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.
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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 |
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