Sirtuin modulators: where are we now? A review of patents from 2015 to 2019

Mitochondrial function, metabolic regulation and human disease viewed through the prism of sirtuin 4 (SIRT4) functions

(2019) Cora N. Betsinger et al.   JOURNAL OF PROTEOME RESEARCH

Updates on the epigenetic roles of sirtuins

(2019) Tatsiana Kosciuk et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

SIRT4 and Its Roles in Energy and Redox Metabolism in Health, Disease and During Exercise

(2019) Yumei Han et al.   Frontiers in Physiology

Enzymatic and Biological Characterization of Novel Sirtuin Modulators against Cancer

(2019) Vincenzo Carafa et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

The Roles of Sirtuin Family Proteins in Cancer Progression

(2019) Erhu Zhao et al.   Cancers

RIP1–HAT1–SIRT Complex Identification and Targeting in Treatment and Prevention of Cancer

(2018) Vincenzo Carafa et al.   CLINICAL CANCER RESEARCH

Functions of the sirtuin deacylase SIRT5 in normal physiology and pathobiology

(2018) Surinder Kumar et al.   CRITICAL REVIEWS IN BIOCHEMISTRY AND MOLECULAR BIOLOGY

Potent and Selective Inhibitors of Human Sirtuin 5

(2018) Diana Kalbas et al.   JOURNAL OF MEDICINAL CHEMISTRY

Sirtuin activators and inhibitors: Promises, achievements, and challenges

(2018) Han Dai et al.   PHARMACOLOGY & THERAPEUTICS

New chemical tools for probing activity and inhibition of the NAD + -dependent lysine deacylase sirtuin 2

(2018) Sören Swyter et al.   PHILOSOPHICAL TRANSACTIONS OF THE ROYAL SOCIETY B-BIOLOGICAL SCIENCES

Pharmacological activation of SIRT6 triggers lethal autophagy in human cancer cells

(2018) Sara Iachettini et al.   Cell Death & Disease

Cyclic tripeptide-based potent human SIRT7 inhibitors

(2018) Shengchao Li et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

An overview of Sirtuins as potential therapeutic target: Structure, function and modulators

(2018) Yijie Wang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Structural Basis of Sirtuin 6 Inhibition by the Hydroxamate Trichostatin A: Implications for Protein Deacylase Drug Development

(2018) Weijie You et al.   JOURNAL OF MEDICINAL CHEMISTRY

Identification of a cellularly active SIRT6 allosteric activator

(2018) Zhimin Huang et al.   Nature Chemical Biology

Development of 1,2,4-Oxadiazoles as Potent and Selective Inhibitors of the Human Deacetylase Sirtuin 2: Structure–Activity Relationship, X-ray Crystal Structure, and Anticancer Activity

(2017) Sébastien Moniot et al.   JOURNAL OF MEDICINAL CHEMISTRY

Chemically Induced Degradation of Sirtuin 2 (Sirt2) by a Proteolysis Targeting Chimera (PROTAC) Based on Sirtuin Rearranging Ligands (SirReals)

(2017) Matthias Schiedel et al.   JOURNAL OF MEDICINAL CHEMISTRY

SIRT6: Novel Mechanisms and Links to Aging and Disease

(2017) Luisa Tasselli et al.   TRENDS IN ENDOCRINOLOGY AND METABOLISM

Crystal structures of the mitochondrial deacylase Sirtuin 4 reveal isoform-specific acyl recognition and regulation features

(2017) Martin Pannek et al.   Nature Communications

Structural Basis of Sirtuin 6 Activation by Synthetic Small Molecules

(2016) Weijie You et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Structure-Based Development of an Affinity Probe for Sirtuin 2

(2016) Matthias Schiedel et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

How much successful are the medicinal chemists in modulation of SIRT1: A critical review

(2016) Ashwani Kumar et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Crystal structures of SIRT3 reveal that the α2-α3 loop and α3-helix affect the interaction with long-chain acyl lysine

(2016) Wei Gai et al.   FEBS LETTERS

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

SIRT7-dependent deacetylation of the U3-55k protein controls pre-rRNA processing

(2016) Sifan Chen et al.   Nature Communications

SIRT7 is a histone desuccinylase that functionally links to chromatin compaction and genome stability

