Novel small-molecule inhibitors of arylamine N-acetyltransferases: drug discovery by high-throughput screening.


:Arylamine N-acetyltransferases (NATs) are a family of enzymes found in eukaryotes and prokaryotes. While the precise endogenous function of NAT remains unknown for most organisms, recent evidence has shown that the expression of human NAT1 is up-regulated in estrogen receptor positive breast cancer. Additionally, NAT in mycobacteria is required for mycobacterial cell wall biosynthesis and survival of the organisms within macrophage. It is therefore important to develop small molecule inhibitors of NATs as molecular tools to study the function of NATs in various organisms. Such inhibitors may also prove useful in future drug design, for example in the development of anti tubercular agents. We describe a high-throughput screen of a proprietary library of 5016 drug-like compounds against three prokaryotic NAT enzymes and two eukaryotic NAT enzymes.


Westwood IM,Kawamura A,Russell AJ,Sandy J,Davies SG,Sim E




Has Abstract


2011-02-01 00:00:00










BSP/CCHTS/E- Pub/00131




  • Identification of Genes Associated with Lung Adenocarcinoma Prognosis.

    abstract:OBJECTIVE:Lung cancer is the most prevalent cancer in the world, and lung adenocarcinoma is the most common lung cancer subtype. Identification and determination of relevant prognostic markers are the key steps to personalized cancer management. METHODS:We collected the gene expression profiles from 265 tumor tissues ...

    journal_title:Combinatorial chemistry & high throughput screening

    pub_type: 杂志文章


    authors: He ZH,Lv W,Wang LM,Wang YQ,Hu J

    更新日期:2019-01-01 00:00:00

  • Artificial Neural Network Methods Applied to Drug Discovery for Neglected Diseases.

    abstract::Among the chemometric tools used in rational drug design, we find artificial neural network methods (ANNs), a statistical learning algorithm similar to the human brain, to be quite powerful. Some ANN applications use biological and molecular data of the training series that are inserted to ensure the machine learning,...

    journal_title:Combinatorial chemistry & high throughput screening

    pub_type: 杂志文章,评审


    authors: Scotti L,Ishiki H,Mendonça Júnior FJ,da Silva MS,Scotti MT

    更新日期:2015-01-01 00:00:00

  • High throughput automated determination of glutathione based on the formation of a UV-absorbing thioacrylate derivative.

    abstract::Sequential injection analysis (SIA) has been employed as the platform for the development of a high throughput automated assay for glutathione (GSH) in nutrition supplements. The proposed assay is based on the on-line formation of a UV-absorbing thioacrylate derivative (lambda(max) = 285 nm) upon reaction of thiol wit...

    journal_title:Combinatorial chemistry & high throughput screening

    pub_type: 杂志文章


    authors: Zacharis CK,Tzanavaras PD

    更新日期:2010-07-01 00:00:00

  • Synthesis of unsaturated α-acyloxybenzothiazoleamides via the Passerini three-component reaction.

    abstract::4-Benzothiazol-2-ylamino-4-oxo-2-butenoic acid, prepared from reaction of 2-aminobenzothiazole and maleic anhydride, are used as an acid component in Passerini three-component reaction, under solvent-free media, to produce unsaturated α-benzothiazole acyloxyamides in good yields. ...

    journal_title:Combinatorial chemistry & high throughput screening

    pub_type: 杂志文章


    authors: Sheikholeslami-Farahani F,Shahvelayati AS

    更新日期:2013-11-01 00:00:00

  • High throughput electrophysiology with Xenopus oocytes.

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    pub_type: 杂志文章,评审


    authors: Papke RL,Smith-Maxwell C

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  • Accelerating research into bio-based FDCA-polyesters by using small scale parallel film reactors.

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    journal_title:Combinatorial chemistry & high throughput screening

    pub_type: 杂志文章


    authors: Gruter GJ,Sipos L,Adrianus Dam M

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  • Ligand Based-Pharmacophore Modeling and Extended Bi oactivity Prediction for Salinosporamide A, B and C from Marine Actino mycetes Salinispora tropica.

