Small molecule colorimetric probes for specific detection of human arylamine N-acetyltransferase 1, a potential breast cancer biomarker.
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.
Laurieri
Nicola
N
Department of Chemistry, Chemistry Research Laboratory, University of Oxford, Mansfield Road, Oxford, OX1 3TA, UK.
Crawford
Matthew H J
MH
Kawamura
Akane
A
Westwood
Isaac M
IM
Robinson
James
J
Fletcher
Ai M
AM
Davies
Stephen G
SG
Sim
Edith
E
Russell
Angela J
AJ
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
D014408:Biomarkers, Tumor; D007527:Isoenzymes; D001191:Arylamine N-Acetyltransferase; C089384:N-acetyltransferase 1; C524206:Nat2 enzyme, mouse