(Q38940509)

English

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.

scientific article

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

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22 February 2020

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 (English)

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22 February 2020

Parkinson's disease

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22 February 2020

Michael Sternberg

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22 February 2020

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22 February 2020

Matthew Fuchter

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22 February 2020

Konstantina Koltsida

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22 February 2020

Paolo Di Fruscia

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Paolo Di Fruscia

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22 February 2020

Emmanouil Zacharioudakis

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Emmanouil Zacharioudakis

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22 February 2020

Sasiwan Laohasinnarong

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22 February 2020

Mattaka Khongkow

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22 February 2020

Karin Schmidtkunz

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22 February 2020

Sébastien Moniot

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22 February 2020

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Clemens Steegborn

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22 February 2020

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Chang Liu

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22 February 2020

Christopher R Reynolds

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22 February 2020

Manfred Jung

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22 February 2020

Kathryn L Chapman

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22 February 2020

David T Dexter

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22 February 2020

publication date

13 November 2014

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22 February 2020

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22 February 2020

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22 February 2020

69-82

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22 February 2020

1

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22 February 2020

Molecular evolution of the histone deacetylase family: functional implications of phylogenetic analysis.

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

Histone deacetylases (HDACs): characterization of the classical HDAC family

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

The biochemistry of sirtuins.

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

Recent progress in the biology and physiology of sirtuins

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

Sirtuins: critical regulators at the crossroads between cancer and aging

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

SIRT4 coordinates the balance between lipid synthesis and catabolism by repressing malonyl CoA decarboxylase

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

Sirt5 is a NAD-dependent protein lysine demalonylase and desuccinylase

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

Sirt5 deacylation activities show differential sensitivities to nicotinamide inhibition

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

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

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

Activation of the protein deacetylase SIRT6 by long-chain fatty acids and widespread deacylation by mammalian sirtuins

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

Sirtuins in mammals: insights into their biological function

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

The Sirtuin family: therapeutic targets to treat diseases of aging

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

Biological and potential therapeutic roles of sirtuin deacetylases

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

Are sirtuins viable targets for improving healthspan and lifespan?

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

SirT2 is a histone deacetylase with preference for histone H4 Lys 16 during mitosis

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

SIRT2 regulates adipocyte differentiation through FoxO1 acetylation/deacetylation

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

SIRT2 deacetylates FOXO3a in response to oxidative stress and caloric restriction

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

The human Sir2 ortholog, SIRT2, is an NAD+-dependent tubulin deacetylase

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

SIRT inhibitors induce cell death and p53 acetylation through targeting both SIRT1 and SIRT2.

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

Role for human SIRT2 NAD-dependent deacetylase activity in control of mitotic exit in the cell cycle

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

SIRT2 downregulation confers resistance to microtubule inhibitors by prolonging chronic mitotic arrest

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

Identification of a small molecule SIRT2 inhibitor with selective tumor cytotoxicity

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

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

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

SIRT2 maintains genome integrity and suppresses tumorigenesis through regulating APC/C activity

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

SIRT2 inhibition achieves neuroprotection by decreasing sterol biosynthesis

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

Sir-two-homolog 2 (Sirt2) modulates peripheral myelination through polarity protein Par-3/atypical protein kinase C (aPKC) signaling

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

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

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

Linking SIRT2 to Parkinson's disease.

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

NAD(+) -dependent histone deacetylases (sirtuins) as novel therapeutic targets

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

Mechanism of sirtuin inhibition by nicotinamide: altering the NAD(+) cosubstrate specificity of a Sir2 enzyme

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

Identification of a class of small molecule inhibitors of the sirtuin family of NAD-dependent deacetylases by phenotypic screening

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

Antitumor activity of a small-molecule inhibitor of human silent information regulator 2 enzymes

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

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

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

Sirtuin 2 inhibitors rescue alpha-synuclein-mediated toxicity in models of Parkinson's disease

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

A brain-permeable small molecule reduces neuronal cholesterol by inhibiting activity of sirtuin 2 deacetylase

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

3-(N-arylsulfamoyl)benzamides, inhibitors of human sirtuin type 2 (SIRT2)

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

Structural and synthetic investigations of tanikolide dimer, a SIRT2 selective inhibitor, and tanikolide seco-acid from the Madagascar marine cyanobacterium Lyngbya majuscula

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

Structure-activity studies on splitomicin derivatives as sirtuin inhibitors and computational prediction of binding mode

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

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

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

Design, synthesis, and biological activity of a novel series of human sirtuin-2-selective inhibitors

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

The Discovery of Novel 10,11-Dihydro-5H-dibenz[b,f]azepine SIRT2 Inhibitors.

