Schistosome sirtuins as drug targets

Design, synthesis and structure–activity relationship studies of novel sirtuin 2 (SIRT2) inhibitors with a benzamide skeleton

(2015) Taki Sakai et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Chemical Probing of the Human Sirtuin 5 Active Site Reveals Its Substrate Acyl Specificity and Peptide-Based Inhibitors

(2014) Claudia Roessler et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Sirtuin 4 Is a Lipoamidase Regulating Pyruvate Dehydrogenase Complex Activity

(2014) Rommel A. Mathias et al.   CELL

A SIRT7-Dependent Acetylation Switch of GABPβ1 Controls Mitochondrial Function

(2014) Dongryeol Ryu et al.   Cell Metabolism

SIRT7 Controls Hepatic Lipid Metabolism by Regulating the Ubiquitin-Proteasome Pathway

(2014) Tatsuya Yoshizawa et al.   Cell Metabolism

A High-Fat Diet and NAD + Activate Sirt1 to Rescue Premature Aging in Cockayne Syndrome

(2014) Morten Scheibye-Knudsen et al.   Cell Metabolism

The Discovery of a Highly Selective 5,6,7,8-Tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4(3H)-one SIRT2 Inhibitor that is Neuroprotective in an in vitro Parkinson’s Disease Model

(2014) Paolo Di Fruscia et al.   ChemMedChem

Sirtuins, metabolism, and DNA repair

(2014) Jee-Eun Choi et al.   CURRENT OPINION IN GENETICS & DEVELOPMENT

New assays and approaches for discovery and design of Sirtuin modulators

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

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

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

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

(2014) Weidong Lu et al.   TUMOR BIOLOGY

Epigenetic control of gene function in schistosomes: a source of therapeutic targets?

(2014) Alejandro Cabezas-Cruz et al.   Frontiers in Genetics

SIRT3 Deacetylates ATP Synthase F1 Complex Proteins in Response to Nutrient- and Exercise-Induced Stress

(2013) Athanassios Vassilopoulos et al.   ANTIOXIDANTS & REDOX SIGNALING

Genealogy of an ancient protein family: the Sirtuins, a family of disordered members

(2013) Susan Costantini et al.   BMC EVOLUTIONARY BIOLOGY

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

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

(2013) Alfred Csibi et al.   CELL

Sirt3 Regulates Metabolic Flexibility of Skeletal Muscle Through Reversible Enzymatic Deacetylation

(2013) E. Jing et al.   DIABETES

Calorie restriction and sirtuins revisited

(2013) L. Guarente   GENES & DEVELOPMENT

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

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

SIRT4 Coordinates the Balance between Lipid Synthesis and Catabolism by Repressing Malonyl CoA Decarboxylase

(2013) Gaëlle Laurent et al.   MOLECULAR CELL

SIRT5-Mediated Lysine Desuccinylation Impacts Diverse Metabolic Pathways

(2013) Jeongsoon Park et al.   MOLECULAR CELL

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

(2013) Hong Jiang et al.   NATURE

Sorting out functions of sirtuins in cancer

(2013) M Roth et al.   ONCOGENE

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

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

(2013) Jiyung Shin et al.   Cell Reports

Schistosoma mansoni Sirtuins: Characterization and Potential as Chemotherapeutic Targets

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

Structural Basis for the Inhibition of Histone Deacetylase 8 (HDAC8), a Key Epigenetic Player in the Blood Fluke Schistosoma mansoni

(2013) Martin Marek et al.   PLoS Pathogens

Metabolic and Neuropsychiatric Effects of Calorie Restriction and Sirtuins

(2012) Sergiy Libert et al.   Annual Review of Physiology

Inhibition of the human deacylase Sirtuin 5 by the indole GW5074

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

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

(2012) Carlos Sebastián et al.   CELL

Sirtuins as emerging anti-parasitic targets

(2012) Weiping Zheng   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Sirtuins of parasitic protozoa: In search of function(s)

