The identification, synthesis, and evaluation of a series of naphthoquinone derivatives as selective inhibitors of human arylamine N-acetyltransferase 1 and mouse arylamine N-acetyltransferase 2 are described. The compounds undergo a distinctive color change (red --> blue) upon binding to these human and mouse NAT isoenzymes driven by a proton transfer event. No color change is observed in the presence of functionally distinct but highly similar isoenzymes which are >70% identical. These molecules may be used as sensors to detect the presence of human NAT1 in cell lysates.
Keywords:
Animals
,Arylamine N-Acetyltransferase
,Biomarkers, Tumor
,Breast Neoplasms
,Colorimetry
,Female
,Humans
,Isoenzymes
,Mice
,Models, Molecular