging-US

Sirt2 Deacetylase Is a Novel AKT Binding Partner Critical for AKT Activation by Insulin

(2014) Gopalakrishnan Ramakrishnan et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Small molecule SIRT1 activators for the treatment of aging and age-related diseases

(2014) Basil P. Hubbard et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Epigenetic silencing of ARRDC3 expression in basal-like breast cancer cells

(2014) Young Hwa Soung et al.   Scientific Reports

SIRT4 Has Tumor-Suppressive Activity and Regulates the Cellular Metabolic Response to DNA Damage by Inhibiting Mitochondrial Glutamine Metabolism

(2013) Seung Min Jeong et al.   CANCER CELL

Lysine-5 Acetylation Negatively Regulates Lactate Dehydrogenase A and Is Decreased in Pancreatic Cancer

(2013) Di Zhao et al.   CANCER CELL

The mTORC1 Pathway Stimulates Glutamine Metabolism and Cell Proliferation by Repressing SIRT4

(2013) Alfred Csibi et al.   CELL

SIRT3 deacetylates FOXO3 to protect mitochondria against oxidative damage

(2013) Anne H.H. Tseng et al.   FREE RADICAL BIOLOGY AND MEDICINE

The tumor suppressor SirT2 regulates cell cycle progression and genome stability by modulating the mitotic deposition of H4K20 methylation

(2013) L. Serrano et al.   GENES & DEVELOPMENT

SIRT2 overexpression in hepatocellular carcinoma mediates epithelial to mesenchymal transition by protein kinase B/glycogen synthase kinase-3β/β-catenin signaling

(2013) Juan Chen et al.   HEPATOLOGY

Activation of the Protein Deacetylase SIRT6 by Long-chain Fatty Acids and Widespread Deacylation by Mammalian Sirtuins

(2013) Jessica L. Feldman et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Screen of Pseudopeptidic Inhibitors of Human Sirtuins 1–3: Two Lead Compounds with Antiproliferative Effects in Cancer Cells

(2013) Paolo Mellini et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Thieno[3,2-d]pyrimidine-6-carboxamides as Potent Inhibitors of SIRT1, SIRT2, and SIRT3

(2013) Jeremy S. Disch et al.   JOURNAL OF MEDICINAL CHEMISTRY

Sirtuin 7 Plays a Role in Ribosome Biogenesis and Protein Synthesis

(2013) Yuan-Chin Tsai et al.   MOLECULAR & CELLULAR PROTEOMICS

HDAC6 and SIRT2 Regulate the Acetylation State and Oncogenic Activity of Mutant K-RAS

(2013) M. H. Yang et al.   MOLECULAR CANCER RESEARCH

Tenovin-D3, a Novel Small-Molecule Inhibitor of Sirtuin SirT2, Increases p21 (CDKN1A) Expression in a p53-Independent Manner

(2013) A. R. McCarthy et al.   MOLECULAR CANCER THERAPEUTICS

Repression of RNA Polymerase I upon Stress Is Caused by Inhibition of RNA-Dependent Deacetylation of PAF53 by SIRT7

(2013) Sifan Chen et al.   MOLECULAR CELL

Acetylation Stabilizes ATP-Citrate Lyase to Promote Lipid Biosynthesis and Tumor Growth

(2013) Ruiting Lin et al.   MOLECULAR CELL

SIRT5-Mediated Lysine Desuccinylation Impacts Diverse Metabolic Pathways

(2013) Jeongsoon Park et al.   MOLECULAR CELL

SIRT1 Positively Regulates Breast Cancer Associated Human Aromatase (CYP19A1) Expression

(2013) Kimberly R. Holloway et al.   MOLECULAR ENDOCRINOLOGY

SIRT1-Mediated FoxO1 Deacetylation Is Essential for Multidrug Resistance-Associated Protein 2 Expression in Tamoxifen-Resistant Breast Cancer Cells

(2013) Hoo-Kyun Choi et al.   MOLECULAR PHARMACEUTICS

SIRT6 regulates TNF-α secretion through hydrolysis of long-chain fatty acyl lysine

(2013) Hong Jiang et al.   NATURE

SIRT6 exhibits nucleosome-dependent deacetylase activity

(2013) R. Gil et al.   NUCLEIC ACIDS RESEARCH

A fluorogenic assay for screening Sirt6 modulators

(2013) Jing Hu et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Inhibition of the NAD-Dependent Protein Deacetylase SIRT2 Induces Granulocytic Differentiation in Human Leukemia Cells

(2013) Yoshitaka Sunami et al.   PLoS One

Enterocyte-Specific Inactivation of SIRT1 Reduces Tumor Load in the APC+/min Mouse Model