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

Discovery of thieno[3,2-d]pyrimidine-6-carboxamides as potent inhibitors of SIRT1, SIRT2, and SIRT3

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

Screen of pseudopeptidic inhibitors of human sirtuins 1-3: two lead compounds with antiproliferative effects in cancer cells

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

Development and characterization of 3-(benzylsulfonamido)benzamides as potent and selective SIRT2 inhibitors

1 reference

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21 January 2018

A novel sirtuin 2 (SIRT2) inhibitor with p53-dependent pro-apoptotic activity in non-small cell lung cancer

1 reference

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21 January 2018

Structure-based development of novel sirtuin inhibitors

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

Assessment of a rule-based virtual screening technology (INDDEx) on a benchmark data set.

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

Novel 3-arylideneindolin-2-ones as inhibitors of NAD+ -dependent histone deacetylases (sirtuins).

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

Adenosine mimetics as inhibitors of NAD+-dependent histone deacetylases, from kinase to sirtuin inhibition

1 reference

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21 January 2018

ZINC: a free tool to discover chemistry for biology

1 reference

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21 January 2018

Drug-like properties and the causes of poor solubility and poor permeability

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

Structure of the histone deacetylase SIRT2

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

Development and validation of a genetic algorithm for flexible docking

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

In vitro assays for the determination of histone deacetylase activity

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

New assays and approaches for discovery and design of Sirtuin modulators

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

New substructure filters for removal of pan assay interference compounds (PAINS) from screening libraries and for their exclusion in bioassays

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

Development of a 384-well colorimetric assay to quantify hydrogen peroxide generated by the redox cycling of compounds in the presence of reducing agents

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

Structures of human sirtuin 3 complexes with ADP-ribose and with carba-NAD+ and SRT1720: binding details and inhibition mechanism

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

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

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

Crystal structures of Sirt3 complexes with 4'-bromo-resveratrol reveal binding sites and inhibition mechanism

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

The SWISS-MODEL workspace: a web-based environment for protein structure homology modelling

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

Structure of the Yeast Hst2 Protein Deacetylase in Ternary Complex with 2′-O-Acetyl ADP Ribose and Histone Peptide

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

Structural and Functional Analysis of Human SIRT1

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

Crystal structures of human SIRT3 displaying substrate-induced conformational changes

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

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

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

Inhibition of SIRT2 potentiates the anti-motility activity of taxanes: implications for antineoplastic combination therapies.

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

Epigenetic targeting of histone deacetylase: therapeutic potential in Parkinson's disease?

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

Proteasome inhibition causes nigral degeneration with inclusion bodies in rats

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

Impairment of the ubiquitin-proteasome system causes dopaminergic cell death and inclusion body formation in ventral mesencephalic cultures

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

Nigral degeneration with inclusion body formation and behavioral changes in rats after proteasomal inhibition

1 reference

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21 January 2018

Non-invasive evaluation of nigrostriatal neuropathology in a proteasome inhibitor rodent model of Parkinson's disease

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

Characterization and transplantation of two neuronal cell lines with dopaminergic properties

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

Discovery of potent and selective sirtuin 2 (SIRT2) inhibitors using a fragment-based approach

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

A continuous microplate assay for sirtuins and nicotinamide-producing enzymes

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

Crystal structure analysis of human Sirt2 and its ADP-ribose complex

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

Neutral red uptake assay for the estimation of cell viability/cytotoxicity

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

Prior use of the neutral red assay and reduction of total protein determination in 96-well plate assays.

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

Structure-activity studies on suramin analogues as inhibitors of NAD+-dependent histone deacetylases (sirtuins)

2 references

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

https://api.crossref.org/works/10.1002%2FCMDC.201402431

7 January 2021

based on heuristic

inferred from DOI database lookup

Two-Step Synthesis of Novel, Bioactive Derivatives of the Ubiquitous Cofactor Nicotinamide Adenine Dinucleotide (NAD)

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

21 January 2018

Identification of novel SIRT2-selective inhibitors using a click chemistry approach

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

7 January 2021

based on heuristic

inferred from DOI database lookup

Different effects of intranigral and intrastriatal administration of the proteasome inhibitor lactacystin on typical neurochemical and histological markers of Parkinson's disease in rats.

1 reference

https://api.crossref.org/works/10.1002%2FCMDC.201402431

7 January 2021

based on heuristic

inferred from DOI database lookup

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