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.
journal_name
Comb Chem High Throughput Screenjournal_title
Combinatorial chemistry & high throughput screeningauthors
Westwood IM,Kawamura A,Russell AJ,Sandy J,Davies SG,Sim Edoi
10.2174/138620711794474051subject
Has Abstractpub_date
2011-02-01 00:00:00pages
117-24issue
2eissn
1386-2073issn
1875-5402pii
BSP/CCHTS/E- Pub/00131journal_volume
14pub_type
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journal_title:Combinatorial chemistry & high throughput screening
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