(2013) Vid Leko et al.   PLoS One

Metabolic Characterization of a Sirt5 deficient mouse model

(2013) Jiujiu Yu et al.   Scientific Reports

SIRT7 Represses Myc Activity to Suppress ER Stress and Prevent Fatty Liver Disease

(2013) Jiyung Shin et al.   Cell Reports

Discovery of Macrocyclic Peptides Armed with a Mechanism-Based Warhead: Isoform-Selective Inhibition of Human Deacetylase SIRT2

(2012) Jumpei Morimoto et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Janus-faced role of SIRT1 in tumorigenesis

(2012) Na-Young Song et al.   Annals of the New York Academy of Sciences

Synthesis and biological characterisation of sirtuin inhibitors based on the tenovins

(2012) Anna R. McCarthy et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Novel acridinedione derivatives: Design, synthesis, SIRT1 enzyme and tumor cell growth inhibition studies

(2012) Mallika Alvala et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Ethylenediamine diacetate (EDDA) mediated synthesis of aurones under ultrasound: Their evaluation as inhibitors of SIRT1

(2012) Khanapur Manjulatha et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Inhibition of the human deacylase Sirtuin 5 by the indole GW5074

(2012) Benjamin Suenkel et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Acetylation-Dependent Regulation of Skp2 Function

(2012) Hiroyuki Inuzuka et al.   CELL

The Histone Deacetylase SIRT6 Is a Tumor Suppressor that Controls Cancer Metabolism

(2012) Carlos Sebastián et al.   CELL

The histone deacetylase SIRT2 stabilizes Myc oncoproteins

(2012) P Y Liu et al.   CELL DEATH AND DIFFERENTIATION

A small molecule Inauhzin inhibits SIRT1 activity and suppresses tumour growth through activation of p53

(2012) Qi Zhang et al.   EMBO Molecular Medicine

Seven sirtuins for seven deadly diseases ofaging

(2012) Brian J. Morris   FREE RADICAL BIOLOGY AND MEDICINE

SIRT3 interacts with the daf-16 homolog FOXO3a in the Mitochondria, as well as increases FOXO3a Dependent Gene expression

(2012) Kristi Muldoon Jacobs et al.   International Journal of Biological Sciences

Design, Synthesis, and Biological Activity of a Novel Series of Human Sirtuin-2-Selective Inhibitors

(2012) Takayoshi Suzuki et al.   JOURNAL OF MEDICINAL CHEMISTRY

Benzodeazaoxaflavins as Sirtuin Inhibitors with Antiproliferative Properties in Cancer Stem Cells

(2012) Dante Rotili et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Salermide-Related Sirtuin Inhibitors: Binding Mode Studies and Antiproliferative Effects in Cancer Cells Including Cancer Stem Cells

(2012) Dante Rotili et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and Evaluation of Substituted Chroman-4-one and Chromone Derivatives as Sirtuin 2-Selective Inhibitors

(2012) Maria Fridén-Saxin et al.   JOURNAL OF MEDICINAL CHEMISTRY

SIRT3 Functions in the Nucleus in the Control of Stress-Related Gene Expression

(2012) T. Iwahara et al.   MOLECULAR AND CELLULAR BIOLOGY

SIRT1 promotes thyroid carcinogenesis driven by PTEN deficiency

(2012) D Herranz et al.   ONCOGENE

SIRT1 deacetylase promotes acquisition of genetic mutations for drug resistance in CML cells

(2012) Z Wang et al.   ONCOGENE

A Brain-Permeable Small Molecule Reduces Neuronal Cholesterol by Inhibiting Activity of Sirtuin 2 Deacetylase

(2011) David M. Taylor et al.   ACS Chemical Biology

SIRT2 activity is required for the survival of C6 glioma cells

(2011) Xin He et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

A mechanism-based potent sirtuin inhibitor containing Nε-thiocarbamoyl-lysine (TuAcK)

(2011) Brett M. Hirsch et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Activation of stress response gene SIRT1 by BCR-ABL promotes leukemogenesis

(2011) H. Yuan et al.   BLOOD

SIRT2 Maintains Genome Integrity and Suppresses Tumorigenesis through Regulating APC/C Activity

(2011) Hyun-Seok Kim et al.   CANCER CELL

SIRT3 Opposes Reprogramming of Cancer Cell Metabolism through HIF1α Destabilization

(2011) Lydia W.S. Finley et al.   CANCER CELL

Oxidative Damage Targets Complexes Containing DNA Methyltransferases, SIRT1, and Polycomb Members to Promoter CpG Islands

