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

Abstract

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.

• Authors: Nicola Laurieri, Matthew H J Crawford, Akane Kawamura, Isaac M Westwood, James Robinson, Ai M Fletcher, Stephen G Davies, Edith Sim, Angela J Russell
• Journal: Journal of the American Chemical Society (J Am Chem Soc) Vol. 132 Issue 10 Pg. 3238-9 (Mar 17 2010) ISSN: 1520-5126 [Electronic] United States
• PMID: 20170182 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Biomarkers, Tumor
• Isoenzymes
• Arylamine N-Acetyltransferase
• N-acetyltransferase 1
• Nat2 enzyme, mouse

Topics

• Animals
• Arylamine N-Acetyltransferase (analysis, antagonists & inhibitors)
• Biomarkers, Tumor (analysis)
• Breast Neoplasms (enzymology)
• Colorimetry (methods)
• Female
• Humans
• Isoenzymes (analysis, antagonists & inhibitors)
• Mice
• Models, Molecular