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    pub_type: 杂志文章


    authors: Dineshkumar K,Vasudevan A,Hopper W

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    journal_title:Combinatorial chemistry & high throughput screening

    pub_type: 杂志文章


    authors: Tammen H,Hess R,Schulte I,Kellmann M,Appel A,Budde P,Zucht HD,Schulz-Knappe P

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    pub_type: 杂志文章


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  • Identification of N-Substituted Triazolo-azetidines as Novel Antibacterials using pDualrep2 HTS Platform.

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    pub_type: 杂志文章


    authors: Ivanenkov YA,Yamidanov RS,Osterman IA,Sergiev PV,Aladinskiy VA,Aladinskaya AV,Terentiev VA,Veselov MS,Ayginin AA,Skvortsov DA,Komarova KS,Chemeris AV,Baimiev AK,Sofronova AA,Malyshev AS,Machulkin AE,Petrov RA,Bezrukov D

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    journal_title:Combinatorial chemistry & high throughput screening

    pub_type: 杂志文章,评审


    authors: Besson T,Chosson E

    更新日期:2007-12-01 00:00:00

  • Systematic evaluation of the mechanisms of Mulberry leaf (Morus alba Linne) acting on diabetes based on network pharmacology and molecular docking.

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    journal_title:Combinatorial chemistry & high throughput screening

    pub_type: 杂志文章


    authors: Wu Q,Hu Y

    更新日期:2020-09-13 00:00:00

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    pub_type: 杂志文章


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    journal_title:Combinatorial chemistry & high throughput screening

    pub_type: 杂志文章


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    journal_title:Combinatorial chemistry & high throughput screening

    pub_type: 杂志文章,评审


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    journal_title:Combinatorial chemistry & high throughput screening

    pub_type: 杂志文章


    authors: Liang L,Zhou Q,Hao Z,Wang F,Zhu Y,Lin Q,Gao J

    更新日期:2018-01-01 00:00:00

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    pub_type: 杂志文章


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    更新日期:2019-01-01 00:00:00

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    journal_title:Combinatorial chemistry & high throughput screening

    pub_type: 杂志文章,评审


    authors: Scopelliti PE,Bongiorno G,Milani P

    更新日期:2011-03-01 00:00:00

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    journal_title:Combinatorial chemistry & high throughput screening

    pub_type: 杂志文章,评审


    authors: Zhu J,Wang J,Yu H,Li Y,Hou T

    更新日期:2011-06-01 00:00:00

  • Hadoop-MCC: Efficient Multiple Compound Comparison Algorithm Using Hadoop.

    abstract:AIM AND OBJECTIVE:In the past decade, the drug design technologies have been improved enormously. The computer-aided drug design (CADD) has played an important role in analysis and prediction in drug development, which makes the procedure more economical and efficient. However, computation with big data, such as ZINC c...

    journal_title:Combinatorial chemistry & high throughput screening

    pub_type: 杂志文章


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    更新日期:2018-01-01 00:00:00

  • Application of QSAR Analysis and Different Quantum Chemical Calculation Methods in Activity Evaluation of Selected Fluoroquinolones.

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    journal_title:Combinatorial chemistry & high throughput screening

    pub_type: 杂志文章


    authors: Kawczak P,Bober L,Bączek T

    更新日期:2018-01-01 00:00:00

  • Selective molecularly imprinted polymer obtained from a combinatorial library for the extraction of bisphenol A.

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    pub_type: 杂志文章


    authors: Martin-Esteban A,Tadeo JL

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  • Screening drugs for metabolic stability using pulsed ultrafiltration mass spectrometry.

    abstract::A pulsed ultrafiltration-mass spectrometric screening method has been developed to evaluate the metabolic stability of drugs. Pooled human liver microsomes containing cytochrome P450 enzymes were trapped by an ultrafiltration membrane in a stirred flow-through chamber, and eight beta-blocker drugs including acebutolol...

    journal_title:Combinatorial chemistry & high throughput screening

    pub_type: 杂志文章


    authors: Geun Shin Y,Bolton JL,van Breemen RB

    更新日期:2002-02-01 00:00:00

  • Scutellaria barbata flavonoids improve the composited Aβ-induced abnormal changes of glial cells in rats' brain.