(2011) Heather M. O'Hagan et al.   CANCER CELL

Nicotinamide Blocks Proliferation and Induces Apoptosis of Chronic Lymphocytic Leukemia Cells through Activation of the p53/miR-34a/SIRT1 Tumor Suppressor Network

(2011) V. Audrito et al.   CANCER RESEARCH

Medicinal Chemistry of Sirtuin Inhibitors

(2011) L. Chen   CURRENT MEDICINAL CHEMISTRY

Salermide up-regulates death receptor 5 expression through the ATF4-ATF3-CHOP axis and leads to apoptosis in human cancer cells

(2011) Guangbo Liu et al.   JOURNAL OF CELLULAR AND MOLECULAR MEDICINE

The effect of combined treatment with cisplatin and histone deacetylase inhibitors on HeLa cells

(2011) Ke Long Jin et al.   Journal of Gynecologic Oncology

Structure-Based Design of Pseudopeptidic Inhibitors for SIRT1 and SIRT2

(2011) Tero Huhtiniemi et al.   JOURNAL OF MEDICINAL CHEMISTRY

The First Identification of Lysine Malonylation Substrates and Its Regulatory Enzyme

(2011) Chao Peng et al.   MOLECULAR & CELLULAR PROTEOMICS

Stabilization of Suv39H1 by SirT1 Is Part of Oxidative Stress Response and Ensures Genome Protection

(2011) Laia Bosch-Presegué et al.   MOLECULAR CELL

Deacetylation of FOXO3 by SIRT1 or SIRT2 leads to Skp2-mediated FOXO3 ubiquitination and degradation

(2011) F Wang et al.   ONCOGENE

SirT3 suppresses hypoxia inducible factor 1α and tumor growth by inhibiting mitochondrial ROS production

(2011) E L Bell et al.   ONCOGENE

Synergistic Interactions between HDAC and Sirtuin Inhibitors in Human Leukemia Cells

(2011) Michele Cea et al.   PLoS One

The c-MYC oncoprotein, the NAMPT enzyme, the SIRT1-inhibitor DBC1, and the SIRT1 deacetylase form a positive feedback loop

(2011) A. Menssen et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Sirt5 Is a NAD-Dependent Protein Lysine Demalonylase and Desuccinylase

(2011) J. Du et al.   SCIENCE

SIRT1 Promotes N-Myc Oncogenesis through a Positive Feedback Loop Involving the Effects of MKP3 and ERK on N-Myc Protein Stability

(2011) Glenn M. Marshall et al.   PLoS Genetics

Mammalian Sirtuins: Biological Insights and Disease Relevance

(2010) Marcia C. Haigis et al.   Annual Review of Pathology-Mechanisms of Disease

Inhibition of SIRT1 by a small molecule induces apoptosis in breast cancer cells

(2010) Arunasree M. Kalle et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Nε-Modified lysine containing inhibitors for SIRT1 and SIRT2

(2010) Tero Huhtiniemi et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Sirtuin-3 (SIRT3), a novel potential therapeutic target for oral cancer

(2010) Turki Y. Alhazzazi et al.   CANCER

SIRT3 Is a Mitochondria-Localized Tumor Suppressor Required for Maintenance of Mitochondrial Integrity and Metabolism during Stress

(2010) Hyun-Seok Kim et al.   CANCER CELL

Identification of Tri- and Tetracyclic Pyrimidinediones as Sirtuin Inhibitors

(2010) Dante Rotili et al.   ChemMedChem

SIRT2 down-regulation in HeLa can induce p53 accumulation via p38 MAPK activation-dependent p300 decrease, eventually leading to apoptosis

(2010) Yanze Li et al.   GENES TO CELLS

Sirtuin-3 deacetylation of cyclophilin D induces dissociation of hexokinase II from the mitochondria

(2010) Nataly Shulga et al.   JOURNAL OF CELL SCIENCE

SIRT Inhibitors Induce Cell Death and p53 Acetylation through Targeting Both SIRT1 and SIRT2

(2010) Barrie Peck et al.   MOLECULAR CANCER THERAPEUTICS

Sirtuin 1 Modulates Cellular Responses to Hypoxia by Deacetylating Hypoxia-Inducible Factor 1α

(2010) Ji-Hong Lim et al.   MOLECULAR CELL

Cytosolic FoxO1 is essential for the induction of autophagy and tumour suppressor activity

(2010) Ying Zhao et al.   NATURE CELL BIOLOGY

SIRT1 regulates Dishevelled proteins and promotes transient and constitutive Wnt signaling

(2010) K. R. Holloway et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Identification of a small molecule SIRT2 inhibitor with selective tumor cytotoxicity

(2009) Yingjia Zhang et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Development and characterization of lysine based tripeptide analogues as inhibitors of Sir2 activity