(2016) Lei Li et al.   Nature Communications

Sirtuin functions and modulation: from chemistry to the clinic

(2016) Vincenzo Carafa et al.   Clinical Epigenetics

Mitochondrial Sirtuins and Their Relationships with Metabolic Disease and Cancer

(2015) Surinder Kumar et al.   ANTIOXIDANTS & REDOX SIGNALING

SIRT5 regulation of ammonia-induced autophagy and mitophagy

(2015) Lucia Polletta et al.   Autophagy

Protective role of SIRT5 against motor deficit and dopaminergic degeneration in MPTP-induced mice model of Parkinson's disease

(2015) Lei Liu et al.   BEHAVIOURAL BRAIN RESEARCH

Human SIRT3 tripeptidic inhibitors containing Nε-thioacetyl-lysine

(2015) Bing Chen et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

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

Sirtuins in Epigenetic Regulation

(2015) Hui Jing et al.   CHEMICAL REVIEWS

Quinazolinedione SIRT6 inhibitors sensitize cancer cells to chemotherapeutics

(2015) Giovanna Sociali et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Sirtuin 3 regulates Foxo3a-mediated antioxidant pathway in microglia

(2015) P. Rangarajan et al.   NEUROSCIENCE

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

SIRT7 inactivation reverses metastatic phenotypes in epithelial and mesenchymal tumors

(2015) Shivani Malik et al.   Scientific Reports

A Randomized, Placebo-Controlled Study of SRT2104, a SIRT1 Activator, in Patients with Moderate to Severe Psoriasis

(2015) James G. Krueger et al.   PLoS One

The Sirt1 activator SRT3025 provides atheroprotection in Apoe−/− mice by reducing hepatic Pcsk9 secretion and enhancing Ldlr expression

(2014) Melroy X. Miranda et al.   EUROPEAN HEART JOURNAL

New assays and approaches for discovery and design of Sirtuin modulators

(2014) Mike Schutkowski et al.   Expert Opinion on Drug Discovery

A potent and selective Sirtuin 1 inhibitor alleviates pathology in multiple animal and cell models of Huntington's disease

(2014) Marianne R. Smith et al.   HUMAN MOLECULAR GENETICS

SIRT5 Regulates the Mitochondrial Lysine Succinylome and Metabolic Networks

(2013) Matthew J. Rardin et al.   Cell Metabolism

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

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

The 2.5 Å Crystal Structure of the SIRT1 Catalytic Domain Bound to Nicotinamide Adenine Dinucleotide (NAD+) and an Indole (EX527 Analogue) Reveals a Novel Mechanism of Histone Deacetylase Inhibition

(2013) Xun Zhao et al.   JOURNAL OF MEDICINAL CHEMISTRY

The Identification of the SIRT1 Activator SRT2104 as a Clinical Candidate

(2013) Pui Ng et al.   Letters in Drug Design & Discovery

Sirtuin 7 Plays a Role in Ribosome Biogenesis and Protein Synthesis

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

An acetylome peptide microarray reveals specificities and deacetylation substrates for all human sirtuin isoforms

(2013) David Rauh et al.   Nature Communications

Forever young: SIRT3 a shield against mitochondrial meltdown, aging, and neurodegeneration

(2013) Brad Kincaid et al.   Frontiers in Aging Neuroscience

Janus-faced role of SIRT1 in tumorigenesis

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

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

SIRT1 Protects against  -Synuclein Aggregation by Activating Molecular Chaperones

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

SIRT7 links H3K18 deacetylation to maintenance of oncogenic transformation

(2012) Matthew F. Barber et al.   NATURE

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

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

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

(2012) Vanita Chopra et al.   Cell Reports

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

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

(2011) Hyunkyung Jeong et al.   NATURE MEDICINE

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

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

SIRT4 Regulates Fatty Acid Oxidation and Mitochondrial Gene Expression in Liver and Muscle Cells

(2010) Nargis Nasrin 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

SIRT2 regulates NF- B-dependent gene expression through deacetylation of p65 Lys310

(2010) K. M. Rothgiesser et al.   JOURNAL OF CELL SCIENCE

Biochemical characterization, localization, and tissue distribution of the longer form of mouse SIRT3

(2010) Lei Jin et al.   PROTEIN SCIENCE

The Critical Role of the Class III Histone Deacetylase SIRT1 in Cancer

(2009) T. Liu et al.   CANCER RESEARCH

SIRT5 Deacetylates Carbamoyl Phosphate Synthetase 1 and Regulates the Urea Cycle

(2009) Takashi Nakagawa et al.   CELL

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

(2009) Kai Harting et al.   EUROPEAN JOURNAL OF CELL BIOLOGY

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

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

Paths of Convergence: Sirtuins in Aging and Neurodegeneration

(2008) Li Gan et al.   NEURON

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