    abstract:AIM:It has been reported that glial cells are involved in Alzheimer's disease (AD). According to our previous research, Scutellaria barbata flavonoids (SBFs) can protect the neuronal disorder and memory impairment for AD-like rats, while the effect of SBFs on the glial cells disorder in AD-like rats has been less well ...

    journal_title:Combinatorial chemistry & high throughput screening

    pub_type: 杂志文章


    authors: Cheng JJ,Guo Q,Wu XG,Ma S,Gao Y,Ya-Zhen S

    更新日期:2020-12-08 00:00:00

  • The Application of High-Throughput Technologies in Precision Diagnosis and Personalized Therapy (Pt III).

    abstract:: ...

    journal_title:Combinatorial chemistry & high throughput screening

    pub_type: 社论


    authors: Huang T

    更新日期:2019-01-01 00:00:00

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    abstract::Trivalent lanthanide ions (Ln(3+)) doped inorganic nanocrystals (NCs) have currently attracted reviving interest and come to the forefront in nanophotonics owing to their potential applications in diverse fields such as luminescent biodetection and bioimaging. As an alternative to conventional biolabels, Ln(3+)-doped ...

    journal_title:Combinatorial chemistry & high throughput screening

    pub_type: 杂志文章,评审


    authors: Ju Q,Tu D,Liu Y,Zhu H,Chen X

    更新日期:2012-08-01 00:00:00

  • Dendrobium officinalis Flower Improves Learning and Reduces Memory Impairment by Mediating Antioxidant Effect and Balancing the Release of Neurotransmitters in Senescent Rats.

    abstract:AIM AND OBJECTIVE:The Dendrobium officinalis flower (DOF) is popular in China due to common belief in its anti-aging properties and positive effects on "nourish yin". However, there have been relatively few confirmatory pharmacological experiments conducted to date. The aim of this work was to evaluate whether DOF has ...

    journal_title:Combinatorial chemistry & high throughput screening

    pub_type: 杂志文章


    authors: Li LZ,Lei SS,Li B,Zhou FC,Chen YH,Su J,Lv GY,Chen SH

    更新日期:2020-01-01 00:00:00

  • Investigation of electrochemical behavior of lipid lowering agent atorvastatin calcium in aqueous media and its determination from pharmaceutical dosage forms and biological fluids using boron-doped diamond and glassy carbon electrodes.

    abstract::The electrochemical behavior of atorvastatin calcium at glassy carbon and boron-doped diamond electrodes has been studied using voltammetric techniques. The possible mechanism of oxidation was discussed with model compounds. The dependence of the peak current and potentials on pH, concentration, scan rate and nature o...

    journal_title:Combinatorial chemistry & high throughput screening

    pub_type: 杂志文章


    authors: Dogan-Topal B,Uslu B,Ozkan SA

    更新日期:2007-08-01 00:00:00

  • Fluorous-enhanced multicomponent reactions for making drug-like library scaffolds.

    abstract::Multicomponent reactions (MCRs) generate multiple bonds in a single reaction process, which is highly efficient to construct relatively complex molecules. Conducting post-MCR modification reactions further increases the molecular complexity and diversity. MCR has become a powerful approach to make drug-like molecules ...

    journal_title:Combinatorial chemistry & high throughput screening

    pub_type: 杂志文章


    authors: Zhang W

    更新日期:2007-03-01 00:00:00

  • Discovery of Potent SARS-CoV-2 Inhibitors from Approved Antiviral Drugs via Docking Screening.

    abstract:BACKGROUND:Corona Virus Disease 2019 (COVID-19) pandemic threatens patients, societies and healthcare systems around the world. There is an emergent need to search for possible medications. OBJECTIVE:This article intends to use virtual screening and molecular docking methods to find potential inhibitors that can respo...

    journal_title:Combinatorial chemistry & high throughput screening

    pub_type: 杂志文章


    authors: Chtita S,Belhassan A,Aouidate A,Belaidi S,Bouachrine M,Lakhlifi T

    更新日期:2020-07-30 00:00:00