(2009) Subhra Prakash Chakrabarty et al.   BIOORGANIC & MEDICINAL CHEMISTRY

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

(2009) Takayoshi Suzuki et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Substrate specificity of SIRT1-catalyzed lysine Nε-deacetylation reaction probed with the side chain modified Nε-acetyl-lysine analogs

(2009) Nuttara Jamonnak et al.   BIOORGANIC CHEMISTRY

miR-34a as a prognostic marker of relapse in surgically resected non-small-cell lung cancer

(2009) Elena Gallardo et al.   CARCINOGENESIS

SIRT5 Deacetylates Carbamoyl Phosphate Synthetase 1 and Regulates the Urea Cycle

(2009) Takashi Nakagawa et al.   CELL

A c-Myc–SIRT1 feedback loop regulates cell growth and transformation

(2009) Jian Yuan et al.   JOURNAL OF CELL BIOLOGY

Nϵ-Thioacetyl-Lysine-Containing Tri-, Tetra-, and Pentapeptides as SIRT1 and SIRT2 Inhibitors

(2009) Päivi H. Kiviranta et al.   JOURNAL OF MEDICINAL CHEMISTRY

Novel Cambinol Analogs as Sirtuin Inhibitors: Synthesis, Biological Evaluation, and Rationalization of Activity

(2009) Federico Medda et al.   JOURNAL OF MEDICINAL CHEMISTRY

Study of 1,4-Dihydropyridine Structural Scaffold: Discovery of Novel Sirtuin Activators and Inhibitors

(2009) Antonello Mai et al.   JOURNAL OF MEDICINAL CHEMISTRY

Novel 3-Arylideneindolin-2-ones as Inhibitors of NAD+-Dependent Histone Deacetylases (Sirtuins)

(2009) Kilian Huber et al.   JOURNAL OF MEDICINAL CHEMISTRY

Characterization of Sirtuin Inhibitors in Nematodes Expressing a Muscular Dystrophy Protein Reveals Muscle Cell and Behavioral Protection by Specific Sirtinol Analogues

(2009) Matthieu Y. Pasco et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structural and Synthetic Investigations of Tanikolide Dimer, a SIRT2 Selective Inhibitor, and Tanikolideseco-Acid from the Madagascar Marine CyanobacteriumLyngbya majuscula

(2009) Marcelino Gutiérrez et al.   JOURNAL OF ORGANIC CHEMISTRY

A role for SIRT1 in cell growth and chemoresistance in prostate cancer PC3 and DU145 cells

(2008) Keitaro Kojima et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Discovery, In Vivo Activity, and Mechanism of Action of a Small-Molecule p53 Activator

(2008) Sonia Lain et al.   CANCER CELL

Impaired DNA Damage Response, Genome Instability, and Tumorigenesis in SIRT1 Mutant Mice

(2008) Rui-Hong Wang et al.   CANCER CELL

Epigenetic Control of rDNA Loci in Response to Intracellular Energy Status

(2008) Akiko Murayama et al.   CELL

Thiobarbiturates as Sirtuin Inhibitors: Virtual Screening, Free-Energy Calculations, and Biological Testing

(2008) Urszula Uciechowska et al.   ChemMedChem

Role of Sirtuin Histone Deacetylase SIRT1 in Prostate Cancer

(2008) Brittney Jung-Hynes et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Structure–Activity Studies on Splitomicin Derivatives as Sirtuin Inhibitors and Computational Prediction of Binding Mode

(2008) Robert C. Neugebauer et al.   JOURNAL OF MEDICINAL CHEMISTRY

SIRT3 Is a Stress-Responsive Deacetylase in Cardiomyocytes That Protects Cells from Stress-Mediated Cell Death by Deacetylation of Ku70

(2008) N. R. Sundaresan et al.   MOLECULAR AND CELLULAR BIOLOGY

Interplay among BRCA1, SIRT1, and Survivin during BRCA1-Associated Tumorigenesis

(2008) Rui-Hong Wang et al.   MOLECULAR CELL

SIRT6 is a histone H3 lysine 9 deacetylase that modulates telomeric chromatin

(2008) Eriko Michishita et al.   NATURE

Salermide, a Sirtuin inhibitor with a strong cancer-specific proapoptotic effect

(2008) E Lara et al.   ONCOGENE

The SIRT1 Deacetylase Suppresses Intestinal Tumorigenesis and Colon Cancer Growth

(2008) Ron Firestein et al.   PLoS One

miR-34a repression of SIRT1 regulates apoptosis

(2008) M. Yamakuchi et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Structural Insights into Intermediate Steps in the Sir2 Deacetylation Reaction

(2008) William F. Hawse et al.   STRUCTURE