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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.

Type

Journal article

Journal

Comb Chem High Throughput Screen

Publication Date

02/2011

Volume

14

Pages

117 - 124

Keywords

Animals, Anti-Bacterial Agents, Antineoplastic Agents, Arylamine N-Acetyltransferase, Bacteria, Bacterial Infections, Breast Neoplasms, Cricetinae, Drug Discovery, Enzyme Inhibitors, Female, High-Throughput Screening Assays, Humans, Mycobacterium, Mycobacterium Infections, Small Molecule Libraries