(2012) Agnieszka A. Religa et al.   MOLECULAR AND BIOCHEMICAL PARASITOLOGY

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

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

Whole-genome sequence of Schistosoma haematobium

(2012) Neil D Young et al.   NATURE GENETICS

Epigenetic protein families: a new frontier for drug discovery

(2012) Cheryl H. Arrowsmith et al.   NATURE REVIEWS DRUG DISCOVERY

New and continuing developments at PROSITE

(2012) Christian J. A. Sigrist et al.   NUCLEIC ACIDS RESEARCH

Inhibitors of the NAD+-Dependent Protein Desuccinylase and Demalonylase Sirt5

(2012) Benjamin Maurer et al.   ACS Medicinal Chemistry Letters

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

Structure and Biochemical Functions of SIRT6

(2011) Patricia W. Pan et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Sirt5 Is a NAD-Dependent Protein Lysine Demalonylase and Desuccinylase

(2011) J. Du et al.   SCIENCE

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

The Histone Deacetylase Sirt6 Regulates Glucose Homeostasis via Hif1α

(2010) Lei Zhong et al.   CELL

ATM activates the pentose phosphate pathway promoting anti-oxidant defence and DNA repair

(2010) Claudia Cosentino et al.   EMBO JOURNAL

Distinct regulation of mitochondrial localization and stability of two human Sirt5 isoforms

(2010) Nobuko Matsushita et al.   GENES TO CELLS

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

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

Lessons on longevity from budding yeast

(2010) Matt Kaeberlein   NATURE

SIRT3 regulates mitochondrial fatty-acid oxidation by reversible enzyme deacetylation

(2010) Matthew D. Hirschey et al.   NATURE

Sirt1 improves healthy ageing and protects from metabolic syndrome-associated cancer

(2010) Daniel Herranz et al.   Nature Communications

Investigating the ADP-ribosyltransferase Activity of Sirtuins with NAD Analogues and32P-NAD†

(2009) Jintang Du et al.   BIOCHEMISTRY

Sirtuins inhibitors: The approach to affinity and selectivity

(2009) Yana Cen   BIOCHIMICA ET BIOPHYSICA ACTA-PROTEINS AND PROTEOMICS

Identification and characterization of novel sirtuin inhibitor scaffolds

(2009) Brandi D. Sanders et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Hepatocyte-Specific Deletion of SIRT1 Alters Fatty Acid Metabolism and Results in Hepatic Steatosis and Inflammation

(2009) Aparna Purushotham et al.   Cell Metabolism

Bisnaphthalimidopropyl Derivatives as Inhibitors ofLeishmaniaSIR2 Related Protein 1

(2009) Joana Tavares et al.   ChemMedChem

Crystal Structures of Human SIRT3 Displaying Substrate-induced Conformational Changes

(2009) Lei Jin et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

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

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

Sirtuin/Sir2 phylogeny, evolutionary considerations and structural conservation

(2009) Sebastian Greiss et al.   MOLECULES AND CELLS

The Schistosoma japonicum genome reveals features of host–parasite interplay

(2009)   NATURE

The genome of the blood fluke Schistosoma mansoni

(2009) Matthew Berriman et al.   NATURE

The Schistosomiasis Control Initiative (SCI): rationale, development and implementation from 2002–2008

(2009) A. FENWICK et al.   PARASITOLOGY

Sir2 Paralogues Cooperate to Regulate Virulence Genes and Antigenic Variation in Plasmodium falciparum

(2009) Christopher J Tonkin et al.   PLOS BIOLOGY

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

(2008) Urszula Uciechowska et al.   ChemMedChem

Praziquantel: mechanisms of action, resistance and new derivatives for schistosomiasis

(2008) Michael J Doenhoff et al.   CURRENT OPINION IN INFECTIOUS DISEASES

Inhibitors of NAD+ Dependent Histone Deacetylases (Sirtuins)

(2008) Manfred Jung et al.   CURRENT PHARMACEUTICAL DESIGN

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

(2008) E Lara et al.   ONCOGENE

A role for the mitochondrial deacetylase Sirt3 in regulating energy homeostasis

(2008) B.-H. Ahn et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA