Abstract
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.
Keywords: Arylamine N-acetyltransferases, NATs, high throughput screening, drug discovery, Amycolatopsis mediterranei, Mycobacterium bovis, Mycobacterium tuberculosis, TBNAT, Salmonella, STNAT, Mycobacterium smegmatis, MSNAT, Pseudomonas aeruginosa, PANAT, Mesorhizobium loti, MLNAT, Mycobacterium marinum, MMNAT, Tecan Sunrise plate reader, basic median-polish mode, Ellman's reagent, pABA, NMR
Combinatorial Chemistry & High Throughput Screening
Title: Novel Small-Molecule Inhibitors of Arylamine N-Acetyltransferases: Drug Discovery by High Throughput Screening
Volume: 14 Issue: 2
Author(s): Isaac M. Westwood, Akane Kawamura, Angela J. Russell, James Sandy, Stephen G. Davies and Edith Sim
Affiliation:
Keywords: Arylamine N-acetyltransferases, NATs, high throughput screening, drug discovery, Amycolatopsis mediterranei, Mycobacterium bovis, Mycobacterium tuberculosis, TBNAT, Salmonella, STNAT, Mycobacterium smegmatis, MSNAT, Pseudomonas aeruginosa, PANAT, Mesorhizobium loti, MLNAT, Mycobacterium marinum, MMNAT, Tecan Sunrise plate reader, basic median-polish mode, Ellman's reagent, pABA, NMR
Abstract: 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.
Export Options
About this article
Cite this article as:
M. Westwood Isaac, Kawamura Akane, J. Russell Angela, Sandy James, G. Davies Stephen and Sim Edith, Novel Small-Molecule Inhibitors of Arylamine N-Acetyltransferases: Drug Discovery by High Throughput Screening, Combinatorial Chemistry & High Throughput Screening 2011; 14 (2) . https://dx.doi.org/10.2174/138620711794474051
DOI https://dx.doi.org/10.2174/138620711794474051 |
Print ISSN 1386-2073 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5402 |
Call for Papers in Thematic Issues
Artificial Intelligence Methods for Biomedical, Biochemical and Bioinformatics Problems
Recently, a large number of technologies based on artificial intelligence have been developed and applied to solve a diverse range of problems in the areas of biomedical, biochemical and bioinformatics problems. By utilizing powerful computing resources and massive amounts of data, methods based on artificial intelligence can significantly improve the ...read more
Eco-friendly Agents for Biological Control of Pathogenic Diseases
The discovery of an alternative biological approach to disease management includes work on medicinal products derived from natural sources as a starting point for the development of eco-friendly agents for these diseases and the injuries they cause, as well as reducing human contact with hazardous chemicals and their residues. We ...read more
Emerging trends in diseases mechanisms, noble drug targets and therapeutic strategies: focus on immunological and inflammatory disorders
Recently infectious and inflammatory diseases have been a key concern worldwide due to tremendous morbidity and mortality world Wide. Recent, nCOVID-9 pandemic is a good example for the emerging infectious disease outbreak. The world is facing many emerging and re-emerging diseases out breaks at present however, there is huge lack ...read more
Exploring Spectral Graph Theory in Combinatorial Chemistry
Scope of the Thematic Issue: Combinatorial chemistry involves the synthesis and analysis of a large number of diverse compounds simultaneously. Traditional methods rely on brute force experimentation, which can be time-consuming and resource-intensive. Spectral Graph Theory, a branch of mathematics dealing with the properties of graphs in relation to the ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Known Triterpenes and their Derivatives as Scaffolds for the Development of New Therapeutic Agents for Cancer
Current Medicinal Chemistry An Insight to Colon Targeted Drug Delivery System
Drug Delivery Letters Accessing the Blood-Brain Barrier to Treat Brain Disorders
Current Nanomedicine Differences and Similarities of Epothilones
Current Cancer Therapy Reviews Human Serum Albumin Conjugated Biomolecules for Cancer Molecular Imaging
Current Pharmaceutical Design How and Why to Screen for CYP2D6 Interindividual Variability in Patients Under Pharmacological Treatments
Current Drug Metabolism Boosting Interleukin-10 Production: Therapeutic Effects and Mechanisms
Current Drug Targets - Immune, Endocrine & Metabolic Disorders Assessment of Ploy Dopamine Coated Fe<sub>3</sub>O<sub>4</sub> Nanoparticles for Melanoma (B16-F10 and A-375) Cells Detection
Anti-Cancer Agents in Medicinal Chemistry Novel Non-Steroidal Anti-Inflammatory Drugs: What we have Learned from Animal Studies
Current Drug Targets - Inflammation & Allergy Anti-Hormonal Therapies for Premenopausal Patients – What did we Learn from the TEXT/SOFT Trials?
Reviews on Recent Clinical Trials Editorial (Thematic Issue: From Gut Inflammation to Gastrointestinal Disorders Current Update on Pathophysiology, Molecular Mechanism and Pharmacological Treatment Modalities)
Current Pharmaceutical Design Postmenopausal Health of Indian Women: A Review
Current Women`s Health Reviews The Role of miR-124 in Drosophila Alzheimer's Disease Model by Targeting Delta in Notch Signaling Pathway
Current Molecular Medicine Monoclonal Antibody-Based Targeted Therapy in Breast Cancer
Current Medicinal Chemistry - Anti-Cancer Agents Dietary Prevention of Cancer: Anticancer and Antiangiogenic Properties of Green Tea Polyphenols
Medicinal Chemistry Reviews - Online (Discontinued) Controlled Drug Delivery Using Microdevices
Current Pharmaceutical Biotechnology VEGF in Tumor Progression and Targeted Therapy
Current Cancer Drug Targets Progress and Prospects of Stem Cells in Treatment of Drug Resistant Tuberculosis
Current Respiratory Medicine Reviews CEACAM1 in Malignant Melanoma: A Diagnostic and Therapeutic Target
Current Topics in Medicinal Chemistry AZT: An Old Drug with New Perspectives
Current Clinical Pharmacology