Sirtuin functions and modulation: from chemistry to the clinic

Aminothiazoles as Potent and Selective Sirt2 Inhibitors: A Structure–Activity Relationship Study

(2016) Matthias Schiedel et al.   JOURNAL OF MEDICINAL CHEMISTRY

1,4-Dihydropyridines Active on the SIRT1/AMPK Pathway Ameliorate Skin Repair and Mitochondrial Function and Exhibit Inhibition of Proliferation in Cancer Cells

(2016) Sergio Valente et al.   JOURNAL OF MEDICINAL CHEMISTRY

The lifespan extension effects of resveratrol are conserved in the honey bee and may be driven by a mechanism related to caloric restriction

(2016) Brenda Rascón et al.   Aging-US

Sirt1 activation by resveratrol is substrate sequence-selective

(2016) Mahadevan Lakshminarasimhan et al.   Aging-US

Tumour-suppressive function of SIRT4 in human colorectal cancer

(2015) M Miyo et al.   BRITISH JOURNAL OF CANCER

An exploratory double-blind, randomized clinical trial with selisistat, a SirT1 inhibitor, in patients with Huntington's disease

(2015) Sigurd D. Süssmuth et al.   BRITISH JOURNAL OF CLINICAL PHARMACOLOGY

SIRT1-Mediated eNAMPT Secretion from Adipose Tissue Regulates Hypothalamic NAD+ and Function in Mice

(2015) Myeong Jin Yoon et al.   Cell Metabolism

The histone deacetylase SIRT6 controls embryonic stem cell fate via TET-mediated production of 5-hydroxymethylcytosine

(2015) Jean-Pierre Etchegaray et al.   NATURE CELL BIOLOGY

Sirtuin 3 regulates Foxo3a-mediated antioxidant pathway in microglia

(2015) P. Rangarajan et al.   NEUROSCIENCE

SIRT1 expression is associated with poor prognosis of lung adenocarcinoma

(2015) Chong Li et al.   OncoTargets and Therapy

Selective Sirt2 inhibition by ligand-induced rearrangement of the active site

(2015) Tobias Rumpf et al.   Nature Communications

Crystallographic structure of a small molecule SIRT1 activator-enzyme complex

(2015) Han Dai et al.   Nature Communications

Honokiol blocks and reverses cardiac hypertrophy in mice by activating mitochondrial Sirt3

(2015) Vinodkumar B. Pillai et al.   Nature Communications

Repositioning antipsychotic chlorpromazine for treating colorectal cancer by inhibiting sirtuin 1

(2015) Wen-Ying Lee et al.   Oncotarget

Acetylation of glucokinase regulatory protein decreases glucose metabolism by suppressing glucokinase activity

(2015) Joo-Man Park et al.   Scientific Reports

The Deacetylase Sirtuin 1 Regulates Human Papillomavirus Replication by Modulating Histone Acetylation and Recruitment of DNA Damage Factors NBS1 and Rad51 to Viral Genomes

(2015) Erika S. Langsfeld et al.   PLoS Pathogens

The Sirtuin-2 Inhibitor AK7 Is Neuroprotective in Models of Parkinson’s Disease but Not Amyotrophic Lateral Sclerosis and Cerebral Ischemia

(2015) Xiqun Chen et al.   PLoS One

High nuclear expression levels of histone-modifying enzymes LSD1, HDAC2 and SIRT1 in tumor cells correlate with decreased survival and increased relapse in breast cancer patients

(2014) Remco S Derr et al.   BMC CANCER

Sirtuin deacetylases: A new target for melanoma management

(2014) Melissa J Wilking et al.   CELL CYCLE

Lysine Glutarylation Is a Protein Posttranslational Modification Regulated by SIRT5

(2014) Minjia Tan et al.   Cell Metabolism

Development of Pyrazolone and Isoxazol-5-one Cambinol Analogues as Sirtuin Inhibitors

(2014) Sumit S. Mahajan et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Potent and Selective Sirtuin 2 (SIRT2) Inhibitors Using a Fragment-Based Approach

(2014) Huaqing Cui et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Novel and Selective SIRT6 Inhibitors

(2014) Marco Daniele Parenti et al.   JOURNAL OF MEDICINAL CHEMISTRY

Chroman-4-one- and Chromone-Based Sirtuin 2 Inhibitors with Antiproliferative Properties in Cancer Cells

(2014) Tina Seifert et al.   JOURNAL OF MEDICINAL CHEMISTRY

Antitumor Effects of a Sirtuin Inhibitor, Tenovin-6, against Gastric Cancer Cells via Death Receptor 5 Up-Regulation

(2014) Sachiko Hirai et al.   PLoS One

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

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

SIRT5 facilitates cancer cell growth and drug resistance in non-small cell lung cancer

(2014) Weidong Lu et al.   TUMOR BIOLOGY

High levels of SIRT1 expression enhance tumorigenesis and associate with a poor prognosis of colorectal carcinoma patients

(2014) Xiaojing Chen et al.   Scientific Reports

SIRT2: Tumour suppressor or tumour promoter in operable breast cancer?

