Small molecule colorimetric probes for specific detection of human arylamine N-acetyltransferase 1, a potential breast cancer biomarker.

Laurieri N, Crawford MHJ, Kawamura A, Westwood IM, Robinson J, Fletcher AM, Davies SG, Sim E, Russell AJ

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

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Arylamine N-Acetyltransferase

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Biomarkers, Tumor

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Breast Neoplasms

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Colorimetry

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Female

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Humans

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Isoenzymes

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Mice

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Models, Molecular