Gene ther
apy holds gre
at promise for the tre
atment of diverse dise
ases, but widespre
ad implement
ationis hindered by difficulties in
assessing the success of tr
ansfection. The development of noninv
asivereporter techniques b
ased on
appropri
ate molecules
and im
aging mod
alities m
ay help to
ass
ay geneexpression. Fluorophenyl-
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D-g
al
actopyr
anosides provide
a novel cl
ass of NMR
active molecules, which
are highly responsive to the
action of
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al
actosid
ase (
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al), the product of the l
acZ gene. The reportermolecules
are st
able in solution
and with respect to wild-type cells, but the enzyme c
auses liber
ationof the
aglycon,
a fluorophenol,
accomp
anied by distinct color form
ation
and
a 19F NMR chemic
al shiftof 5-10 ppm, depending on pH. Synthetic str
ategy, experiment
al methods,
and molecul
ar
and
19FNMR ch
ar
acteristics
are reported for
a series of molecules in solution, blood,
and tumor cells. Thiscl
ass of molecules presents
a new str
ategy for
ass
aying gene expression with
a highly vers
atilemolecul
ar structur
al pl
atform.