(2013) Liane M. McGlynn et al.   EUROPEAN JOURNAL OF CANCER

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

A Nitric Oxide-dependent Cross-talk between Class I and III Histone Deacetylases Accelerates Skin Repair

(2013) Francesco Spallotta 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

Regulation of SIRT2 levels for human non-small cell lung cancer therapy

(2013) Ziming Li et al.   LUNG CANCER

Antitumor Effect of SIRT1 Inhibition in Human HCC Tumor Models In Vitro and In Vivo

(2013) S. Portmann et al.   MOLECULAR CANCER THERAPEUTICS

Sirt1 Promotes Axonogenesis by Deacetylation of Akt and Inactivation of GSK3

(2013) Xiao-hong Li et al.   MOLECULAR NEUROBIOLOGY

SIRT1 Expression Is Associated with the Chemotherapy Response and Prognosis of Patients with Advanced NSCLC

(2013) Tao Zhang et al.   PLoS One

Ex-527 inhibits Sirtuins by exploiting their unique NAD+-dependent deacetylation mechanism

(2013) M. Gertz et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Evidence for a Common Mechanism of SIRT1 Regulation by Allosteric Activators

(2013) B. P. Hubbard et al.   SCIENCE

Schistosoma mansoni Sirtuins: Characterization and Potential as Chemotherapeutic Targets

(2013) Julien Lancelot et al.   PLoS Neglected Tropical Diseases

Sirtuin activators and inhibitors

(2012) José M. Villalba et al.   BIOFACTORS

Resveratrol Ameliorates Aging-Related Metabolic Phenotypes by Inhibiting cAMP Phosphodiesterases

(2012) Sung-Jun Park 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

SIRT1, Is It a Tumor Promoter or Tumor Suppressor?

(2012) Chu-Xia Deng   International Journal of Biological Sciences

High expression of the longevity gene product SIRT1 and apoptosis induction by sirtinol in adult T-cell leukemia cells

(2012) Tomohiro Kozako et al.   INTERNATIONAL JOURNAL OF CANCER

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

SIRT1 Protects against  -Synuclein Aggregation by Activating Molecular Chaperones

(2012) G. Donmez et al.   JOURNAL OF NEUROSCIENCE

Autophagy induced by the class III histone deacetylase Sirt1 prevents prion peptide neurotoxicity

(2012) Jae-Kyo Jeong et al.   NEUROBIOLOGY OF AGING

Peptides and Pseudopeptides as SIRT6 Deacetylation Inhibitors

(2012) Piia Kokkonen et al.   ACS Medicinal Chemistry Letters

The Sirtuin 2 Inhibitor AK-7 Is Neuroprotective in Huntington’s Disease Mouse Models

(2012) Vanita Chopra et al.   Cell Reports

Sirtuins and Disease: The Road Ahead

(2012) Vincenzo Carafa et al.   Frontiers in Pharmacology

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

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

Small-Molecule Allosteric Activators of Sirtuins

(2011) David A. Sinclair et al.   Annual Review of Pharmacology and Toxicology

SIRT2 activity is required for the survival of C6 glioma cells

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

Simplification of the tetracyclic SIRT1-selective inhibitor MC2141: Coumarin- and pyrimidine-based SIRT1/2 inhibitors with different selectivity profile

(2011) Dante Rotili et al.   BIOORGANIC & MEDICINAL CHEMISTRY

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

(2011) H. Yuan et al.   BLOOD

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

Sirt1 mediates neuroprotection from mutant huntingtin by activation of the TORC1 and CREB transcriptional pathway

(2011) Hyunkyung Jeong et al.   NATURE MEDICINE

Succinate Dehydrogenase Is a Direct Target of Sirtuin 3 Deacetylase Activity

(2011) Lydia W. S. Finley et al.   PLoS One

Sirt5 Is a NAD-Dependent Protein Lysine Demalonylase and Desuccinylase

(2011) J. Du et al.   SCIENCE

SRT1720 improves survival and healthspan of obese mice

(2011) Robin K. Minor et al.   Scientific Reports

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

Nε-Modified lysine containing inhibitors for SIRT1 and SIRT2

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

Sirt3 Mediates Reduction of Oxidative Damage and Prevention of Age-Related Hearing Loss under Caloric Restriction

(2010) Shinichi Someya et al.   CELL

Identification of Tri- and Tetracyclic Pyrimidinediones as Sirtuin Inhibitors

(2010) Dante Rotili et al.   ChemMedChem

SIRT1 Activation by Small Molecules

(2010) Han Dai et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

SRT1720, SRT2183, SRT1460, and Resveratrol Are Not Direct Activators of SIRT1

(2010) Michelle Pacholec et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Sirt3-Mediated Deacetylation of Evolutionarily Conserved Lysine 122 Regulates MnSOD Activity in Response to Stress

(2010) Randa Tao et al.   MOLECULAR CELL

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

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

SIRT2-mediated protein deacetylation: An emerging key regulator in brain physiology and pathology

(2009) Kai Harting et al.   EUROPEAN 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

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

Inhibition of Human Sirtuins by in Situ Generation of an Acetylated Lysine−ADP−Ribose Conjugate

(2009) Tomomi Asaba et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

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 of oxazolo[4,5-b]pyridines and related heterocyclic analogs as novel SIRT1 activators

(2008) Jean E. Bemis et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

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

(2008) Sonia Lain et al.   CANCER CELL

Substituting Nε-thioacetyl-lysine for Nε-acetyl-lysine in Peptide Substrates as a General Approach to Inhibiting Human NAD+-dependent Protein Deacetylases

(2008) David Fatkins et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

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

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

(2008) E Lara et al.   ONCOGENE