title: 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.affiliation: Department of Chemistry, Chemistry Research Laboratory, University of Oxford, Mansfield Road, Oxford, OX1 3TA, UK.
authors.forename: Nicola
authors.initials: N
authors.lastname: Laurieri
authors.forename: Matthew H J
authors.initials: MH
authors.lastname: Crawford
authors.forename: Akane
authors.initials: A
authors.lastname: Kawamura
authors.forename: Isaac M
authors.initials: IM
authors.lastname: Westwood
authors.forename: James
authors.initials: J
authors.lastname: Robinson
authors.forename: Ai M
authors.initials: AM
authors.lastname: Fletcher
authors.forename: Stephen G
authors.initials: SG
authors.lastname: Davies
authors.forename: Edith
authors.initials: E
authors.lastname: Sim
authors.forename: Angela J
authors.initials: AJ
authors.lastname: Russell
mesh_terms: D000818:Animals; D001191:Arylamine N-Acetyltransferase / Q000032:analysis* / Q000037:antagonists & inhibitors; D014408:Biomarkers, Tumor / Q000032:analysis*; D001943:Breast Neoplasms / Q000201:enzymology*; D003124:Colorimetry / Q000379:methods*; D005260:Female; D006801:Humans; D007527:Isoenzymes / Q000032:analysis* / Q000037:antagonists & inhibitors; D051379:Mice; D008958:Models, Molecular
chemical_list: D014408:Biomarkers, Tumor; D007527:Isoenzymes; D001191:Arylamine N-Acetyltransferase; C089384:N-acetyltransferase 1; C524206:Nat2 enzyme, mouse