Selective small molecule inhibitors of the potential breast cancer marker, human arylamine N-acetyltransferase 1, and its murine homologue, mouse arylamine N-acetyltransferase 2.

Journal article

The identification, synthesis and evaluation of a series of rhodanine and thiazolidin-2,4-dione derivatives as selective inhibitors of human arylamine N-acetyltransferase 1 and mouse arylamine N-acetyltransferase 2 is described. The most potent inhibitors identified have submicromolar activity and inhibit both the recombinant proteins and human NAT1 in ZR-75 cell lysates in a competitive manner. (1)H NMR studies on purified mouse Nat2 demonstrate that the inhibitors bind within the putative active site of the enzyme.

Authors: Russell, A; Westwood, I; Crawford, M; Robinson, J; Kawamura, A

• Publication status: Published
• Journal: Bioorganic and medicinal chemistry
• Volume: 17
• Issue: 2
• Pages: 905-918
• Publication date: 2009-01-01
• DOI: 10.1016/j.bmc.2008.11.032
• EISSN: 1464-3391
• ISSN: 0968-0896
• Language: English
• Keywords: Enzyme Inhibitors; Humans; Tumor Markers, Biological; Isoenzymes; Rhodanine; Binding Sites; Thiazolidinediones; Breast Neoplasms; Animals; Female; Arylamine N-Acetyltransferase; Mice