PNAS: Novel molecular imaging probes from estrogen enzyme substrates
A study published in the April issue of Proceedings of the National Academy of Sciences suggests that molecular imaging probes can be developed from specific substrates for estrogen sulfotransferase.
Estrogen sulfotransferase (SULT1E1) is a key enzyme in estrogen homeostasis, playing a central role in the prevention and development of human disease.
Jorge R. Barrio, PhD, professor of molecular and medical pharmacology at the David Geffen School of Medicine at the University of California, Los Angeles and colleagues tested several 6-hydroxy-2-arylbenzothiazoles and demonstrated excellent affinity and specificity for SULT1E1.
According to Barrio and colleagues, high PET signal was detected in the presence of radiolabeled 11C-(2-[4-(Methylamino) phenyl]-6-hydroxybenzothiazole)-6-O-sulfate using microPET scanning.
Barrio and colleagues concluded that because 2-[4-(Methylamino)phenyl]-6-hydroxybenzothiazole)-6-O-sulfate and other members of the family specific for SULT1E1 can be labeled with carbon-11 or fluorine-18, in vivo assays of SULT1E1 functional activity are now feasible in humans.
Estrogen sulfotransferase (SULT1E1) is a key enzyme in estrogen homeostasis, playing a central role in the prevention and development of human disease.
Jorge R. Barrio, PhD, professor of molecular and medical pharmacology at the David Geffen School of Medicine at the University of California, Los Angeles and colleagues tested several 6-hydroxy-2-arylbenzothiazoles and demonstrated excellent affinity and specificity for SULT1E1.
According to Barrio and colleagues, high PET signal was detected in the presence of radiolabeled 11C-(2-[4-(Methylamino) phenyl]-6-hydroxybenzothiazole)-6-O-sulfate using microPET scanning.
Barrio and colleagues concluded that because 2-[4-(Methylamino)phenyl]-6-hydroxybenzothiazole)-6-O-sulfate and other members of the family specific for SULT1E1 can be labeled with carbon-11 or fluorine-18, in vivo assays of SULT1E1 functional activity are now feasible in humans.